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Sample records for 3-methyl-2-benzothiazolinone hydrazone hydrochloride

  1. Simple and sensitive method for the quantification of total bilirubin in human serum using 3-methyl-2-benzothiazolinone hydrazone hydrochloride as a chromogenic probe

    NASA Astrophysics Data System (ADS)

    Nagaraja, Padmarajaiah; Avinash, Krishnegowda; Shivakumar, Anantharaman; Dinesh, Rangappa; Shrestha, Ashwinee Kumar

    2010-11-01

    We here describe a new spectrophotometric method for measuring total bilirubin in serum. The method is based on the cleavage of bilirubin giving formaldehyde which further reacts with diazotized 3-methyl-2-benzothiazolinone hydrazone hydrochloride giving blue colored solution with maximum absorbance at 630 nm. Sensitivity of the developed method was compared with Jendrassik-Grof assay procedure and its applicability has been tested with human serum samples. Good correlation was attained between both methods giving slope of 0.994, intercept 0.015, and R2 = 0.997. Beers law obeyed in the range of 0.068-17.2 μM with good linearity, absorbance y = 0.044 Cbil + 0.003. Relative standard deviation was 0.006872, within day precision ranged 0.3-1.2% and day-to-day precision ranged 1-6%. Recovery of the method varied from 97 to 102%. The proposed method has higher sensitivity with less interference. The obtained product was extracted and was spectrally characterized for structural confirmation with FT-IR, 1H NMR.

  2. Phenoloxidases in ascidian hemocytes: characterization of the pro-phenoloxidase activating system.

    PubMed

    Parrinello, Nicolò; Arizza, Vincenzo; Chinnici, Cinzia; Parrinello, Daniela; Cammarata, Matteo

    2003-08-01

    The phenoloxidase (PO) activity of the hemocytes lysate supernatant from three ascidians species, assayed by means of 3-methyl-2-benzothiazolinone hydrazone hydrochloride, have been compared. PO-containing hemocytes were identified by a cytochemical reaction and the enzymatic activity measured by a spectrophotometric assay of lysate supernatant from hemocyte populations separated on a discontinuous Percoll density gradient. In Styela plicata, the enzyme appeared to be contained in morula cells only. In Ciona intestinalis, PO activity was shown in univacuolar refractile granulocyte and granular hemocyte. In Phallusia mammillata both compartment cell and granular hemocytes were positive. Enzymatic assay following electrophoretic analysis on polyacrylamide gel electrophoresis (PAGE) or SDS-PAGE indicated that hemocyte lysate presented orthodiphenoloxidase (catecholase) activity. The enzymes from the three species differed in molecular size, activating substances and trypsin sensitivity. PMID:12892750

  3. Development and validation of sensitive kinetic spectrophotometric method for the determination of moxifloxacin antibiotic in pure and commercial tablets

    NASA Astrophysics Data System (ADS)

    Ashour, Safwan; Bayram, Roula

    2015-04-01

    New, accurate, sensitive and reliable kinetic spectrophotometric method for the assay of moxifloxacin hydrochloride (MOXF) in pure form and pharmaceutical formulations has been developed. The method involves the oxidative coupling reaction of MOXF with 3-methyl-2-benzothiazolinone hydrazone hydrochloride monohydrate (MBTH) in the presence of Ce(IV) in an acidic medium to form colored product with lambda max at 623 and 660 nm. The reaction is followed spectrophotometrically by measuring the increase in absorbance at 623 nm as a function of time. The initial rate and fixed time methods were adopted for constructing the calibration curves. The linearity range was found to be 1.89-40.0 μg mL-1 for initial rate and fixed time methods. The limit of detection for initial rate and fixed time methods is 0.644 and 0.043 μg mL-1, respectively. Molar absorptivity for the method was found to be 0.89 × 104 L mol-1 cm-1. Statistical treatment of the experimental results indicates that the methods are precise and accurate. The proposed method has been applied successfully for the estimation of moxifloxacin hydrochloride in tablet dosage form with no interference from the excipients. The results are compared with the official method.

  4. Optimized and validated spectrophotometric methods for the determination of nicorandil in drug formulations and biological fluids.

    PubMed

    Rahman, Nafisur; Ahmad Khan, Nadeem; Hejaz Azmi, Syed Najmul

    2004-07-01

    Two simple, sensitive and economical spectrophotometric methods have been developed for the determination of nicorandil in drug formulations and biological fluids. Method A is based on the reaction of the drug with brucine-sulphanilic acid reagent in sulphuric acid medium producing a yellow-coloured product, which absorbs maximally at 410 nm. Method B depends on the formation of the intensely blue-coloured product which results due to the interaction of an electrophilic intermediate of 3-methyl-2-benzothiazolinone hydrazone hydrochloride (MBTH) with oxidized product of 4-(methyl amino) phenol sulphate (metol) in the presence of nicorandil as an oxidizing agent in sulphuric acid medium. The coloured product shows absorbance maximum at 560 nm. Under the optimized experimental conditions, Beer's law is obeyed in the concentration range of 2.5-35.0 and 0.40-2.2 microg ml(-1) for Methods A and B, respectively. Both the methods have been successfully applied to the determination of nicorandil in drug formulations and biological fluids. The results are validated statistically and through recovery studies. In order to establish the bias and the performance of the proposed methods, the point and interval hypothesis tests have been performed. The experimental true bias of all samples is smaller than +/-2%. PMID:15231427

  5. A novel use of oxidative coupling reactions for determination of some statins (cholesterol-lowering drugs) in pharmaceutical formulations

    NASA Astrophysics Data System (ADS)

    Ashour, Safwan; Bahbouh, Mahmoud; Khateeb, Mouhammed

    2011-03-01

    New, accurate and reliable spectrophotometric methods for the assay of three statin drugs, atorvastatin calcium (AVS), fluvastatin sodium (FVS) and pravastatin sodium (PVS) in pure form and pharmaceutical formulations have been described. All methods involve the oxidative coupling reaction of AVS, FVS and PVS with 3-methyl-2-benzothiazolinone hydrazone hydrochloride monohydrate (MBTH) in the presence of Ce(IV) in an acidic medium to form colored products with λmax at 566, 615 and 664 nm, respectively. Beer's law was obeyed in the ranges of 2.0-20.0, 4.9-35.4 and 7.0-30.0 μg mL -1 for AVS-MBTH, FVS-MBTH and PVS-MBTH, respectively. Molar absorptivities for the above three methods were found to be 3.24 × 10 4, 1.05 × 10 4 and 0.68 × 10 4 L mol -1 cm -1, respectively. Statistical treatment of the experimental results indicates that the methods are precise and accurate. The proposed methods have been applied to the determination of the components in commercial forms with no interference from the excipients. A comparative study between the suggested procedures and the official methods for these compounds in the commercial forms showed no significant difference between the two methods.

  6. A review exploring biological activities of hydrazones

    PubMed Central

    Verma, Garima; Marella, Akranth; Shaquiquzzaman, Mohammad; Akhtar, Mymoona; Ali, Mohammad Rahmat; Alam, Mohammad Mumtaz

    2014-01-01

    The development of novel compounds, hydrazones has shown that they possess a wide variety of biological activities viz. antimicrobial, anticonvulsant, antidepressant, anti-inflammatory, analgesic, antiplatelet, antimalarial, anticancer, antifungal, antitubercular, antiviral, cardio protective etc., Hydrazones/azomethines/imines possess-NHN = CH- and constitute an important class of compounds for new drug development. A number of researchers have synthesized and evaluated the biological activities of hydrazones. This review aims at highlighting the diverse biological activities of hydrazones. PMID:24741273

  7. Glucosamine hydrochloride

    MedlinePlus

    ... or it can be made in the laboratory. Glucosamine hydrochloride is one of several forms of glucosamine. It ... as supplements. These products may contain glucosamine sulfate, glucosamine hydrochloride, or N-acetyl-glucosamine. These different chemicals have ...

  8. Glucosamine hydrochloride

    MedlinePlus

    ... sulfate. People take glucosamine hydrochloride by mouth for osteoarthritis, rheumatoid arthritis, glaucoma, a jaw disorder called temporomandibular ... with chondroitin sulfate, shark cartilage, and camphor for osteoarthritis. Glucosamine hydrochloride is used parenterally and short-term ...

  9. Hydrolytic Stability of Hydrazones and Oximes**

    PubMed Central

    Kalia, Jeet; Raines, Ronald T.

    2009-01-01

    Hydrazones and oximes are common conjugates, but are labile to hydrolysis. The hydrolytic stability of isostructural hydrazones and an oxime have been determined at pD 5.0–9.0. The hydrolysis of each adduct was catalyzed by acid. Rate constants for oxime hydrolysis were nearly 103-fold lower than those for simple hydrazones; a trialkylhydrazonium ion (formed after condensation) was even more stable than the oxime. The data suggest a general mechanism for conjugate hydrolysis. PMID:18712739

  10. A note concerning acetate activation of peroxidative activity of catalases using 2,2'-azino-bis(3-ethylbenzthiazoline)-6-sulfonic acid as a substrate.

    PubMed

    Baker, Warren L; Key, Christopher; Lonergan, Greg T

    2005-01-01

    Beef liver catalases showed peroxidative activity using 2,2'-azino-bis-(3-ethylbenzthiazoline)-6-sulfonic acid as the electron donor and hydrogen peroxide as the acceptor at a pH of 5. This activity was not observed at pH 7. The reaction depended on acetate concentration, although succinate and propionate could partly replace the acetate as a catalyst. Other haem proteins also catalyzed a peroxidative effect. The reaction using syringaldazine or the coupling between dimethylaminobenzoic acid and 3-methyl-2-benzothiazolinone hydrazone was less effective and less sensitive. Evidence is presented that the reaction is associated with a conformational change of the catalase. PMID:15932252

  11. Ultrastructural and Immunocytochemical Studies on the H2O2-Producing Enzyme Pyranose Oxidase in Phanerochaete chrysosporium Grown under Liquid Culture Conditions

    PubMed Central

    Daniel, Geoffrey; Volc, Jindrich; Kubatova, Elena; Nilsson, Thomas

    1992-01-01

    The ultrastructural distribution of the sugar-oxidizing enzyme pyranose 2-oxidase (POD) in hyphae of Phanerochaete chrysosporium K-3 grown under liquid culture conditions optimal for the enzyme's production was studied by transmission electron microscopy immunocytochemistry. Using the 3-dimethylaminobenzoic acid-3-methyl-2-benzothiazolinone hydrazone hydrochloride H2O2 peroxidase spectrophotometric assay, POD was detected in mycelial extracts from days 7 to 18, with maximum activity recorded on day 12. Onset of POD activity occurred in the secondary phase of hyphal development at a time of stationary growth, glucose limitation, and pH increase. POD was also detected extracellularly in the culture fluid from days 7 to 18, with maximum activity recorded on day 13. At early stages of development (3 to 4 days), using anti-POD antibodies and immunogold labeling, POD was localized in multivesicular and electron-dense bodies and in cell membrane regions. After 10 to 12 days of growth, at maximum POD activity, POD was concentrated within the periplasmic space where it was associated with membrane-bound vesicles and other membrane structures. At later stages of development (17 to 18 days), when the majority of hyphae were lysed, POD was observed associated with residual intracellular membrane systems and vesicles. Transmission electron microscopy immunocytochemical studies also demonstrated an extracellular distribution of the enzyme at the stationary growth phase, showing its association with fungal extracellular slime. In studies of ligninolytic cultures of the same fungus, POD was found to have a similar intracellular and extracellular distribution in slime as that recorded for cultures grown with cornsteep. POD's peripheral cytoplasmic distribution shows similarities to the cellular distribution of that reported previously for H2O2-dependent lignin and manganese peroxidases in P. chrysosporium. Images PMID:16348809

  12. Therapeutic Potential of Hydrazones as Anti-Inflammatory Agents

    PubMed Central

    Bala, Suman; Sharma, Neha; Saini, Vipin

    2014-01-01

    Hydrazones are a special class of organic compounds in the Schiff base family. Hydrazones constitute a versatile compound of organic class having basic structure (R1R2C=NNR3R4). The active centers of hydrazone, that is, carbon and nitrogen, are mainly responsible for the physical and chemical properties of the hydrazones and, due to the reactivity toward electrophiles and nucleophiles, hydrazones are used for the synthesis of organic compound such as heterocyclic compounds with a variety of biological activities. Hydrazones and their derivatives are known to exhibit a wide range of interesting biological activities like antioxidant, anti-inflammatory, anticonvulsant, analgesic, antimicrobial, anticancer, antiprotozoal, antioxidant, antiparasitic, antiplatelet, cardioprotective, anthelmintic, antidiabetic, antitubercular, trypanocidal, anti-HIV, and so forth. The present review summarizes the efficiency of hydrazones as potent anti-inflammatory agents. PMID:25383223

  13. Lucanthone hydrochloride

    PubMed Central

    Blair, D. M.

    1958-01-01

    This review of the published work on the treatment of bilharziasis with lucanthone hydrochloride draws attention to the inconclusive nature of many of the trials carried out so far: either the dosage was inadequate or the patients were not followed up for a sufficient length of time. The author stresses the importance of obtaining a high concentration of lucanthone in the body fluids. He suggests that better results might be obtained if the total dose were given in two days or even as a single, massive dose. This method might also reduce the side effects, which do not appear, as a rule, until the second or third day. PMID:13573122

  14. Hydrazones as Singular Reagents in Asymmetric Organocatalysis.

    PubMed

    de Gracia Retamosa, María; Matador, Esteban; Monge, David; Lassaletta, José M; Fernández, Rosario

    2016-09-12

    This Minireview summarizes strategies and developments regarding the use of hydrazones as reagents in asymmetric organocatalysis, their distinct roles in nucleophile-electrophile, cycloaddition, and cyclization reactions. The key structural elements governing the reactivity of these reagents in a preferred pathway will be discussed, as well as their different interactions with organocatalysts, leading to diverse activation modes. Along these studies, the synthetic equivalence of N-monoalkyl, N,N-dialkyl, and N-acyl hydrazones with several synthons is also highlighted. Emphasis is also put on the mechanistic studies performed to understand the observed reactivities. Finally, the functional group transformations performed from the available products has also been analyzed, highlighting the synthetic value of these methodologies, which served to access numerous families of valuable multifunctional compounds and nitrogen-containing heterocycles. PMID:27552942

  15. Bupropion Hydrochloride.

    PubMed

    Khan, S R; Berendt, R T; Ellison, C D; Ciavarella, A B; Asafu-Adjaye, E; Khan, M A; Faustino, P J

    2016-01-01

    Bupropion hydrochloride is a norepinephrine-dopamine disinhibitor (NDDI) approved for the treatment of depression and smoking cessation. Bupropion is a trimethylated monocyclic phenylaminoketone second-generation antidepressant, which differs structurally from most antidepressants, and resides in a novel mechanistic class that has no direct action on the serotonin system. Comprehensive chemical, physical, and spectroscopic profiles are presented. This analytical profile provides an extensive spectroscopic investigation utilizing mass spectrometry, one- and two-dimensional NMR, solid-state NMR, IR, NIR, Raman, UV, and X-ray diffraction. The profile also includes significant wet chemistry studies for pH, solubility, solution, and plasma stability. Both HPLC and UPLC methodology are presented for bupropion and its related impurities or major metabolites. The profile concludes with an overview of biological properties that includes toxicity, drug metabolism, and pharmacokinetics. PMID:26940167

  16. Colesevelam hydrochloride.

    PubMed

    Steinmetz, Karen L

    2002-05-15

    The pharmacology, pharmacodynamics, clinical efficacy, drug interactions, adverse effects, and dosage and administration of colesevelam hydrochloride are reviewed. Colesevelam hydrochloride is a nonabsorbed lipid-lowering agent approved for use alone or in combination with hydroxymethylglutaryl-coenzyme A (HMG-CoA) reductase inhibitors for the reduction of low-density-lipoprotein (LDL) cholesterol in patients with primary hypercholesterolemia. Colesevelam forms nonabsorbable complexes with bile acids in the gastrointestinal (GI) tract, resulting in changes in plasma lipid levels, including total, LDL, and high-density-lipoprotein cholesterol and triglycerides. Colesevelam has been reported to be four to six times as potent as traditional bile acid sequestrants (BASs), perhaps because of its greater binding affinity for glycocholic acid. Unlike cholestyramine and colestipol, colesevelam appears to reduce LDL cholesterol in a dose-dependent manner. In clinical trials, colesevelam demonstrated efficacy either alone or in combination with HMG-CoA reductase inhibitors in the treatment of primary hypercholesterolemia. Combination therapy appeared to be more effective than monotherapy. Although infection, headache, and GI adverse effects have been reported for colesevelam, the rates do not differ significantly from those occurring with placebo. The constipation that typically hinders compliance with traditional BASs is minimal. In one study, the rate of compliance with colesevelam was 93%. There is little evidence of clinically significant interactions involving colesevelam. The maintenance dosage is three 625-mg tablets twice daily or six tablets once daily, taken with meals. Colesevelam provides an effective alternative to cholestyramine and colestipol while offering the potential for fewer adverse effects and better compliance. Studies are needed to directly compare colesevelam with traditional BASs. PMID:12040732

  17. Biomimetic Modeling of Copper Complexes: A Study of Enantioselective Catalytic Oxidation on D-(+)-Catechin and L-( − )-Epicatechin with Copper Complexes

    PubMed Central

    Mutti, Francesco G.; Pievo, Roberta; Sgobba, Maila; Gullotti, Michele; Santagostini, Laura

    2008-01-01

    The biomimetic catalytic oxidations of the dinuclear and trinuclear copper(II) complexes versus two catechols, namely, D-(+)-catechin and L-( − )-epicatechin to give the corresponding quinones are reported. The unstable quinones were trapped by the nucleophilic reagent, 3-methyl-2-benzothiazolinone hydrazone (MBTH), and have been calculated the molar absorptivities of the different quinones. The catalytic efficiency is moderate, as inferred by kinetic constants, but the complexes exhibit significant enantio-differentiating ability towards the catechols, albeit for the dinuclear complexes, this enantio-differentiating ability is lower. In all cases, the preferred enantiomeric substrate is D-(+)-catechin to respect the other catechol, because of the spatial disposition of this substrate. PMID:18825268

  18. Study and characterization of polyphenol oxidase from eggplant (Solanum melongena L.).

    PubMed

    Todaro, Aldo; Cavallaro, Rosalinda; Argento, Sergio; Branca, Ferdinando; Spagna, Giovanni

    2011-10-26

    In this study the catecholase and cresolase activities of eggplant polyphenol oxidase (PPO) were investigated. Enzyme activity was determined by measuring the increase in absorbance using catechol as substrate and 3-methyl-2-benzothiazolinone hydrazone (MBTH) as coupled reagent. The effects of substrate specificity, heat inactivation, temperature, pH, and inhibitors were investigated to understand the enzymatic alteration of ready-to-eat preparations. Browning of vegetables was determined through a colorimeter. Decrease of lightness (L*) and increase of color difference values (ΔE*) were correlated with tissue browning. Antibrowning agents were tested on PPO under the same conditions. The enzyme activity was strongly inhibited by 0.4 M citric acid. Under natural pH conditions, the enzyme was also inhibited by tartaric acid and acetic acid. All of the results were used to understand the best conditions for food transformation (ready-to-eat and grilled eggplant slices). PMID:21942648

  19. Netupitant and Palonosetron Hydrochloride

    Cancer.gov

    This page contains brief information about netupitant and palonosetron hydrochloride and a collection of links to more information about the use of this combination drug, research results, and ongoing clinical trials.

  20. Trifluridine and Tipiracil Hydrochloride

    Cancer.gov

    This page contains brief information about trifluridine and tipiracil hydrochloride and a collection of links to more information about the use of this combination drug, research results, and ongoing clinical trials.

  1. QSAR studies of hydrazone uncouplers of oxidative phosphorylation.

    PubMed

    Winkler, D A; Holan, G; Smith, D R; Middleton, E J; Hart, N K; Rihs, K; Smith, K W

    1988-07-01

    Semiempirical molecular orbital calculations have been performed on a series of hydrazone uncouplers of mitochondrial oxidative phosphorylation which show insecticidal activity. Regression analysis yielded significant correlations between uncoupling activity, insecticidal potency and such physicochemical or theoretically-derived parameters as lipophilicity, pKa and atom charges. PMID:3255329

  2. Drug release from hydrazone-containing peptide amphiphiles.

    PubMed

    Matson, John B; Stupp, Samuel I

    2011-07-28

    Hydrolytically-labile hydrazones in peptide amphiphiles were studied as degradable tethers for release of the drug nabumetone from nanofiber gels. On-resin addition of the novel compound tri-Boc-hydrazido adipic acid to a lysine ε-amine allowed for precise placement of a hydrazide in a peptide sequence. PMID:21674107

  3. Drug release from hydrazone-containing peptide amphiphiles

    SciTech Connect

    Matson, John B.; Stupp, Samuel I.

    2012-03-15

    Hydrolytically-labile hydrazones in peptide amphiphiles were studied as degradable tethers for release of the drug nabumetone from nanofiber gels. On-resin addition of the novel compound tri-Boc-hydrazido adipic acid to a lysine E-amine allowed for precise placement of a hydrazide in a peptide sequence.

  4. Antimalarial Activity of Small-Molecule Benzothiazole Hydrazones.

    PubMed

    Sarkar, Souvik; Siddiqui, Asim A; Saha, Shubhra J; De, Rudranil; Mazumder, Somnath; Banerjee, Chinmoy; Iqbal, Mohd S; Nag, Shiladitya; Adhikari, Susanta; Bandyopadhyay, Uday

    2016-07-01

    We synthesized a new series of conjugated hydrazones that were found to be active against malaria parasite in vitro, as well as in vivo in a murine model. These hydrazones concentration-dependently chelated free iron and offered antimalarial activity. Upon screening of the synthesized hydrazones, compound 5f was found to be the most active iron chelator, as well as antiplasmodial. Compound 5f also interacted with free heme (KD [equilibrium dissociation constant] = 1.17 ± 0.8 μM), an iron-containing tetrapyrrole released after hemoglobin digestion by the parasite, and inhibited heme polymerization by parasite lysate. Structure-activity relationship studies indicated that a nitrogen- and sulfur-substituted five-membered aromatic ring present within the benzothiazole hydrazones might be responsible for their antimalarial activity. The dose-dependent antimalarial and heme polymerization inhibitory activities of the lead compound 5f were further validated by following [(3)H]hypoxanthine incorporation and hemozoin formation in parasite, respectively. It is worth mentioning that compound 5f exhibited antiplasmodial activity in vitro against a chloroquine/pyrimethamine-resistant strain of Plasmodium falciparum (K1). We also evaluated in vivo antimalarial activity of compound 5f in a murine model where a lethal multiple-drug-resistant strain of Plasmodium yoelii was used to infect Swiss albino mice. Compound 5f significantly suppressed the growth of parasite, and the infected mice experienced longer life spans upon treatment with this compound. During in vitro and in vivo toxicity assays, compound 5f showed minimal alteration in biochemical and hematological parameters compared to control. In conclusion, we identified a new class of hydrazone with therapeutic potential against malaria. PMID:27139466

  5. Menthone aryl acid hydrazones: a new class of anticonvulsants.

    PubMed

    Jain, Jainendra; Kumar, Y; Sinha, Reema; Kumar, Rajeev; Stables, James

    2011-01-01

    A series of ten compounds (Compounds J(1)-J(10)) of (±) 3-menthone aryl acid hydrazone was synthesized and characterized by thin layer chromatography and spectral analysis. Synthesized compounds were evaluated for anticonvulsant activity after intraperitoneal (i.p) administration to mice by maximal electroshock (MES) and subcutaneous pentylenetetrazole (scPTZ) induced seizure method and minimal clonic seizure test. Minimal motor impairment was also determined for these compounds. Results obtained showed that four compounds out of ten afforded significant protection in the minimal clonic seizure screen at 6 Hz. Compound J(6), 4-Chloro-N-(2-isopropyl-5-methylcyclohexylidene) benzohydrazide was found to be the most active compound with MES ED(50) of 16.1 mg/kg and protective index (pI) of greater than 20, indicating that (±) 3-menthone aryl acid hydrazone possesses better and safer anticonvulsant properties than other reported menthone derivatives viz. menthone Schiff bases, menthone semicarbazides and thiosemicarbazides. PMID:21235520

  6. Antioxidant activity of hydrazones with sterically hindered phenol fragments

    NASA Astrophysics Data System (ADS)

    Nikolaevskii, A. N.; Kniga, O. P.; Khizhan, E. I.; Tikhonova, G. A.; Vinogradov, V. V.; Khizhan, A. I.

    2012-12-01

    Kinetic parameters of the antiradical activity of derivatives of hydrazones of 4-hydroxy-3,5-di- tert-butyl-benzaldehyde are determined photocolorimetrically in their reactions with a stable diphenylpicrylhydrazyl radical, and by chemiluminescence from the capture of peroxide radicals upon the initiated oxidation of ethylbenzene. It is found that during inhibited oxidation, the reactive centers (N-H and O-H) in hetaryl- and acylhydrazone molecules operate in parallel. Regularities of the compounds' inhibiting effect are studied in heterogeneous systems upon the initiated oxidation of ethylbenzene in emulsion, and in a water-lipid model of the oxidation of phosphatidylcholine dispersion. It is established that hydrazone derivatives are antioxidants of combined action in heterophase processes of the oxidation of unsaturated substrates, displaying properties of hydroperoxide deactivators in addition to their antiradical activity.

  7. Transition metal complexes of an isatinic quinolyl hydrazone

    PubMed Central

    2011-01-01

    Background The importance of the isatinic quinolyl hydrazones arises from incorporating the quinoline ring with the indole ring in the same compound. Quinoline ring has therapeutic and biological activities. On the other hand, isatin (1H-indole-2,3-dione) and its derivatives exhibit a wide range of biological activities. Also, the indole ring occurs in Jasmine flowers and Orange blossoms. Recently, the physiological and biological activities of quinolyl hydrazones arise from their tendency to form metal chelates with transition metal ions. In this context, we have reported to isolate, characterize and study the biological activity of some transition metal complexes of an isatinic quinolyl hydrazone; 3-[2-(4-methyl quinolin-2-yl)hydrazono] indolin-2-one. Results Mono- and binuclear as well as dimeric chelates were obtained from the reaction of a new isatinic quinolyl hydrazone with Fe(III), Co(II), Ni(II), Cu(II), VO(II) and Pd(II) ions. The ligand showed a variety of modes of bonding viz. (NNO)2-, (NO)- and (NO) per each metal ion supporting its ambidentate and flexidentate characters. The mode of bonding and basicity of the ligand depend mainly on the type of the metal cation and its counter anion. All the obtained Pd(II)- complexes have the preferable square planar geometry (D4h- symmetry) and depend mainly on the mole ratio (M:L). Conclusion The effect of the type of the metal ion for the same anion (Cl-) is obvious from either structural diversity of the isolated complexes (Oh, Td and D4h) or the various modes of bonding. The isatinic hydrazone uses its lactim form in all complexes (Cl-) except complex 5 (SO42-) in which it uses its lactam form. The obtained Pd(II)- complexes (dimeric, mono- and binuclear) are affected by the mole ratio (M:L) and have the square planar (D4h) geometry. Also, the antimicrobial activity is highly influenced by the nature of the metal ion and the order for S. aureus bacteria is as follows: Nickel(II) > Vanadyl(II) > Cobalt

  8. Mutagenic activity of cytostatic methyl hydrazones with different strains of Salmonella typhimurium.

    PubMed

    Gericke, D; Braun, R; Dittmar, W

    1979-07-11

    Experiments are performed to ascertain the mutagenic properties of four new cytostatic methyl-hydrazones in the Ames test using different strains of Salmonella typhimurium. As could be demonstrated all four hydrazones are mutagenic per se without a metabolic activation through rat liver microsomes (S-9 fraction). Whereas the beta-chloroethyl hydrazones B1 and B2 cause a base-pair substitution with the strains TA100 and TA1535 the methyl-hydrazones EB4 and CyB4 both cause base-pair substitution with TA100 and frameshift mutation with TA98. At both strains the mutagenic activity of Cy84 ist powerful. Furthermore, no relation could be detected between the mutagenic properties of the methyl-hydrazones and their alkylating behaviour on 4-(4-nitrobenzyl)-pyridine. PMID:383045

  9. Ligand substitution reactions of a phenolic quinolyl hydrazone; oxidovanadium (IV) complexes

    PubMed Central

    2011-01-01

    Background Quinoline ring has therapeutic and biological activities. Quinolyl hydrazones constitute a class of excellent chelating agents. Recently, the physiological and biological activities of quinolyl hydrazones arise from their tendency to form metal chelates with transition metal ions. In this context, we have aimed to study the competency effect of a phenolic quinolyl hydrazone (H2L; primary ligand) with some auxiliary ligands (Tmen, Phen or Oxine; secondary ligands) towards oxidovanadium (IV) ions. Results Mono- and binuclear oxidovanadium (IV) - complexes were obtained from the reaction of a phenolic quinolyl hydrazone with oxidovanadium (IV)- ion in absence and presence of N,N,N',N'- tetramethylethylenediamine (Tmen), 1,10-phenanthroline (Phen) or 8-hydroxyquinoline (Oxine). The phenolic quinolyl hydrazone ligand behaves as monobasic bidentate (NO- donor with O- bridging). All the obtained complexes have the preferable octahedral geometry except the oxinato complex (2) which has a square pyramid geometry with no axial interaction; the only homoleptic complex in this study. Conclusion The ligand exchange (substitution/replacement) reactions reflect the strong competency power of the auxiliary aromatic ligands (Phen/Oxine) compared to the phenolic quinolyl hydrazone (H2L) towards oxidovanadium (IV) ion; (complexes 2 and 3). By contrast, in case of the more flexible aliphatic competitor (Tmen), an adduct was obtained (4). The obtained complexes reflect the strength of the ligand field towards the oxidovanadium (IV)- ion; Oxine or Phen >> phenolic hydrazone (H2L) > Tmen. PMID:21846387

  10. Novel dehydrogenase catalyzes oxidative hydrolysis of carbon-nitrogen double bonds for hydrazone degradation.

    PubMed

    Itoh, Hideomi; Suzuta, Tetsuya; Hoshino, Takayuki; Takaya, Naoki

    2008-02-29

    Hydrazines and their derivatives are versatile artificial and natural compounds that are metabolized by elusive biological systems. Here we identified microorganisms that assimilate hydrazones and isolated the yeast, Candida palmioleophila MK883. When cultured with adipic acid bis(ethylidene hydrazide) as the sole source of carbon, C. palmioleophila MK883 degraded hydrazones and accumulated adipic acid dihydrazide. Cytosolic NAD+- or NADP+-dependent hydrazone dehydrogenase (Hdh) activity was detectable under these conditions. The production of Hdh was inducible by adipic acid bis(ethylidene hydrazide) and the hydrazone, varelic acid ethylidene hydrazide, under the control of carbon catabolite repression. Purified Hdh oxidized and hydrated the C=N double bond of acetaldehyde hydrazones by reducing NAD+ or NADP+ to produce relevant hydrazides and acetate, the latter of which the yeast assimilated. The deduced amino acid sequence revealed that Hdh belongs to the aldehyde dehydrogenase (Aldh) superfamily. Kinetic and mutagenesis studies showed that Hdh formed a ternary complex with the substrates and that conserved Cys is essential for the activity. The mechanism of Hdh is similar to that of Aldh, except that it catalyzed oxidative hydrolysis of hydrazones that requires adding a water molecule to the reaction catalyzed by conventional Aldh. Surprisingly, both Hdh and Aldh from baker's yeast (Ald4p) catalyzed the Hdh reaction as well as aldehyde oxidation. Our findings are unique in that we discovered a biological mechanism for hydrazone utilization and a novel function of proteins in the Aldh family that act on C=N compounds. PMID:18096698

  11. Photochemistry of phenazopyridine hydrochloride.

    PubMed

    Iqbal, J; Gupta, A; Husain, A

    2006-09-01

    Phenazopyridine hydrochloride (1) is an azo dye with local analgesic and anaesthetic effects on the urinary tract. Its photochemistry was studied in different reaction media including the drug adsorbed on silica gel. This resulted in photochemical cyclodehydrogenation, reductive photodegradation and rearrangement of the drug molecule. Four major products were isolated and identified on the basis of IR, NMR and mass spectral studies. The products are: pyrido[3,4-c]cinnoline-2,4-diamine (2), N3-phenylpyridine-2,3,4,6-tetraamine (3), pyridine-2,3,6-triamine (4), 2,6-diamino-1-(4-aminophenyl)pyridin-4(1H)-one (5). PMID:17020148

  12. Structural and spectroscopic investigation on a new potentially bioactive di-hydrazone containing thiophene heterocyclic rings

    NASA Astrophysics Data System (ADS)

    Nogueira, Vanessa de S.; Ramalho Freitas, Maria Clara; Cruz, Wellington S.; Ribeiro, Tatiana S.; Resende, Jackson A. L. C.; Rey, Nicolás A.

    2016-02-01

    Hydrazones and several substituted hydrazones are associated with a broad spectrum of biological activities, as well as compounds containing the thiophene ring. In this context, a novel di-hydrazone derived from 2-thiophenecarboxylic acid hydrazide was synthesized and completely characterized by elemental analysis, XRD, FT-IR, Raman and UV-Vis spectroscopies, thermogravimetry, 1H NMR, 1H-1H COSY and 1H-1H ROESY. A preliminary in silico pharmacological evaluation was also performed in order to assess the performance of the new compound regarding some molecular properties relevant for a drug's pharmacokinetics in the human body.

  13. Structural studies of PCU-hydrazones: NMR spectroscopy, X-ray diffractions, and DFT calculations

    NASA Astrophysics Data System (ADS)

    Veljković, Jelena; Šekutor, Marina; Molčanov, Krešimir; Lo, Rabindranath; Ganguly, Bishwajit; Mlinarić-Majerski, Kata

    2011-06-01

    In this article we present a detailed structural investigation for the configurational isomers of PCU-hydrazones. The structural characterization of these hydrazones was performed using NMR spectroscopy, X-ray diffraction analysis and theoretical calculations. The single crystal X-ray structures of PCU-hydrazones 6B and 6C have been solved and used to conclusively confirm the characterization obtained via NMR spectra of a particular isomer. Nuclear magnetic shielding values calculated for 6A-C using DFT calculations were correlated with the experimentally determined chemical shifts. The computed results were found to be in good agreement with the observed 13C NMR values. The computed NMR results helped to ascertain the isomers of PCU-hydrazones 4A-C.

  14. The antibacterial activity of some sulfonamides and sulfonyl hydrazones, and 2D-QSAR study of a series of sulfonyl hydrazones

    NASA Astrophysics Data System (ADS)

    Aslan, H. Güzin; Özcan, Servet; Karacan, Nurcan

    2012-12-01

    Benzenesulfonicacid-1-methylhydrazide (1) and its four aromatic sulfonyl hydrazone derivatives (1a-1d), N-(3-amino-2-hydroxypropyl)benzene sulfonamide (2) and N-(2-hydroxyethyl)benzenesulfonamide (3) were synthesized and their structures were determined by IR, 1H NMR, 13C NMR, and LCMS techniques. Antibacterial activities of new synthesized compounds were evaluated against various bacteria strains by microdilution and disk diffusion methods. The experimental results show that presence of OH group on sulfonamides reduces the antimicrobial activity, and antimicrobial activities of the sulfonyl hydrazones (1a-1d) are smaller than that of the parent sulfonamide (1), except Candida albicans. In addition, 2D-QSAR analysis was performed on 28 aromatic sulfonyl hydrazones as antimicrobial agents against Escherichia coli and Staphylococcus aureus. In the QSAR models, the most important descriptor is total point-charge component of the molecular dipole for E. coli, and partial negative surface area (PNSA-1) for S. aureus.

  15. 21 CFR 522.1222b - Ketamine hydrochloride with promazine hydrochloride and aminopentamide hydrogen sulfate injection.

    Code of Federal Regulations, 2011 CFR

    2011-04-01

    ... hydrochloride and aminopentamide hydrogen sulfate injection. 522.1222b Section 522.1222b Food and Drugs FOOD AND... hydrochloride with promazine hydrochloride and aminopentamide hydrogen sulfate injection. (a) Chemical name... hydrochloride, 10- phenothiazine monohydrochloride, and aminopentamide hydrogen sulfate. (b) Specifications....

  16. 21 CFR 522.1222b - Ketamine hydrochloride with promazine hydrochloride and aminopentamide hydrogen sulfate injection.

    Code of Federal Regulations, 2013 CFR

    2013-04-01

    ... hydrochloride and aminopentamide hydrogen sulfate injection. 522.1222b Section 522.1222b Food and Drugs FOOD AND... hydrochloride with promazine hydrochloride and aminopentamide hydrogen sulfate injection. (a) Chemical name... hydrochloride, 10- phenothiazine monohydrochloride, and aminopentamide hydrogen sulfate. (b) Specifications....

  17. 21 CFR 522.1222b - Ketamine hydrochloride with promazine hydrochloride and aminopentamide hydrogen sulfate injection.

    Code of Federal Regulations, 2012 CFR

    2012-04-01

    ... hydrochloride and aminopentamide hydrogen sulfate injection. 522.1222b Section 522.1222b Food and Drugs FOOD AND... hydrochloride with promazine hydrochloride and aminopentamide hydrogen sulfate injection. (a) Chemical name... hydrochloride, 10- phenothiazine monohydrochloride, and aminopentamide hydrogen sulfate. (b) Specifications....

  18. 21 CFR 522.1222b - Ketamine hydrochloride with promazine hydrochloride and aminopentamide hydrogen sulfate injection.

    Code of Federal Regulations, 2010 CFR

    2010-04-01

    ... hydrochloride and aminopentamide hydrogen sulfate injection. 522.1222b Section 522.1222b Food and Drugs FOOD AND... hydrochloride with promazine hydrochloride and aminopentamide hydrogen sulfate injection. (a) Chemical name... hydrochloride, 10- phenothiazine monohydrochloride, and aminopentamide hydrogen sulfate. (b) Specifications....

  19. 21 CFR 582.5875 - Thiamine hydrochloride.

    Code of Federal Regulations, 2010 CFR

    2010-04-01

    ... DRUGS, FEEDS, AND RELATED PRODUCTS SUBSTANCES GENERALLY RECOGNIZED AS SAFE Nutrients and/or Dietary Supplements 1 § 582.5875 Thiamine hydrochloride. (a) Product. Thiamine hydrochloride. (b) Conditions of...

  20. 21 CFR 582.5676 - Pyridoxine hydrochloride.

    Code of Federal Regulations, 2013 CFR

    2013-04-01

    ... 21 Food and Drugs 6 2013-04-01 2013-04-01 false Pyridoxine hydrochloride. 582.5676 Section 582.5676 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED... Dietary Supplements 1 § 582.5676 Pyridoxine hydrochloride. (a) Product. Pyridoxine hydrochloride....

  1. 21 CFR 582.5676 - Pyridoxine hydrochloride.

    Code of Federal Regulations, 2014 CFR

    2014-04-01

    ... 21 Food and Drugs 6 2014-04-01 2014-04-01 false Pyridoxine hydrochloride. 582.5676 Section 582.5676 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED... Dietary Supplements 1 § 582.5676 Pyridoxine hydrochloride. (a) Product. Pyridoxine hydrochloride....

  2. 21 CFR 582.5676 - Pyridoxine hydrochloride.

    Code of Federal Regulations, 2011 CFR

    2011-04-01

    ... 21 Food and Drugs 6 2011-04-01 2011-04-01 false Pyridoxine hydrochloride. 582.5676 Section 582.5676 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED... Dietary Supplements 1 § 582.5676 Pyridoxine hydrochloride. (a) Product. Pyridoxine hydrochloride....

  3. 21 CFR 582.5676 - Pyridoxine hydrochloride.

    Code of Federal Regulations, 2012 CFR

    2012-04-01

    ... 21 Food and Drugs 6 2012-04-01 2012-04-01 false Pyridoxine hydrochloride. 582.5676 Section 582.5676 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED... Dietary Supplements 1 § 582.5676 Pyridoxine hydrochloride. (a) Product. Pyridoxine hydrochloride....

  4. Synthesis, spectroscopic characterizations, crystal structures and DFT studies of nalidixic acid carbonyl hydrazones derivatives

    NASA Astrophysics Data System (ADS)

    Bergamini, F. R. G.; Ribeiro, M. A.; Lancellotti, M.; Machado, D.; Miranda, P. C. M. L.; Cuin, A.; Formiga, A. L. B.; Corbi, P. P.

    2016-09-01

    This article describes the synthesis and characterization of the 1-ethyl-7-methyl-4-oxo-1,4-dihydro-1,8-naphthyridine-3-carbohydrazide (hzd) and six carbonyl hydrazones derivatives of the nalidixic with 1H-pyrrol-2-ylmethylidene (hpyrr), 1H-imidazol-2-ylmethylidene (h2imi), pyridin-2-ylmethylidene (h2py), pyridin-3-ylmethylidene (h3py), pyridin-4-ylmethylidene(h4py) and (2-hydroxyphenyl)methylidene (hsali). The carbonyl hydrazones were characterized by elemental and ESI-QTOF-MS analyses, IR and detailed NMR spectroscopic measurements. The 2D NMR experiments allowed the unambiguous assignment of the hydrogen, carbon and nitrogen atoms, which have not been reported for nalidixic acid carbonyl hydrazone derivatives so far. Crystal structures of hzd and the new carbonyl hydrazones h2imi, hpyrr and h3py were determined by X-ray diffraction studies. Although the synthesis of hzd was reported decades ago, the hzd crystal structure have not been reported yet. Geometric optimizations of all the characterized structures were performed with the aid of DFT studies. Despite the fact that the hydrazones with 2-pyridine carboxylic acid (h2py) and salicyl aldehyde (hsali) were already reported by literature, a detailed spectroscopic study followed by DFT studies are also reported for such compounds in this manuscript. Antimicrobial studies of the compounds are also presented.

  5. The tautomerization between keto- to phenol-hydrazone induced by anions in the solution

    NASA Astrophysics Data System (ADS)

    Shang, Xuefang; Yuan, Jianmei; Wang, Yingling; Zhang, Jinlian; Xu, Xiufang

    2012-02-01

    Two simple anion receptors, 2-[(2-hydroxy-5-nitrophenyl)methylene]hydrazone (1) and 2-[(3,5-dibromo-2-hydroxyphenyl)methylene]hydrazone (2) with -OH binding sites, were synthesized and characterized. The anion binding ability of receptors 1 and 2 with halide anions (F-, Cl-, Br- and I-), AcO- and HPO4- was investigated using visual (naked-eye), UV-vis titration experiments in dry DMSO together with DFT theoretical calculation. The addition of F-, AcO- and HPO4- to the host solution resulted in a red shift of the charge-transfer absorbance band accompanied by a color change from yellow to orange in the naked-eye experiments. Receptor 1 containing a nitro group at the para position and receptor 2 containing two bromine groups at the ortho and para positions both showed strong binding ability for HPO4- ion in the form of phenol-hydrazone. Moreover, receptor 1, induced by anion species in the solution, converted to the form of phenol-hydrazone from keto-hydrazone.

  6. Synthesis and antibacterial activity against ralstonia solanacearum for novel hydrazone derivatives containing a pyridine moiety

    PubMed Central

    2012-01-01

    Background Ralstonia solanacearum, one of the most important bacterial diseases on plants, is a devastating, soil-borne plant pathogen with a global distribution and an unusually wide host range. In order to discover new bioactive molecules and pesticides acting on tobacco bacterial wilt, we sought to combine the active structure of hydrazone and pyridine together to design and synthesize a series of novel hydrazone derivatives containing a pyridine moiety. Results A series of hydrazone derivatives containing a pyridine moiety were synthesized. Their structures were characterized by 1 H-NMR, 13 C-NMR, IR, and elemental analysis. The preliminary biological activity tests showed that compound 3e and 3g exhibited more than 80% activity against Ralstonia solanacearum at 500 mg/L, especially compound 3g displayed relatively good activity to reach 57.0% at 200 mg/L. Conclusion A practical synthetic route to hydrazone derivatives containing a pyridine moiety by the reaction of intermediates 2 with different aldehydes in ethanol at room temperature using 2-chloronicotinic acid and 2-amino-5-chloro-3-methylbenzoic acid as start materials is presented. This study suggests that the hydrazone derivatives containing a substituted pyridine ring could inhibit the growth of Ralstonia solanacearum. PMID:22483270

  7. Synthesis and biological evaluation of hydrazone derivatives as antifungal agents.

    PubMed

    Casanova, Bruna B; Muniz, Mauro N; de Oliveira, Thayse; de Oliveira, Luís Flavio; Machado, Michel M; Fuentefria, Alexandre M; Gosmann, Grace; Gnoatto, Simone C B

    2015-01-01

    Emerging yeasts are among the most prevalent causes of systemic infections with high mortality rates and there is an urgent need to develop specific, effective and non-toxic antifungal agents to respond to this issue. In this study 35 aldehydes, hydrazones and hydrazines were obtained and their antifungal activity was evaluated against Candida species (C. parapsilosis, C. tropicalis, C. krusei, C. albicans, C. glabrata and C. lusitaneae) and Trichosporon asahii, in an in vitro screening. The minimum inhibitory concentrations (MICs) of the active compounds in the screening was determined against 10 clinical isolates of C. parapsilosis and 10 of T. asahii. The compounds 4-pyridin-2-ylbenzaldehyde] (13a) and tert-butyl-(2Z)-2-(3,4,5-trihydroxybenzylidine)hydrazine carboxylate (7b) showed the most promising MIC values in the range of 16-32 μg/mL and 8-16 μg/mL, respectively. The compounds' action on the stability of the cell membrane and cell wall was evaluated, which suggested the action of the compounds on the fungal cell membrane. Cell viability of leukocytes and an alkaline comet assay were performed to evaluate the cytotoxicity. Compound 13a was not cytotoxic at the active concentrations. These results support the discovery of promising candidates for the development of new antifungal agents. PMID:26007181

  8. Radical additions to chiral hydrazones: stereoselectivity and functional group compatibility.

    PubMed

    Friestad, Gregory K

    2012-01-01

    Free radical additions to imino compounds offer increased synthetic accessibility of chiral amines, but lack of general methods for stereocontrol has hindered their development. This review focuses on two asymmetric amine synthesis strategies designed to address this problem, with emphasis on addition of functionalized radicals which may facilitate applications to synthesis of complex targets. First, chiral N-acylhydrazones are acceptors for intermolecular radical additions of a wide range of primary, secondary, and tertiary alkyl halides to the C=N bond, with radicals generated under manganese-, tin-, or boron-mediated conditions. A variety of aldehydes and ketones serve as viable precursors for the chiral hydrazones, and the highly stereoselective reactions tolerate electrophilic functionality in both coupling components. Second, radical precursors may be linked to chiral α-hydroxyhydrazones via a silicon tether to the hydroxyl group; conformational constraints impart stereocontrol during 5-exo radical cyclization under stannyl- or thiyl-mediated conditions. The silicon tether may later be removed to reveal the formal adducts of hydroxymethyl, vinyl, acetyl, and 2-oxoethyl radicals to the C=N bond. Methodology development and applications to biologically important targets are discussed. PMID:21842359

  9. Ruthenium(II) hydrazone Schiff base complexes: Synthesis, spectral study and catalytic applications

    NASA Astrophysics Data System (ADS)

    Manikandan, R.; Viswanathamurthi, P.; Muthukumar, M.

    2011-12-01

    Ruthenium(II) hydrazone Schiff base complexes of the type [RuCl(CO)(B)(L)] (were B = PPh 3, AsPh 3 or Py; L = hydrazone Schiff base ligands) were synthesized from the reactions of hydrazone Schiff base ligand (obtained from isonicotinoylhydrazide and different hydroxy aldehydes) with [RuHCl(CO)(EPh 3) 2(B)] (where E = P or As; B = PPh 3, AsPh 3 or Py) in 1:1 molar ratio. All the new complexes have been characterized by analytical and spectral (FT-IR, electronic, 1H, 13C and 31P NMR) data. They have been tentatively assigned an octahedral structure. The synthesized complexes have exhibited catalytic activity for oxidation of benzyl alcohol to benzaldehyde and cyclohexanol to cyclohexanone in the presence of N-methyl morpholine N-oxide (NMO) as co-oxidant. They were also found to catalyze the transfer hydrogenation of aliphatic and aromatic ketones to alcohols in KOH/Isopropanol.

  10. Supramolecular arrangement in mono and bi-camphor acyl hydrazones: A structural study

    NASA Astrophysics Data System (ADS)

    Galvão, Adelino M.; Carvalho, M. Fernanda N. N.; Ferreira, Ana S. D.

    2016-03-01

    New acyl hydrazones were synthesized by condensation with camphorquinone aiming at extending the range of applications of the biologically active camphor compounds and structural studies by XRD, 1H-NMR and IR were used in conjunction with advanced computational methodologies to understand the new structural chemistry enabled by the conjugation of the camphor ketone group to the hydrazone Ndbnd C double bond. In particular, were analysed supramolecular arrangements either by hydrogen bonding to water molecules or electrostatic interactions with non protic solvents. The relative stability of all conformers (E/Z) prompted by the hydrazone bond was addressed by state of the art methods such as CR-CCSD(T) and their inter-conversion in both S0 and S1 by CR-EOM-CCSD(T).

  11. Tridentate hydrazone metal complexes derived from cephalexin and 2-hydrazinopyridine: Synthesis, characterization and antibacterial activity

    NASA Astrophysics Data System (ADS)

    Anacona, J. R.; Rincones, Maria

    2015-04-01

    Metal(II) coordination compounds of a tridentate hydrazone ligand (HL) derived from the condensation of cephalexin antibiotic with 2-hydrazinopyridine were synthesized. The hydrazone ligand and mononuclear [ML(OAc)(H2O)] (M(II) = Mn, Co, Ni, Cu, Zn, Ag) complexes were characterized by several techniques, including elemental and thermal analysis, molar conductance and magnetic susceptibility measurements, electronic, FT-IR, EPR and 1H NMR spectral studies. The cephalexin 2-pyridinylhydrazone ligand HL behaves as a monoanionic tridentate NNO chelating agent. The biological applications of complexes have been studied on three bacteria strains (Escherichia coli, Acinetobacter baumannii and Enterococcus faecalis) by agar diffusion disc method.

  12. Synthesis, characterization and biological evaluation of some 5-methylpyrazine carbohydrazide based hydrazones.

    PubMed

    Ahmad, Mushtaq; Hameed, Shahid; Tahir, Muhammad Nawaz; Israr, Muhammad; Anwar, Muhammad; Shah, Muhammad Abdullah Shah Abdullah; Khan, Shad Ali; Din, Ghiasud

    2016-05-01

    Pyrazine carbohydrazide based hydrazones were synthesized starting from 5-methylpyrazine-2-carboxylic acid. The acid was first converted to its methyl ester, which on further treatment with hydrazine hydrate transformed to carbohydrazide. The carbohydrazide was treated with differently substituted aromatic carbonyl compounds giving hydrazones. Characterization of the synthesized compounds was carried out using modern spectroscopic techniques and unambiguously confirmed through X-ray crystallographic studies of compound 3d. The purity of the compounds was verified using elemental analysis. The target molecules were evaluated for urease inhibition, antioxidant and antimicrobial activity. PMID:27166526

  13. Tridentate hydrazone metal complexes derived from cephalexin and 2-hydrazinopyridine: synthesis, characterization and antibacterial activity.

    PubMed

    Anacona, J R; Rincones, Maria

    2015-04-15

    Metal(II) coordination compounds of a tridentate hydrazone ligand (HL) derived from the condensation of cephalexin antibiotic with 2-hydrazinopyridine were synthesized. The hydrazone ligand and mononuclear [ML(OAc)(H2O)] (M(II)=Mn, Co, Ni, Cu, Zn, Ag) complexes were characterized by several techniques, including elemental and thermal analysis, molar conductance and magnetic susceptibility measurements, electronic, FT-IR, EPR and (1)H NMR spectral studies. The cephalexin 2-pyridinylhydrazone ligand HL behaves as a monoanionic tridentate NNO chelating agent. The biological applications of complexes have been studied on three bacteria strains (Escherichia coli, Acinetobacter baumannii and Enterococcus faecalis) by agar diffusion disc method. PMID:25677531

  14. Asymmetric Synthesis of 2-Substituted Azetidin-3-ones via Metalated SAMP/RAMP Hydrazones.

    PubMed

    Pancholi, Alpa K; Geden, Joanna V; Clarkson, Guy J; Shipman, Michael

    2016-09-01

    2-Substituted azetidin-3-ones can be prepared in good yields and enantioselectivities (up to 85% ee) by a one-pot procedure involving the metalation of the SAMP/RAMP hydrazones of N-Boc-azetidin-3-one, reaction with a wide range of electrophiles, including alkyl, allyl, and benzyl halides and carbonyl compounds, followed by hydrolysis using oxalic acid. PMID:27447363

  15. POLYSTYRENE SULFONIC ACID CATALYZED GREENER SYNTHESIS OF HYDRAZONES IN AQUEOUS MEDIUM USING MICROWAVES

    EPA Science Inventory

    An environmentally benign aqueous protocol for the synthesis of cyclic, bi-cyclic, and heterocyclic hydrazones using polystyrene sulfonic acid (PSSA) as a catalyst has been developed; the simple reaction proceeds efficiently in water in the absence of any organic solvent under mi...

  16. Conformational analysis of 2 -diphenylacetyl- 1,3 - indandione- 1 -hydrazone and its derivatives

    NASA Astrophysics Data System (ADS)

    Partridge, Ashton C.; Charlesworth, John M.

    1991-10-01

    Conformational analysis in solution of 2-diphenylacetyl-1,3-indandione-1-hydrazone (DI- PAIN, 1) and its derivatives was achieved by NMR, FT-IR and fluorescence spectroscopy. The spectral evidence indicates that the enamine tautomer is the only isomeric form adopted in solution.

  17. Diastereoselective addition of Grignard reagents to α-epoxy N-sulfonyl hydrazones.

    PubMed

    Uteuliyev, Maulen M; Nguyen, Thien T; Coltart, Don M

    2015-12-01

    The α-alkylation of ketones and their derivatives by the addition of their corresponding enolates to alkyl halides is a fundamental synthetic transformation, but its utility is limited because the key bond-forming step proceeds in a bimolecular nucleophilic substitution fashion. Here we describe how an umpolung strategy that involves the addition of Grignard reagents to α-epoxy N-sulfonyl hydrazones-directed by the alkoxide of the 1-azo-3-alkoxy propenes formed in situ via base-induced ring opening of the epoxide-leads to the syn-selective production of α-alkyl-β-hydroxy N-sulfonyl hydrazones with α-quaternary centres. This transformation is remarkable in its ability to incorporate an unprecedented range of carbon-based substituents, which include primary, secondary and tertiary alkyl, as well as alkenyl, aryl, allenyl and alkynyl groups. Subsequent hydrolysis of the β-hydroxy N-sulfonyl hydrazone products produces the corresponding β-hydroxy ketones. In addition to hydrolysis, the hydrazone products are poised to undergo numerous different known synthetic transformations via well-established chemistry, which would provide access to a wide array of useful structures. PMID:26587719

  18. Synthesis, characterization and antitumor activities of some steroidal derivatives with side chain of 17-hydrazone aromatic heterocycle.

    PubMed

    Cui, Jianguo; Liu, Liang; Zhao, Dandan; Gan, Chunfang; Huang, Xin; Xiao, Qi; Qi, Binbin; Yang, Lei; Huang, Yanmin

    2015-03-01

    Here a series of dehydroepiandrosterone-17-hydrazone and estrone-17-hydrazone derivatives possessing various aromatic heterocycle structures in 17-side chain of their steroidal nucleus were synthesized and their structures were evaluated. The antiproliferative activity of synthesized compounds against some cancer cells was investigated. The results have demonstrated that some dehydroepiandrosterone-17-hydrazone derivatives show distinct antiproliferative activity against some cancer cells through inducing cancer cell apoptosis, and compound 8 with a quinoline structure in 17-side chain displays excellent antiproliferative activity in vitro against SGC 7901 cancer cell (human gastric carcinoma) with an IC50 value of 1 μM. In addition, estrone-17-hydrazone derivatives having a key feature of indole group in the structure showed a special obvious cytotoxicity against HeLa cells, but almost inactive against other cells. The information obtained from the studies is valuable for the design of novel steroidal chemotherapeutic drugs. PMID:25578734

  19. Tetradentate metal complexes derived from cephalexin and 2,6-diacetylpyridine bis(hydrazone): Synthesis, characterization and antibacterial activity.

    PubMed

    Anacona, J R; Rangel, Victor; Loroño, Marcos; Camus, Juan

    2015-10-01

    Metal(II) coordination compounds of a hydrazone ligand (HL) derived from the condensation of cephalexin antibiotic with 2,6-diacetylpyridine bis(hydrazone) were synthesized. The hydrazone ligand and mononuclear [ML(H2O)2][PF6] (M(II)=Mn, Co, Ni, Zn) complexes were characterized by several techniques, including elemental and thermal analysis, molar conductance and magnetic susceptibility measurements, electronic, FT-IR, EPR and (1)H NMR spectral studies. The cephalexin 2,6-diacetylpyridine bis(hydrazone) ligand HL behaves as a monoanionic tetradentate NNNO chelating agent. The biological applications of complexes have been studied on two bacteria strains (Escherichia coli and Staphylococcus aureus) by agar diffusion disc method. PMID:25942081

  20. Tetradentate metal complexes derived from cephalexin and 2,6-diacetylpyridine bis(hydrazone): Synthesis, characterization and antibacterial activity

    NASA Astrophysics Data System (ADS)

    Anacona, J. R.; Rangel, Victor; Loroño, Marcos; Camus, Juan

    2015-10-01

    Metal(II) coordination compounds of a hydrazone ligand (HL) derived from the condensation of cephalexin antibiotic with 2,6-diacetylpyridine bis(hydrazone) were synthesized. The hydrazone ligand and mononuclear [ML(H2O)2][PF6] (M(II) = Mn, Co, Ni, Zn) complexes were characterized by several techniques, including elemental and thermal analysis, molar conductance and magnetic susceptibility measurements, electronic, FT-IR, EPR and 1H NMR spectral studies. The cephalexin 2,6-diacetylpyridine bis(hydrazone) ligand HL behaves as a monoanionic tetradentate NNNO chelating agent. The biological applications of complexes have been studied on two bacteria strains (Escherichia coli and Staphylococcus aureus) by agar diffusion disc method.

  1. Density functional theory studies on the nano-scaled composites consisted of graphene and acyl hydrazone molecules

    NASA Astrophysics Data System (ADS)

    Ren, J. L.; Zhou, L.; Lv, Z. C.; Ding, C. H.; Wu, Y. H.; Bai, H. C.

    2016-07-01

    Graphene, which is the first obtained single atomic layer 2D materials, has drawn a great of concern in nano biotechnology due to the unique property. On one hand, acyl hydrazone compounds belonging to the Schif bases have aroused considerable attention in medicine, pharmacy, and analytical reagent. However, few understanding about the interaction between graphene and acyl hydrazone molecules is now available. And such investigations are much crucial for the applications of these new nano-scaled composites. The current work revealed theoretical investigations on the nano-scaled composites built by acyl hydrazone molecules loaded on the surface of graphene. The relative energy, electronic property and the interaction between the counterparts of graphene/acyl hydrazone composites are investigated based on the density functional theory calculations. According to the obtained adsorption energy, the formation of the nano-scaled composite from the isolated graphene and acyl hydrazone molecule is exothermic, and thus it is energetically favorable to form these nano composites in viewpoint of total energy change. The frontier molecular orbital for the nano composite is mainly distributed at the graphene part, leading to that the energy levels of the frontier molecular orbital of the nano composites are very close to that of isolated graphene. Moreover, the counterpart interaction for the graphene/acyl hydrazone composites is also explored based on the discussions of orbital hybridization, charge redistribution and Van der Waals interaction.

  2. 21 CFR 556.410 - Metoserpate hydrochloride.

    Code of Federal Regulations, 2012 CFR

    2012-04-01

    ... 21 Food and Drugs 6 2012-04-01 2012-04-01 false Metoserpate hydrochloride. 556.410 Section 556.410 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL... Tolerances for Residues of New Animal Drugs § 556.410 Metoserpate hydrochloride. A tolerance of 0.02 part...

  3. 21 CFR 556.350 - Levamisole hydrochloride.

    Code of Federal Regulations, 2012 CFR

    2012-04-01

    ... 21 Food and Drugs 6 2012-04-01 2012-04-01 false Levamisole hydrochloride. 556.350 Section 556.350 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL... Tolerances for Residues of New Animal Drugs § 556.350 Levamisole hydrochloride. A tolerance of 0.1 part...

  4. 21 CFR 556.410 - Metoserpate hydrochloride.

    Code of Federal Regulations, 2013 CFR

    2013-04-01

    ... 21 Food and Drugs 6 2013-04-01 2013-04-01 false Metoserpate hydrochloride. 556.410 Section 556.410 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL... Tolerances for Residues of New Animal Drugs § 556.410 Metoserpate hydrochloride. A tolerance of 0.02 part...

  5. 21 CFR 556.350 - Levamisole hydrochloride.

    Code of Federal Regulations, 2013 CFR

    2013-04-01

    ... 21 Food and Drugs 6 2013-04-01 2013-04-01 false Levamisole hydrochloride. 556.350 Section 556.350 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL... Tolerances for Residues of New Animal Drugs § 556.350 Levamisole hydrochloride. A tolerance of 0.1 part...

  6. 21 CFR 556.350 - Levamisole hydrochloride.

    Code of Federal Regulations, 2014 CFR

    2014-04-01

    ... 21 Food and Drugs 6 2014-04-01 2014-04-01 false Levamisole hydrochloride. 556.350 Section 556.350 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL... Tolerances for Residues of New Animal Drugs § 556.350 Levamisole hydrochloride. A tolerance of 0.1 part...

  7. 21 CFR 556.410 - Metoserpate hydrochloride.

    Code of Federal Regulations, 2014 CFR

    2014-04-01

    ... 21 Food and Drugs 6 2014-04-01 2014-04-01 false Metoserpate hydrochloride. 556.410 Section 556.410 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL... Tolerances for Residues of New Animal Drugs § 556.410 Metoserpate hydrochloride. A tolerance of 0.02 part...

  8. 21 CFR 556.410 - Metoserpate hydrochloride.

    Code of Federal Regulations, 2011 CFR

    2011-04-01

    ... 21 Food and Drugs 6 2011-04-01 2011-04-01 false Metoserpate hydrochloride. 556.410 Section 556.410 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL... Tolerances for Residues of New Animal Drugs § 556.410 Metoserpate hydrochloride. A tolerance of 0.02 part...

  9. 21 CFR 556.350 - Levamisole hydrochloride.

    Code of Federal Regulations, 2011 CFR

    2011-04-01

    ... 21 Food and Drugs 6 2011-04-01 2011-04-01 false Levamisole hydrochloride. 556.350 Section 556.350 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL... Tolerances for Residues of New Animal Drugs § 556.350 Levamisole hydrochloride. A tolerance of 0.1 part...

  10. LC-UV/MS methods for the analysis of prochelator-boronyl salicylaldehyde isonicotinoyl hydrazone (BSIH) and its active chelator salicylaldehyde isonicotinoyl hydrazone (SIH).

    PubMed

    Bureš, Jan; Jansová, Hana; Stariat, Ján; Filipský, Tomáš; Mladěnka, Přemysl; Šimůnek, Tomáš; Kučera, Radim; Klimeš, Jiří; Wang, Qin; Franz, Katherine J; Kovaříková, Petra

    2015-02-01

    Salicylaldehyde isonicotinoyl hydrazone (SIH) is an intracellular iron chelator with well documented potential to protect against oxidative injury both in vitro and in vivo. However, it suffers from short biological half-life caused by fast hydrolysis of the hydrazone bond. Recently, a concept of boronate prochelators has been introduced as a strategy that might overcome these limitations. This study presents two complementary analytical methods for detecting the prochelator-boronyl salicylaldehyde isonicotinoyl hydrazone-BSIH along with its active metal-binding chelator SIH in different solution matrices and concentration ranges. An LC-UV method for determination of BSIH and SIH in buffer and cell culture medium was validated over concentrations of 7-115 and 4-115 μM, respectively, and applied to BSIH activation experiments in vitro. An LC-MS assay was validated for quantification of BSIH and SIH in plasma over the concentration range of 0.06-23 and 0.24-23 μM, respectively, and applied to stability studies in plasma in vitro as well as analysis of plasma taken after i.v. administration of BSIH to rats. A Zorbax-RP bonus column and mobile phases containing either phosphate buffer with EDTA or ammonium formate and methanol/acetonitrile mixture provided suitable conditions for the LC-UV and LC-MS analysis, respectively. Samples were diluted or precipitated with methanol prior to analysis. These separative analytical techniques establish the first validated protocols to investigate BSIH activation by hydrogen peroxide in multiple matrices, directly compare the stabilities of the prochelator and its chelator in plasma, and provide the first basic pharmacokinetic data of this prochelator. Experiments reveal that BSIH is stable in all media tested and is partially converted to SIH by H2O2. The observed integrity of BSIH in plasma samples from the in vivo study suggests that the concept of prochelation might be a promising strategy for further development of

  11. LC-UV/MS methods for the analysis of prochelator - boronyl salicylaldehyde isonicotinoyl hydrazone (BSIH) and its active chelator salicylaldehyde isonicotinoyl hydrazone (SIH)

    PubMed Central

    Bureš, Jan; Jansová, Hana; Stariat, Ján; Filipský, Tomáš; Mladěnka, Přemysl; Šimůnek, Tomáš; Kučera, Radim; Klimeš, Jiří; Wang, Qin; Franz, Katherine J.; Kovaříková, Petra

    2015-01-01

    Salicylaldehyde isonicotinoyl hydrazone (SIH) is an intracellular iron chelator with well documented potential to protect against oxidative injury both in vitro and in vivo. However, it suffers from short biological half-life caused by fast hydrolysis of the hydrazone bond. Recently, a concept of boronate prochelators has been introduced as a strategy that might overcome these limitations. This study presents two complementary analytical methods for detecting the prochelator BSIH (boronyl salicylaldehyde isonicotinoyl hydrazone) along with its active metal-binding chelator SIH in different solution matrices and concentration ranges. An LC-UV method for determination of BSIH and SIH in buffer and cell culture medium was validated over concentrations of 7 – 115 and 4 – 115 μM, respectively, and applied to BSIH activation experiments in vitro. An LC-MS assay was validated for quantification of BSIH and SIH in plasma over the concentration range of 0.06 – 23 and 0.24 – 23 μM, respectively, and applied to stability studies in plasma in vitro as well as analysis of plasma taken after i.v. administration of BSIH to rats. A Zorbax-RP bonus column and mobile phases containing either phosphate buffer with EDTA or ammonium formate and methanol/acetonitrile mixture provided suitable conditions for the LC-UV and LC-MS analysis, respectively. Samples were diluted or precipitated with methanol prior to analysis. These separative analytical techniques establish the first validated protocols to investigate BSIH activation by hydrogen peroxide in multiple matrices, directly compare the stabilities of the prochelator and chelator in plasma, and provide the first basic pharmacokinetic data of this prochelator. Experiments reveal that BSIH is stable in all media tested and is partially converted to SIH by H2O2. The observed integrity of BSIH in plasma samples from the in vivo study suggest that the concept of prochelation might be a promising strategy for further development

  12. 21 CFR 522.883 - Etorphine hydrochloride injection.

    Code of Federal Regulations, 2013 CFR

    2013-04-01

    ... milliliter of etorphine hydrochloride injection, veterinary, contains 1 mg of etorphine hydrochloride in... use the drug unless diprenorphine hydrochloride injection, veterinary, as provided for in § 522.723, is available for use in reversing the effects of etorphine hydrochloride injection, veterinary....

  13. 21 CFR 522.883 - Etorphine hydrochloride injection.

    Code of Federal Regulations, 2012 CFR

    2012-04-01

    ... milliliter of etorphine hydrochloride injection, veterinary, contains 1 mg of etorphine hydrochloride in... use the drug unless diprenorphine hydrochloride injection, veterinary, as provided for in § 522.723, is available for use in reversing the effects of etorphine hydrochloride injection, veterinary....

  14. Spectroscopic and theoretical study of the o-vanillin hydrazone of the mycobactericidal drug isoniazid

    NASA Astrophysics Data System (ADS)

    González-Baró, Ana C.; Pis-Diez, Reinaldo; Parajón-Costa, Beatriz S.; Rey, Nicolás A.

    2012-01-01

    A complete and detailed study of the hydrazone obtained from condensation of antituberculous isoniazid (hydrazide of the isonicotinic acid, INH) and o-vanillin (2-hydroxy-3-methoxybenzaldehyde, o-HVa) is performed. It includes structural and spectroscopic analyses, comparing experimental and theoretical results. The compound was obtained as a chloride of the pyridinic salt (INHOVA +Cl -) but it will be referred as INHOVA for the sake of simplicity. The conformational space was searched and optimized geometries were determined both in gas phase and including solvent effects. Vibrational (IR and Raman), electronic and NMR spectra were registered and assigned with the help of computational methods based on the Density Functional Theory. Isoniazid hydrazones are good candidates for therapeutic agents against tuberculosis with conserved efficiency and lower toxicity and resistance than parent INH.

  15. Antibacterial, antifungal and antimycobacterial activities of some pyrazoline, hydrazone and chalcone derivatives.

    PubMed

    Evranos-Aksöz, Begüm; Onurdağ, Fatma Kaynak; Özgacar, Selda Özgen

    2015-07-01

    Twenty-seven previously reported chalcones and their pyrazoline and hydrazone derivatives as well as two further chalcones have been screened for their antimicrobial, antifungal and antimycobacterial activities against standard microbial strains and drug resistant isolates. The minimum inhibitory concentration (MIC) value of each compound was determined by a two-fold serial microdilution technique. The compounds were found to possess a broad spectrum of antimicrobial activities with MIC values of 8-128 μg/mL. One compound [(E)-1-(4-hydroxyphenyl)-3-p-tolylprop-2-en-1-one] had equal activity with gentamycin (8 μg/mL) against Enterococcus faecalis. Chalcones were found to be more active than their hydrazone and 2-pyrazoline derivatives against Staphylococcus aureus ATCC 29213 and E. faecalis ATCC 29212. PMID:26372110

  16. Development of Chiral Bis-hydrazone Ligands for the Enantioselective Cross-Coupling Reactions of Aryldimethylsilanolates

    PubMed Central

    2015-01-01

    A palladium-catalyzed, enantioselective, aryl–aryl cross-coupling reaction using 1-naphthyldimethylsilanolates and chiral bis-hydrazone ligands has been developed. A family of glyoxal bis-hydrazone ligands containing various 2,5-diarylpyrrolidine groups was prepared to evaluate the influence of ligand structure on the rate and enantioselectivity of the cross-coupling. New synthetic routes to the 1-amino-2,5-diarylpyrrolidines were developed to enable the structure/reactivity–selectivity studies. Role reversal experiments of aryldimethylsilanolates and aryl bromides result in biaryl products with the same configuration and similar enantioselectivities implying that reductive elimination is the stereodetermining step. The origin of stereoselectivity is rationalized through computational modeling of diarylpalldium(II) complex which occurs through a conrotatory motion for the two aryl groups undergoing C–C bond formation. PMID:25494058

  17. Mechanism and selectivity of N-triflylphosphoramide catalyzed (3(+) + 2) cycloaddition between hydrazones and alkenes.

    PubMed

    Hong, Xin; Küçük, Hatice Başpınar; Maji, Modhu Sudan; Yang, Yun-Fang; Rueping, Magnus; Houk, K N

    2014-10-01

    Brønsted acid catalyzed (3(+) + 2) cycloadditions between hydrazones and alkenes provide a general approach to pyrazolidines. The acidity of the Brønsted acid is crucial for the catalytic efficiency: the less acidic phosphoric acids are ineffective, while highly acidic chiral N-triflylphosphoramides are very efficient and can promote highly enantioselective cycloadditions. The mechanism and origins of catalytic efficiencies and selectivities of these reactions have been explored with density functional theory (M06-2X) calculations. Protonation of hydrazones by N-triflylphosphoramide produces hydrazonium-phosphoramide anion complexes. These ion-pair complexes are very reactive in (3(+) + 2) cycloadditions with alkenes, producing pyrazolidine products. Alternative 1,3-dipolar (3 + 2) cycloadditions with the analogous azomethine imines are much less favorable due to the endergonic isomerization of hydrazone to azomethine imine. With N-triflylphosphoramide catalyst, only a small distortion of the ion-pair complex is required to achieve its geometry in the (3(+) + 2) cycloaddition transition state. In contrast, the weak phosphoric acid does not protonate the hydrazone, and only a hydrogen-bonded complex is formed. Larger distortion energy is required for the hydrogen-bonded complex to achieve the "ion-pair" geometry in the cycloaddition transition state, and a significant barrier is found. On the basis of this mechanism, we have explained the origins of enantioselectivities when a chiral N-triflylphosphoramide catalyst is employed. We also report the experimental studies that extend the substrate scope of alkenes to ethyl vinyl ethers and thioethers. PMID:25226575

  18. Yohimbine hydrochloride as an antagonist to xylazine hydrochloride-ketamine hydrochloride immobilization of white-tailed deer

    USGS Publications Warehouse

    Mech, L.D.; DelGiudice, G.D.; Karns, P.D.; Seal, U.S.

    1985-01-01

    Thirteen captive and one free-ranging white-tailed deer (Odocoileus virginianus) were immobilized one to six times each with ketamine hydrochloride and xylazine hydrochloride during winter and spring in northern Minnesota. Administration of 0.09 to 0.53 mg of yohimbine hydrochloride per kg IV after each trial reversed the immobilization. The deer raised their heads within a median time of 2.0 min, stood in 6.0 min and walked away in 9.5 min. No adverse side effects were observed for several weeks following the immobilization.

  19. Synthesis, characterization and antitubercular activities of novel pyrrolyl hydrazones and their Cu-complexes.

    PubMed

    Joshi, Shrinivas D; Kumar, Devendra; Dixit, Sheshagiri R; Tigadi, Nageshwar; More, Uttam A; Lherbet, Christian; Aminabhavi, Tejraj M; Yang, Kap Seung

    2016-10-01

    Novel pyrrolyl hydrazones and their copper complexes have been synthesized and characterized using analytical and spectral techniques to show the tetrahedral geometry for Cu(II) complexes. Biological activities of hydrazones have been assessed to understand the role of metal ion on their biological activity and the effect of pyrrolyl hydrazones. In vitro antitubercular activity against Mycobacterium tuberculosis of the metal complexes (13b and 13r) exhibited the highest antitubercular activity that are quite close to rifampicin (0.4 μg/mL), giving a MIC of 0.8 μg/mL. All other compounds showed good activity with the MIC values ranging from 1.6 to 100 μg/mL. A comparative study of inhibition values of the ligands and their complexes showed higher antimicrobial activity of the complexes than the ligands. Some compounds have a good activity against InhA and in particular, compounds 12r, 13b and 13r exhibited more than 60% binding with the enzyme even at 5 μM (exhibited good IC50 upto 2.4 μM). Most of the active molecules have a very less cytotoxicity against the human lung cancer cell-line A549. The docking and 3D-QSAR studies have been carried out to provide some insights into the mechanism of action for this class of compounds. PMID:27214509

  20. Bach Adsorption Study for the Extraction of Silver Ions by Hydrazone Compounds from Aqueous Solution

    PubMed Central

    Mohamad Ali, Abdussalam Salhin; Abdul Razak, Norfarhah; Ab Rahman, Ismail

    2012-01-01

    Sorbent materials based on a hydrazone Schiff base compound, C14H11BrN4O4, were prepared either by immobilizing the ligand into sol-gel (SG1) or bonding to silica (SG2). The sorbent materials were characterized by FT-IR, EDX, SEM, TEM, and TGA. The sorption characteristics of a matrix of eight transition metal ions (Ag+, Cu2+, Co2+, Ni2+, Fe3+, Pb2+, Zn2+, and Mn2+) using batch method were studied. Several key parameters that affected the extraction efficiency such as pH, contact time, metal ions concentration, and gel size (for SGl) were investigated and optimized. Under the optimized conditions, the physically immobilized hydrazone sorbent (SG1) exhibits highest selectivity towards Ag+ ions, while the chemically bonded hydrazone sorbent (SG2) exhibits high extraction for all metal ions tested. However, for practical applications such as the removal and preconcentration of Ag+, the physically immobilized sorbent (SG1) is preferred. PMID:22629138

  1. Biaryl Amides and Hydrazones as Therapeutics for Prion Disease in Transgenic Mice

    PubMed Central

    Lu, Duo; Giles, Kurt; Li, Zhe; Rao, Satish; Dolghih, Elena; Gever, Joel R.; Geva, Michal; Elepano, Manuel L.; Oehler, Abby; Bryant, Clifford; Renslo, Adam R.; Jacobson, Matthew P.; DeArmond, Stephen J.; Silber, B. Michael

    2013-01-01

    The only small-molecule compound demonstrated to substantially extend survival in prion-infected mice is a biaryl hydrazone termed “Compd B” (4-pyridinecarboxaldehyde,2-[4-(5-oxazolyl)phenyl]hydrazone). However, the hydrazone moiety of Compd B results in toxic metabolites, making it a poor candidate for further drug development. We developed a pharmacophore model based on diverse antiprion compounds identified by high-throughput screening; based on this model, we generated biaryl amide analogs of Compd B. Medicinal chemistry optimization led to multiple compounds with increased potency, increased brain concentrations, and greater metabolic stability, indicating that they could be promising candidates for antiprion therapy. Replacing the pyridyl ring of Compd B with a phenyl group containing an electron-donating substituent increased potency, while adding an aryl group to the oxazole moiety increased metabolic stability. To test the efficacy of Compd B, we applied bioluminescence imaging (BLI), which was previously shown to detect prion disease onset in live mice earlier than clinical signs. In our studies, Compd B showed good efficacy in two lines of transgenic mice infected with the mouse-adapted Rocky Mountain Laboratory (RML) strain of prions, but not in transgenic mice infected with human prions. The BLI system successfully predicted the efficacies in all cases long before extension in survival could be observed. Our studies suggest that this BLI system has good potential to be applied in future antiprion drug efficacy studies. PMID:23965382

  2. Design, synthesis, computational calculation and biological evaluation of some novel 2-thiazolyl hydrazones

    NASA Astrophysics Data System (ADS)

    Anbazhagan, R.; Sankaran, K. R.

    2015-01-01

    In the present study a novel series of 1-(1-(4-isobutylphenyl)ethylidene)-2-(4-phenylthiazol-2-yl)hydrazine 2a and its derivatives 2b-2f have been synthesized by the cyclization of 1-(1-(4-isobutylphenyl)ethylidene)thiosemicarbazide with 2-bromoacetophenone/ 4-substituted 2-bromoacetophenones. The structures of the synthesized thiazolyl hydrazones 2a-2f were characterized by FT-IR, 1H, 13C NMR, 2D NMR and mass spectral techniques. The molecular geometries were also investigated theoretically using B3LYP functional with 6-311G(d,p) basis set. To explain the molecular properties energy gap (Eg), electronegativity (χ), hardness (g), electrophilicity (ω) and softness (S) were computed, natural bonding orbital (NBO) analysis and molecular electrostatic potential (MEP) were also performed at the same level of theory. All the synthesized thiazolyl hydrazones 2a-2f were screened for their in vitro antimicrobial activity against selected bacterial and fungal strains. The results showed that the heterocyclic thiazolyl hydrazone derivatives exhibit a promising selective inhibitory activity against various bacterial and fungal strains.

  3. Design, synthesis, computational calculation and biological evaluation of some novel 2-thiazolyl hydrazones.

    PubMed

    Anbazhagan, R; Sankaran, K R

    2015-01-25

    In the present study a novel series of 1-(1-(4-isobutylphenyl)ethylidene)-2-(4-phenylthiazol-2-yl)hydrazine 2a and its derivatives 2b-2f have been synthesized by the cyclization of 1-(1-(4-isobutylphenyl)ethylidene)thiosemicarbazide with 2-bromoacetophenone/ 4-substituted 2-bromoacetophenones. The structures of the synthesized thiazolyl hydrazones 2a-2f were characterized by FT-IR, (1)H, (13)C NMR, 2D NMR and mass spectral techniques. The molecular geometries were also investigated theoretically using B3LYP functional with 6-311G(d,p) basis set. To explain the molecular properties energy gap (Eg), electronegativity (χ), hardness (g), electrophilicity (ω) and softness (S) were computed, natural bonding orbital (NBO) analysis and molecular electrostatic potential (MEP) were also performed at the same level of theory. All the synthesized thiazolyl hydrazones 2a-2f were screened for their in vitro antimicrobial activity against selected bacterial and fungal strains. The results showed that the heterocyclic thiazolyl hydrazone derivatives exhibit a promising selective inhibitory activity against various bacterial and fungal strains. PMID:25168236

  4. Diastereoselective addition of Grignard reagents to α-epoxy N-sulfonyl hydrazones

    NASA Astrophysics Data System (ADS)

    Uteuliyev, Maulen M.; Nguyen, Thien T.; Coltart, Don M.

    2015-12-01

    The α-alkylation of ketones and their derivatives by the addition of their corresponding enolates to alkyl halides is a fundamental synthetic transformation, but its utility is limited because the key bond-forming step proceeds in a bimolecular nucleophilic substitution fashion. Here we describe how an umpolung strategy that involves the addition of Grignard reagents to α-epoxy N-sulfonyl hydrazones—directed by the alkoxide of the 1-azo-3-alkoxy propenes formed in situ via base-induced ring opening of the epoxide—leads to the syn-selective production of α-alkyl-β-hydroxy N-sulfonyl hydrazones with α-quaternary centres. This transformation is remarkable in its ability to incorporate an unprecedented range of carbon-based substituents, which include primary, secondary and tertiary alkyl, as well as alkenyl, aryl, allenyl and alkynyl groups. Subsequent hydrolysis of the β-hydroxy N-sulfonyl hydrazone products produces the corresponding β-hydroxy ketones. In addition to hydrolysis, the hydrazone products are poised to undergo numerous different known synthetic transformations via well-established chemistry, which would provide access to a wide array of useful structures.

  5. In vitro nematicidal activity of aryl hydrazones and comparative GC-MS metabolomics analysis.

    PubMed

    Eloh, Kodjo; Demurtas, Monica; Deplano, Alessandro; Ngoutane Mfopa, Alvine; Murgia, Antonio; Maxia, Andrea; Onnis, Valentina; Caboni, Pierluigi

    2015-11-18

    A series of aryl hydrazones were synthesized and in vitro assayed for their activity on the root-knot nematode Meloidogyne incognita. The phenylhydrazones of thiophene-2-carboxyaldehyde 5, 3-methyl-2-thiophenecarboxyaldehyde, 6, and salicylaldehyde, 2, were the most potent with EC50/48h values of 16.6 ± 2.2, 23.2 ± 2.7, and 24.3 ± 1.4 mg/L, respectively. A GC-MS metabolomics analysis, after in vitro nematode treatment with hydrazone 6 at 100 mg/L for 12 h, revealed elevated levels of fatty acids such as lauric acid, stearic acid, 2-octenoic acid, and palmitic acid. Whereas control samples showed the highest levels of monoacylglycerols such as monostearin and 2-monostearin, surprisingly, 2 h after treatment with hydrazone 6, nematodes excreted 3 times the levels of ammonia eliminated in the same conditions by controls. Thus, phenylhydrazones may represent a good scaffold in the discovery and synthesis of new nematicidal compounds, and a metabolomics approach may be helpful in understanding their mechanisms of toxicity and mode of action. PMID:26528945

  6. Immobilization of swift foxes with ketamine hydrochloride-xylazine hydrochloride

    USGS Publications Warehouse

    Telesco, R.L.; Sovada, M.A.

    2002-01-01

    There is an increasing need to develop field immobilization techniques that allow researchers to handle safely swift foxes (Vulpes velox) with minimal risk of stress or injury. We immobilized captive swift foxes to determine the safety and effectiveness of ketamine hydrochloride and xylazine hydrochloride at different dosages. We attempted to determine appropriate dosages to immobilize swift foxes for an adequate field-handling period based on three anesthesia intervals (induction period, immobilization period, and recovery period) and physiologic responses (rectal temperature, respiration rate, and heart rate). Between October 1998-July 1999, we conducted four trials, evaluating three different dosage ratios of ketamine and xylazine (2.27:1.2, 5.68:1.2, and 11.4:1.2 mg/kg ketamine:mg/kg xylazine, respectively), followed by a fourth trial with a higher dosage at the median ratio (11.4 mg/kg ketamine:2.4 mg/kg xylazine). We found little difference in induction and recovery periods among trials 1-3, but immobilization time increased with increasing dosage (P<0.08). Both the immobilization period and recovery period increased in trial 4 compared with trials 1-3 (P???0.03). There was a high variation in responses of individual foxes across trials, making it difficult to identify an appropriate dosage for field handling. Heart rate and respiration rates were depressed but all physiologic measures remained within normal parameters established for domestic canids. We recommend a dosage ratio of 10 mg/kg ketamine to 1 mg/kg xylazine to immobilize swift foxes for field handling.

  7. 21 CFR 520.222 - Bunamidine hydrochloride.

    Code of Federal Regulations, 2014 CFR

    2014-04-01

    .... (a) Chemical name. N,N-Dibutyl-4-(hexyloxy)-1-naphthamidine hydrochloride. (b) Specifications. The... kilogram of body weight. The drug should be given on an empty stomach and food should not be given for...

  8. 21 CFR 520.1962 - Promazine hydrochloride.

    Code of Federal Regulations, 2014 CFR

    2014-04-01

    .... (a)(1) Chemical name. 10- phenothiazine monohydrochloride. (2) Specifications. Conforms to N.F. XII... of 0.45 to 0.9 milligrams of promazine hydrochloride per pound of body weight mixed with an amount...

  9. 21 CFR 184.1676 - Pyridoxine hydrochloride.

    Code of Federal Regulations, 2010 CFR

    2010-04-01

    ... hydrochloride that is prepared by chemical synthesis. (b) The ingredient meets the specifications of the Food...)(31) of this chapter; plant protein products as defined in § 170.3(n)(33) of this chapter; and...

  10. 21 CFR 184.1676 - Pyridoxine hydrochloride.

    Code of Federal Regulations, 2012 CFR

    2012-04-01

    ... hydrochloride that is prepared by chemical synthesis. (b) The ingredient meets the specifications of the Food...)(31) of this chapter; plant protein products as defined in § 170.3(n)(33) of this chapter; and...

  11. 21 CFR 184.1676 - Pyridoxine hydrochloride.

    Code of Federal Regulations, 2011 CFR

    2011-04-01

    ... hydrochloride that is prepared by chemical synthesis. (b) The ingredient meets the specifications of the Food...)(31) of this chapter; plant protein products as defined in § 170.3(n)(33) of this chapter; and...

  12. 21 CFR 184.1676 - Pyridoxine hydrochloride.

    Code of Federal Regulations, 2013 CFR

    2013-04-01

    ... hydrochloride that is prepared by chemical synthesis. (b) The ingredient meets the specifications of the Food...)(31) of this chapter; plant protein products as defined in § 170.3(n)(33) of this chapter; and...

  13. 21 CFR 520.2002 - Propiopromazine hydrochloride.

    Code of Federal Regulations, 2010 CFR

    2010-04-01

    ... propiopromazine hydrochloride per pound of body weight once or twice daily depending upon the degree of... may produce significant depression. (3) For use only by or on the order of a licensed veterinarian....

  14. Synthesis and solid state structure of a hydrazone-disulfide macrocycle and its dynamic covalent ring-opening under acidic and basic conditions.

    PubMed

    von Delius, Max; Geertsema, Edzard M; Leigh, David A; Slawin, Alexandra M Z

    2010-10-21

    The synthesis and characterisation, including solid state structure, of a macrocycle containing both a hydrazone and a disulfide linkage is described. Selective ring-opening of the macrocycle under thermodynamic control could be achieved at either the disulfide or the hydrazone linkage by applying mutually exclusive sets of reaction conditions. PMID:20725686

  15. 21 CFR 522.2470 - Tiletamine hydrochloride and zolazepam hydrochloride for injection.

    Code of Federal Regulations, 2013 CFR

    2013-04-01

    ... reconstituted with sterile distilled water provides tiletamine hydrochloride and zolazepam hydrochloride... analgesia. (2) Amount. Expressed as milligrams of the drug combination: (i) In healthy dogs: An initial... healthy cats: An initial intramuscular dosage of 4.4 to 5.4 milligrams per pound of body weight...

  16. 21 CFR 522.2470 - Tiletamine hydrochloride and zolazepam hydrochloride for injection.

    Code of Federal Regulations, 2010 CFR

    2010-04-01

    ... reconstituted with sterile distilled water provides tiletamine hydrochloride and zolazepam hydrochloride... analgesia. (2) Amount. Expressed as milligrams of the drug combination: (i) In healthy dogs: An initial... healthy cats: An initial intramuscular dosage of 4.4 to 5.4 milligrams per pound of body weight...

  17. 21 CFR 522.2470 - Tiletamine hydrochloride and zolazepam hydrochloride for injection.

    Code of Federal Regulations, 2012 CFR

    2012-04-01

    ... reconstituted with sterile distilled water provides tiletamine hydrochloride and zolazepam hydrochloride... analgesia. (2) Amount. Expressed as milligrams of the drug combination: (i) In healthy dogs: An initial... healthy cats: An initial intramuscular dosage of 4.4 to 5.4 milligrams per pound of body weight...

  18. 21 CFR 522.2470 - Tiletamine hydrochloride and zolazepam hydrochloride for injection.

    Code of Federal Regulations, 2011 CFR

    2011-04-01

    ... reconstituted with sterile distilled water provides tiletamine hydrochloride and zolazepam hydrochloride... analgesia. (2) Amount. Expressed as milligrams of the drug combination: (i) In healthy dogs: An initial... healthy cats: An initial intramuscular dosage of 4.4 to 5.4 milligrams per pound of body weight...

  19. Potent antimycobacterial activity of the pyridoxal isonicotinoyl hydrazone analog 2-pyridylcarboxaldehyde isonicotinoyl hydrazone: a lipophilic transport vehicle for isonicotinic acid hydrazide.

    PubMed

    Ellis, Samantha; Kalinowski, Danuta S; Leotta, Lisa; Huang, Michael L H; Jelfs, Peter; Sintchenko, Vitali; Richardson, Des R; Triccas, James A

    2014-02-01

    The rise in drug-resistant strains of Mycobacterium tuberculosis is a major threat to human health and highlights the need for new therapeutic strategies. In this study, we have assessed whether high-affinity iron chelators of the pyridoxal isonicotinoyl hydrazone (PIH) class can restrict the growth of clinically significant mycobacteria. Screening a library of PIH derivatives revealed that one compound, namely, 2-pyridylcarboxaldehyde isonicotinoyl hydrazone (PCIH), exhibited nanomolar in vitro activity against Mycobacterium bovis bacille Calmette-Guérin and virulent M. tuberculosis. Interestingly, PCIH is derived from the condensation of 2-pyridylcarboxaldehyde with the first-line antituberculosis drug isoniazid [i.e., isonicotinic acid hydrazide (INH)]. PCIH displayed minimal host cell toxicity and was effective at inhibiting growth of M. tuberculosis within cultured macrophages and also in vivo in mice. Further, PCIH restricted mycobacterial growth at high bacterial loads in culture, a property not observed with INH, which shares the isonicotinoyl hydrazide moiety with PCIH. When tested against Mycobacterium avium, PCIH was more effective than INH at inhibiting bacterial growth in broth culture and in macrophages, and also reduced bacterial loads in vivo. Complexation of PCIH with iron decreased its effectiveness, suggesting that iron chelation may play some role in its antimycobacterial efficacy. However, this could not totally account for its potent efficacy, and structure-activity relationship studies suggest that PCIH acts as a lipophilic vehicle for the transport of its intact INH moiety into the mammalian cell and the mycobacterium. These results demonstrate that iron-chelating agents such as PCIH may be of benefit in the treatment and control of mycobacterial infection. PMID:24243647

  20. Metallo-hydrazone complexes immobilized in zeolite Y: Synthesis, identification and acid violet-1 degradation

    NASA Astrophysics Data System (ADS)

    Ahmed, Ayman H.; Thabet, M. S.

    2011-12-01

    Copper(II), cobalt(II) and nickel(II) complexes of hydrazone ligand (SAPH) derived from salicylaldehyde and phenylhydrazine have been encapsulated in zeolite-Y super cages via ship-in-a-bottle synthesis. Detailed characterization of the intrazeolitic complexes were performed by elemental analysis, spectral (FT-IR, UV-Vis.) studies, magnetic measurements and X-ray diffraction. Furthers, surface texture and thermal analysis (TG, DTG, DTA) have provided further evidence for successful immobilization of the metal complexes inside zeolite Y. Investigation of the stereochemistry of these incorporated chelates pointed out that, SAPH ligand is capable to coordinate with the central metal through the (C dbnd N), phenolic (OH) and (NH) groups forming polynuclear structures. The involvement of zeolite oxygen in coordination was postulated in the hybrid materials. The intrazeolitic copper, cobalt and nickel-SAPH complexes have distorted tetrahedral, octahedral and square-pyramidal configurations, respectively. The zeolite encapsulated complexes are thermally stable up to 800 °C except Cu(II) sample which is thermally stable up to midpoint 428 °C. The assessment of the catalytic activity was performed by the use of the photo-degradation of acid violet-1 dye as a probe reaction in presence of H 2O 2 as an oxidant. Decolorization of acid violet-1 dye was examined under the same conditions whereas the unpromoted zeolite and Cu II, Co II, Ni II-hydrazone complexes supported on zeolite showed 13% and 76%, 53%, 43% color removal, respectively. The results revealed that, the zeolite encapsulated Cu(II) complex generally exhibited better catalytic efficiency (76%) compared with other investigated zeolite encapsulated metal-hydrazone samples.

  1. Synthesis, Spectroscopic Properties and Antioxidant Activity of Bis-Hydrazones and Schiff's bases Derived from Terephthalic Dihydrazide.

    PubMed

    Jois, H S Vidyashree; Kalluraya, Balakrishna; Vishwanath, T

    2015-05-01

    A series of novel Schiff base containing bis-1,2,4-triazole and bis-hydrazone derived from terephthalic dihydrazide was synthesized. All the newly synthesized compounds were characterized by (1)H, (13)C NMR, mass spectra, FTIR and elemental analysis. UV-vis spectra and fluorescent spectra of the compounds were recorded. The effect of substituent such as electron withdrawing and electron donating groups on the fluorescent spectra was studied. Also, the comparative discussion on fluorescent spectra of Schiff's base and hydrazones has been described. The antioxidant activity of the compounds revealed that compound 5c and 5f are the most potent compounds in this series. PMID:25820870

  2. Copper-catalyzed aerobic oxidative transformation of ketone-derived N-tosyl hydrazones: an entry to alkynes.

    PubMed

    Li, Xianwei; Liu, Xiaohang; Chen, Huoji; Wu, Wanqing; Qi, Chaorong; Jiang, Huanfeng

    2014-12-22

    A novel strategy involving Cu-catalyzed oxidative transformation of ketone-derived hydrazone moiety to various synthetic valuable internal alkynes and diynes has been developed. This method features inexpensive metal catalyst, green oxidant, good functional group tolerance, high regioselectivity and readily available starting materials. Oxidative deprotonation reactions were carried out to form internal alkynes and symmetrical diynes. Cross-coupling reactions of hydrazones with halides and terminal alkynes were performed to afford functionalized alkynes and unsymmetrical conjugated diynes. A mechanism proceeding through a Cu-carbene intermediate is proposed for the CC triple bond formation. PMID:25424976

  3. Iron(III)-Mediated Radical Nitration of Bisarylsulfonyl Hydrazones: Synthesis of Bisarylnitromethyl Sulfones.

    PubMed

    Sar, Dinabandhu; Bag, Raghunath; Bhattacharjee, Debajyoti; Deka, Ramesh Chandra; Punniyamurthy, Tharmalingam

    2015-07-01

    Iron(III)-mediated radical nitration of bisarylsulfonyl hydrazones is described. In this protocol, the nontoxic and inexpensive Fe(NO3)3·9H2O plays a dual role as catalyst as well as nitro source. The mild conditions, broad substrate scope, and the functional group compatibility are the significant features. The reaction pathway has been demonstrated using DFT calculations, and the products can be subsequently converted into oximes using SnCl2·2H2O in high yields. PMID:26036359

  4. Synthesis and anticancer activities of novel 8-azapurine carbocyclic nucleoside hydrazones.

    PubMed

    Wang, Yeming; Yan, Hong; Ma, Chao; Lu, Dan

    2015-10-15

    A series of novel 8-azapurine carbocyclic nucleoside hydrazones were synthesized through a useful procedure starting from amino alcohol and pyrimido dichloride. All the products were characterized by (1)H NMR, (13)C NMR and HRMS spectral analysis and the stereochemical structure of key intermediate was also confirmed by a single crystal X-ray diffraction crystallographic analysis. Moreover, the anticancer activities were evaluated in vitro against human liver cancer Huh-7 cell line and human breast cancer A549 cell line. PMID:26364944

  5. Persistent Enhanced Conductivity Induced by Light Irradiation in Hydrazone-Polycarbonate Dispersions

    NASA Astrophysics Data System (ADS)

    Hirao, Akiko; Nishizawa, Hideyuki; Hosoya, Masahiro

    1994-04-01

    Photoinduced spins with extended lifetime have been observed in hydrazone-polycarbonate dispersions. The presence of the spins changed the electrical characteristics of the dispersions. Measurements of electrical current associated with thermal equilibration after photoexcitation in dispersions of diethylamino-benzaldehyde diphenylhydrazone (DEH) in polycarbonate have been carried out. Sandwiched layers of the dispersions were excited with absorbed light. After withdrawal of the light, a voltage was applied and the current was measured. Experimental data provide evidence that photoinduced spins are derived from trapped carriers.

  6. Synthesis, Antifungal Activities and Qualitative Structure Activity Relationship of Carabrone Hydrazone Derivatives as Potential Antifungal Agents

    PubMed Central

    Wang, Hao; Ren, Shuang-Xi; He, Ze-Yu; Wang, De-Long; Yan, Xiao-Nan; Feng, Jun-Tao; Zhang, Xing

    2014-01-01

    Aimed at developing novel fungicides for relieving the ever-increasing pressure of agricultural production caused by phytopathogenic fungi, 28 new hydrazone derivatives of carabrone, a natural bioactive sesquisterpene, in three types were designed, synthesized and their antifungal activities against Botrytis cinerea and Colletotrichum lagenarium were evaluated. The result revealed that all the derivatives synthesized exhibited considerable antifungal activities in vitro and in vivo, which led to the improved activities for carabrone and its analogues and further confirmed their potential as antifungal agents. PMID:24619221

  7. 21 CFR 522.1465 - Naltrexone hydrochloride injection.

    Code of Federal Regulations, 2012 CFR

    2012-04-01

    ... 21 Food and Drugs 6 2012-04-01 2012-04-01 false Naltrexone hydrochloride injection. 522.1465... § 522.1465 Naltrexone hydrochloride injection. (a) Specifications. Each milliliter of sterile aqueous solution contains 50 milligrams of naltrexone hydrochloride. (b) Sponsor. See 053923 in § 510.600(c)...

  8. 21 CFR 522.1465 - Naltrexone hydrochloride injection.

    Code of Federal Regulations, 2013 CFR

    2013-04-01

    ... 21 Food and Drugs 6 2013-04-01 2013-04-01 false Naltrexone hydrochloride injection. 522.1465... § 522.1465 Naltrexone hydrochloride injection. (a) Specifications. Each milliliter of sterile aqueous solution contains 50 milligrams of naltrexone hydrochloride. (b) Sponsor. See 053923 in § 510.600(c)...

  9. 21 CFR 522.1465 - Naltrexone hydrochloride injection.

    Code of Federal Regulations, 2011 CFR

    2011-04-01

    ... 21 Food and Drugs 6 2011-04-01 2011-04-01 false Naltrexone hydrochloride injection. 522.1465... § 522.1465 Naltrexone hydrochloride injection. (a) Specifications. Each milliliter of sterile aqueous solution contains 50 milligrams of naltrexone hydrochloride. (b) Sponsor. See 053923 in § 510.600(c)...

  10. 21 CFR 182.1047 - Glutamic acid hydrochloride.

    Code of Federal Regulations, 2012 CFR

    2012-04-01

    ... 21 Food and Drugs 3 2012-04-01 2012-04-01 false Glutamic acid hydrochloride. 182.1047 Section 182.1047 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED... Food Substances § 182.1047 Glutamic acid hydrochloride. (a) Product. Glutamic acid hydrochloride....

  11. 21 CFR 182.1047 - Glutamic acid hydrochloride.

    Code of Federal Regulations, 2010 CFR

    2010-04-01

    ... 21 Food and Drugs 3 2010-04-01 2009-04-01 true Glutamic acid hydrochloride. 182.1047 Section 182.1047 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED... Food Substances § 182.1047 Glutamic acid hydrochloride. (a) Product. Glutamic acid hydrochloride....

  12. 21 CFR 182.1047 - Glutamic acid hydrochloride.

    Code of Federal Regulations, 2011 CFR

    2011-04-01

    ... 21 Food and Drugs 3 2011-04-01 2011-04-01 false Glutamic acid hydrochloride. 182.1047 Section 182.1047 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED... Food Substances § 182.1047 Glutamic acid hydrochloride. (a) Product. Glutamic acid hydrochloride....

  13. 21 CFR 182.1047 - Glutamic acid hydrochloride.

    Code of Federal Regulations, 2014 CFR

    2014-04-01

    ... 21 Food and Drugs 3 2014-04-01 2014-04-01 false Glutamic acid hydrochloride. 182.1047 Section 182...) SUBSTANCES GENERALLY RECOGNIZED AS SAFE Multiple Purpose GRAS Food Substances § 182.1047 Glutamic acid hydrochloride. (a) Product. Glutamic acid hydrochloride. (b) (c) Limitations, restrictions, or explanation....

  14. 21 CFR 182.1047 - Glutamic acid hydrochloride.

    Code of Federal Regulations, 2013 CFR

    2013-04-01

    ... 21 Food and Drugs 3 2013-04-01 2013-04-01 false Glutamic acid hydrochloride. 182.1047 Section 182.1047 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED... Food Substances § 182.1047 Glutamic acid hydrochloride. (a) Product. Glutamic acid hydrochloride....

  15. Variation in the biomolecular interactions of nickel(II) hydrazone complexes upon tuning the hydrazide fragment.

    PubMed

    Krishnamoorthy, Paramasivam; Sathyadevi, Palanisamy; Butorac, Rachel R; Cowley, Alan H; Bhuvanesh, Nattamai S P; Dharmaraj, Nallasamy

    2012-06-14

    Three new bivalent nickel hydrazone complexes have been synthesised from the reactions of [NiCl(2)(PPh(3))(2)] with H(2)L {L = dianion of the hydrazones derived from the condensation of o-hydroxynaphthaldehyde with furoic acid hydrazide (H(2)L(1)) (1)/thiophene-2-acid hydrazide (H(2)L(2)) (2)/isonicotinic acid hydrazide (H(2)L(3)) (3)} and formulated as [Ni(L(1))(PPh(3))] (4), [Ni(L(2))(PPh(3))] (5) and [Ni(L(3))(PPh(3))] (6). Structural characterization of these compounds 4-6 were accomplished by using various physico-chemical techniques. Single crystal X-ray diffraction data of complexes 4 and 5 proved their distorted square planar geometry. In order to ascertain the potential of the above synthesised compounds towards biomolecular interactions, additional experiments involving interaction with calf thymus DNA (CT DNA) and bovine serum albumin (BSA) were carried out. All the ligands and corresponding nickel(ii) chelates have been screened for their scavenging effect towards O(2)(-), OH and NO radicals. The efficiency of complexes 4-6 to arrest the growth of HeLa, HepG-2 and A431 tumour cell lines has been studied along with the cell viability test against the non-cancerous NIH 3T3 cells under in vitro conditions. PMID:22506273

  16. Synthesis, Antiplatelet Activity and Cytotoxicity Assessment of Indole-Based Hydrazone Derivatives

    PubMed Central

    Haj Mohammad Ebrahim Tehrani, Kamaleddin; Esfahani Zadeh, Marjan; Mashayekhi, Vida; Hashemi, Maryam; Kobarfard, Farzad; Gharebaghi, Farhad; Mohebbi, Shohreh

    2015-01-01

    A series of indole-based aryl(aroyl)hydrazone analogs of antiplatelet indole-3-carboxaldehyde phenylhydrazone were synthesized by the Schiff base formation reaction and their antiplatelet activity was assessed using human platelet rich plasma. The platelet concentrate was obtained using a two-step centrifugation protocol and ADP, arachidonic acid and collagen were used as inducers of platelet aggregation. Based on the results, substituted phenylhydrazones showed promising activity. Among them, compound 1i was the most potent derivative with an IC50 comparable to that of indomethacin as a standard drug. The hydrazone derivatives were also tested for their cytotoxicity using on platelet concentrates and fibroblast L929 cells. The majority of the derivatives showed an acceptable selectivity towards antiplatelet aggregation activity. Based on the activity data, phenylhydrazone derivatives (1a-i) exhibited considerable antiplatelet activity and minimal toxic effect on platelet cells. The results of the present study could provide a better understanding of the structure activity relationship of antiplatelet indolehydrazones. PMID:26664374

  17. Highly efficient donor-acceptor hydrazone dyes-inorganic Si/TiO₂ hybrid solar cells.

    PubMed

    Al-Sehemi, Abdullah G; Irfan, Ahmad; Al-Melfi, Mohrah Abdullah M

    2015-06-15

    We have synthesized the two donor-bridge-acceptor organic dyes (hydrazone dye 1 (HD1) and hydrazone dye 2 (HD2)) with the aim to enhance intra-molecular charge transfer then characterized by FTIR and NMR. The ground state geometries have been optimized at three different levels of theories, i.e., B3LYP/6-31G, B3LYP/6-31G and Hartee-Fock HF/6-31G. The absorption spectra and oscillator strengths in different solvents have been computed and compared with the experimental data. The vibrational spectral assignments have been performed on the recorded FTIR spectra based on the theoretical predicted wavenumbers at three different levels of theories. The effect of different solvents (CHCl3, CH3CN and C2H5OH) has been studied on the absorption wavelengths. Furthermore, we have computed the ionization potentials, electron affinities and reorganization energies of studied compounds and shed light on the charge transport properties. The hetero-junction solar cell devices were fabricated by organic-inorganic hetero-junction (Si/TiO2/dye) then the efficiency has been measured by applying the incident power 30, 50 and 70 mW/cm(2). The maximum efficiency 3.12% has been observed for HD1. PMID:25766477

  18. Synthesis, spectral characterization, DNA interaction, radical scavenging and cytotoxicity studies of ruthenium(II) hydrazone complexes.

    PubMed

    Mohanraj, Maruthachalam; Ayyannan, Ganesan; Raja, Gunasekaran; Jayabalakrishnan, Chinnasamy

    2016-05-01

    Three new ruthenium(II) complexes with hydrazone ligands, furan-2-carboxylic acid (2,4-dihydroxy-benzylidene)-hydrazide (HL(1)), furan-2-carboxylic acid [4-(ethyl-propyl-amino)-2-hydroxy-benzylidene]-hydrazide (HL(2)) and furan-2-carboxylic acid (3-ethoxy-2-hydroxy-benzylidene)-hydrazide (HL(3)) were synthesized and characterized by various spectro-analytical techniques. The hydrazone ligands act as a tridendate ligand with ONO as the donor sites and are preferably found in the enol form in all the complexes. The molecular structure of the ligands was determined by single crystal X-ray diffraction technique. The interaction of the ligands and the complexes with CT-DNA were evaluated by an absorption titration method which revealed that the compounds interact with CT-DNA through intercalation. Gel electrophoresis assay demonstrated the ability of the complexes to cleave the calf thymus DNA hydrolytically. Antioxidant studies showed that the ruthenium(II) complexes have a strong radical-scavenging properties. Further, the cytotoxic effect of the compounds examined on cancerous cell lines showed that the complexes exhibited substantial anticancer activity. PMID:26974577

  19. Synthesis, characterization and modeling structures of isatin-3-Girard T (IGT) and P (IGP) hydrazone complexes.

    PubMed

    Salah, Sabah; El-Wahab, Zeinab H Abd; Farag, Rabei S; Mostafa, Mohsen M

    2014-04-24

    The reactions of isatin Girard's T hydrazone, N,N,N-trimethyl-2-oxo-2[(2z)-2-(2-oxo-1,2-dihydro-3H-indole-3-ylidene)hydrazino]ethan ammonium chloride (IGT) and isatin Girard's P hydrazone, 1-{2-oxo-2-[(2z)(2-oxo-1,2-dihydro-3H-indole-3-ylidene)hydrazine]ethyl} pyridinium chloride (IGP), with Fe(3+), Al(3+), Sb(3+) and Sn(2+) salts afford different types of complexes. The isolated solid complexes were characterized by elemental analyses, molar conductance, spectral (IR, UV-Vis, (1)H NMR, mass), magnetic moment and thermal measurements. The results suggest that all the complexes are conducting in polar solvents (EtOH, H2O and DMF). The IR spectral data suggest that the ligands coordinate in a tridentate manner via the two carbonyl of both isatin and Girard's and the azomethine (C=N) groups. The amounts of solvents inside and outside the coordination sphere were determined using thermal data (TGA) and weight loss method. The octahedral geometry of the complexes is confirmed using DFT method from DMOL(3) calculations. The ligands and their metal complexes were tested against different strains of bacteria and fungi. PMID:24509535

  20. Vanadium Complexes with Hydrazone or Thiosemicarbazone Ligands as Potential Anti-Mycobacterium tuberculosis Agents.

    PubMed

    de Souza, Paula C; Maia, Pedro I S; de Barros, Heloisa B; Leite, Clarice Q F; Deflon, Victor M; Pavan, Fernando R

    2015-01-01

    Tuberculosis (TB) is an infectious disease caused mainly by Mycobacterium tuberculosis (MTB) and still an important public health problem worldwide. Some factors like the emergence of multidrug resistant (MDR) and extensively drug-resistant (XDR) strains make urgent the research of new active compounds. Searching for new inorganic compounds against TB, three new dioxovanadium(V) complexes were obtained upon reaction of [VO(acac)2] with hydrazone and thiosemicarbazone ligands derived from di-2-pyridyl ketone. Spectroscopic studies and X-ray crystallography revealed asymmetrically oxo bridged binuclear complexes of the type [{VO(L(1,2))}2(μ-O)2], involving the hydrazone ligands, while a mononuclear square pyramidal complex of the type [VO2(L(3))] was formed with the thiosemicarbazone ligand. The compounds were tested against M. tuberculosis and three of them, with MICs values between 2.00 and 3.76 μM were considered promising for TB treatment. Such MIC values are comparable or better than those found for some drugs currently used in TB treatment. PMID:24433444

  1. Identification and determination of ketotifen hydrogen fumarate, azelastine hydrochloride, dimetindene maleate and promethazine hydrochloride by densitometric method.

    PubMed

    Wyszomirska, Elzbieta; Czerwińska, Krystyna; Kublin, Elzbieta; Mazurek, Aleksander P

    2013-01-01

    Conditions for determination of: ketotifen hydrogen fumarate, azelastine hydrochloride, dimetindene maleate and promethazine hydrochloride by densitometric method in substances and pharmaceuticals were provided. Maximum wavelenghts were: 228 nm for ketotifen hydrogen fumarate, 295 nm for azelastine hydrochloride, 265 nm for dimetindene maleate and 255 nm for promethazine hydrochloride. The limits of quantification were in the ranges of 0.2-5 microg/spot. The statistical data showed adequate accuracy and precision of developed methods. PMID:24383318

  2. Synthesis and structural characterization of zinc(II) and cobalt(II) complexes based on multidentate hydrazone ligands

    NASA Astrophysics Data System (ADS)

    Li, Li; Zhang, Yuan Zhuo; Liu, E.; Yang, Chengxiong; Golen, James A.; Rheingold, Arnold L.; Zhang, Guoqi

    2016-04-01

    Two multidentate Schiff base ligands containing a hydrazone unit have been synthesized and investigated for zinc(II) and cobalt(II) coordination chemistry. The reactions of the 4-pyridyl derived hydrazone ligand HL1 with zinc(II) or cobalt(II) salts gave three mononuclear complexes that were structurally characterized by X-ray diffraction analysis. The results revealed that the ligand could adopt different coordination modes when various counter anions were employed. While in the case that zinc dichloride was used as a metal salt a neutral mononuclear mono-ligand complex was formed, the deprotonation of hydrazone occurred when zinc(II) or cobalt(II) nitrate were present and two new isostructural mononuclear bis-ligand complexes were isolated. Modification of the hydrazone ligand with oxygen donors was found to have a significant impact on the ligand reactivity, and a similar reaction of H2L2 with cobalt(II) nitrate gave a protonated product of H2L2 without the incorporation of cobalt(II), which features a one-dimensional hydrogen-bonded network in the solid state.

  3. Structure-Activity Relationships of Novel Salicylaldehyde Isonicotinoyl Hydrazone (SIH) Analogs: Iron Chelation, Anti-Oxidant and Cytotoxic Properties

    PubMed Central

    Potůčková, Eliška; Hrušková, Kateřina; Bureš, Jan; Kovaříková, Petra; Špirková, Iva A.; Pravdíková, Kateřina; Kolbabová, Lucie; Hergeselová, Tereza; Hašková, Pavlína; Jansová, Hana; Macháček, Miloslav; Jirkovská, Anna; Richardson, Vera; Lane, Darius J. R.; Kalinowski, Danuta S.; Richardson, Des R.; Vávrová, Kateřina; Šimůnek, Tomáš

    2014-01-01

    Salicylaldehyde isonicotinoyl hydrazone (SIH) is a lipophilic, tridentate iron chelator with marked anti-oxidant and modest cytotoxic activity against neoplastic cells. However, it has poor stability in an aqueous environment due to the rapid hydrolysis of its hydrazone bond. In this study, we synthesized a series of new SIH analogs (based on previously described aromatic ketones with improved hydrolytic stability). Their structure-activity relationships were assessed with respect to their stability in plasma, iron chelation efficacy, redox effects and cytotoxic activity against MCF-7 breast adenocarcinoma cells. Furthermore, studies assessed the cytotoxicity of these chelators and their ability to afford protection against hydrogen peroxide-induced oxidative injury in H9c2 cardiomyoblasts. The ligands with a reduced hydrazone bond, or the presence of bulky alkyl substituents near the hydrazone bond, showed severely limited biological activity. The introduction of a bromine substituent increased ligand-induced cytotoxicity to both cancer cells and H9c2 cardiomyoblasts. A similar effect was observed when the phenolic ring was exchanged with pyridine (i.e., changing the ligating site from O, N, O to N, N, O), which led to pro-oxidative effects. In contrast, compounds with long, flexible alkyl chains adjacent to the hydrazone bond exhibited specific cytotoxic effects against MCF-7 breast adenocarcinoma cells and low toxicity against H9c2 cardiomyoblasts. Hence, this study highlights important structure-activity relationships and provides insight into the further development of aroylhydrazone iron chelators with more potent and selective anti-neoplastic effects. PMID:25393531

  4. RP-HPLC and Spectrophotometric Estimation of Ambroxol Hydrochloride and Cetirizine Hydrochloride in Combined Dosage Form.

    PubMed

    Bhatia, Neela M; Ganbavale, S K; Bhatia, M S; More, H N; Kokil, S U

    2008-09-01

    Rapid, precise, accurate, specific and sensitive reverse phase liquid chromatographic and absorbance ratio spectrophotometric methods have been developed for the simultaneous analysis of ambroxol hydrochloride and cetirizine hydrochloride in their tablet formulation. The chromatographic methods were standardized using a HIQ SIL-C(18) column (250×4.6 mm i.d., 10 μm particle size) with UV detection at 229 nm and mobile phase consisting of methanol-acetonitrile-water (40:40:20, v/v/v). Ambroxol hydrochloride and cetirizine hydrochloride have absorbance maxima at 243 nm and 229 nm, respectively. The isoabsorptive wavelength for both the drugs was 236 nm. For absorbance ratio method developed, wavelengths selected were 243 nm and 236 nm. The proposed methods were successfully applied to the determination of ambroxol hydrochloride and cetirizine hydrochloride in tablets, with high percentage of recovery, good accuracy and acceptable precision. Different analytical performance parameters such as linearity, precision, accuracy, limit of detection, limit of quantitation and robustness were determined according to International Conference on Harmonization ICH Q2B guidelines. Results of analysis of the developed method were compared by performing ANOVA. PMID:21394256

  5. 21 CFR 556.580 - Robenidine hydrochloride.

    Code of Federal Regulations, 2012 CFR

    2012-04-01

    ... 21 Food and Drugs 6 2012-04-01 2012-04-01 false Robenidine hydrochloride. 556.580 Section 556.580 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL DRUGS, FEEDS, AND RELATED PRODUCTS TOLERANCES FOR RESIDUES OF NEW ANIMAL DRUGS IN FOOD...

  6. 21 CFR 556.580 - Robenidine hydrochloride.

    Code of Federal Regulations, 2013 CFR

    2013-04-01

    ... 21 Food and Drugs 6 2013-04-01 2013-04-01 false Robenidine hydrochloride. 556.580 Section 556.580 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL DRUGS, FEEDS, AND RELATED PRODUCTS TOLERANCES FOR RESIDUES OF NEW ANIMAL DRUGS IN FOOD...

  7. 21 CFR 556.580 - Robenidine hydrochloride.

    Code of Federal Regulations, 2014 CFR

    2014-04-01

    ... 21 Food and Drugs 6 2014-04-01 2014-04-01 false Robenidine hydrochloride. 556.580 Section 556.580 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL DRUGS, FEEDS, AND RELATED PRODUCTS TOLERANCES FOR RESIDUES OF NEW ANIMAL DRUGS IN FOOD...

  8. 21 CFR 558.515 - Robenidine hydrochloride.

    Code of Federal Regulations, 2012 CFR

    2012-04-01

    ... Federal Register citations affecting § 558.515, see the List of CFR Sections Affected, which appears in... chapter. (d) Conditions of use. It is used in feed for chickens as follows: Robenidine hydrochloride in... and fryer chickens: As an aid in the prevention of coccidiosis caused by E. mivati, E. brunetti,...

  9. 21 CFR 558.515 - Robenidine hydrochloride.

    Code of Federal Regulations, 2011 CFR

    2011-04-01

    ... Federal Register citations affecting § 558.515, see the List of CFR Sections Affected, which appears in... chapter. (d) Conditions of use. It is used in feed for chickens as follows: Robenidine hydrochloride in... and fryer chickens: As an aid in the prevention of coccidiosis caused by E. mivati, E. brunetti,...

  10. 21 CFR 558.515 - Robenidine hydrochloride.

    Code of Federal Regulations, 2013 CFR

    2013-04-01

    ... Federal Register citations affecting § 558.515, see the List of CFR Sections Affected, which appears in... chapter. (d) Conditions of use. It is used in feed for chickens as follows: Robenidine hydrochloride in... and fryer chickens: As an aid in the prevention of coccidiosis caused by E. mivati, E. brunetti,...

  11. 21 CFR 558.515 - Robenidine hydrochloride.

    Code of Federal Regulations, 2010 CFR

    2010-04-01

    ... Federal Register citations affecting § 558.515, see the List of CFR Sections Affected, which appears in... chapter. (d) Conditions of use. It is used in feed for chickens as follows: Robenidine hydrochloride in... and fryer chickens: As an aid in the prevention of coccidiosis caused by E. mivati, E. brunetti,...

  12. 21 CFR 556.410 - Metoserpate hydrochloride.

    Code of Federal Regulations, 2010 CFR

    2010-04-01

    ... 21 Food and Drugs 6 2010-04-01 2010-04-01 false Metoserpate hydrochloride. 556.410 Section 556.410 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL DRUGS, FEEDS, AND RELATED PRODUCTS TOLERANCES FOR RESIDUES OF NEW ANIMAL DRUGS IN FOOD Specific Tolerances for Residues of New Animal Drugs §...

  13. 21 CFR 556.580 - Robenidine hydrochloride.

    Code of Federal Regulations, 2011 CFR

    2011-04-01

    ... 21 Food and Drugs 6 2011-04-01 2011-04-01 false Robenidine hydrochloride. 556.580 Section 556.580 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL DRUGS, FEEDS, AND RELATED PRODUCTS TOLERANCES FOR RESIDUES OF NEW ANIMAL DRUGS IN FOOD...

  14. 21 CFR 556.580 - Robenidine hydrochloride.

    Code of Federal Regulations, 2010 CFR

    2010-04-01

    ... 21 Food and Drugs 6 2010-04-01 2010-04-01 false Robenidine hydrochloride. 556.580 Section 556.580 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL DRUGS, FEEDS, AND RELATED PRODUCTS TOLERANCES FOR RESIDUES OF NEW ANIMAL DRUGS IN FOOD Specific Tolerances for Residues of New Animal Drugs...

  15. 21 CFR 556.350 - Levamisole hydrochloride.

    Code of Federal Regulations, 2010 CFR

    2010-04-01

    ... 21 Food and Drugs 6 2010-04-01 2010-04-01 false Levamisole hydrochloride. 556.350 Section 556.350 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL DRUGS, FEEDS, AND RELATED PRODUCTS TOLERANCES FOR RESIDUES OF NEW ANIMAL DRUGS IN FOOD Specific Tolerances for Residues of New Animal Drugs...

  16. Coordination Structure Conversion of Hydrazone-Palladium(II) Complexes in the Solid State and in Solution.

    PubMed

    Kitamura, Fumi; Sawaguchi, Kana; Mori, Asami; Takagi, Shoji; Suzuki, Takayoshi; Kobayashi, Atsushi; Kato, Masako; Nakajima, Kiyohiko

    2015-09-01

    We prepared hydrazone-palladium(II) complexes of [PdCl2(HL(n))] and [PdCl(L(n))] (n = 1-3) by the reaction of [PdCl2(cod)] or [PdCl2(PhCN)2] and the hydrazone ligands of HL(n) {N'-(pyridin-2-ylmethylene)picolinohydrazide (HL(1)), N'-[1-(pyridin-2-yl)ethylidene]picolinohydrazide (HL(2)), and N'-[(6-methylpyridin-2-yl)methylene]picolinohydrazide (HL(3))}. The structures of the complexes were determined by X-ray analysis. The hydrazone ligands had κN(py1),κN(imine) and κN(amidate),κN(py2) bidentate coordination modes in [PdCl2(HL(n))] (1, n = 1; 2, n = 2) and in [PdCl2(HL(3))] (3), respectively. In contrast, tridentate coordination modes of κN(py1),κN(imine),κN(py2) and κN(py1),κN(amidate),κN(py2) were observed in [PdCl(L(n))] (4, n = 1; 5, n = 2) and in [PdCl(L(n))] (6, n = 1; 7, n = 2; 8, n = 3). Thermal conversion of complexes 1-3 to complexes 6-8 proceeded in acetonitrile. Complexes 4 and 5 were obtained from complexes 1 and 2, respectively, in a basic acetonitrile solution under dark conditions. Complex 4 reverted immediately to complex 1 in an acidic acetonitrile solution that included hydrochloric acid. However, under room light, in the basic acetonitrile solution that included trimethylamine, complex 4 converted photochemically to complex 6. The thermochromic or vapochromic structure conversion of these complexes also occurred in the solid state. On heating at 180 °C, the color of the crystals of complexes 1, 2, and 3 changed from yellow to orange in the solid state. (1)H NMR and/or UV-vis absorption spectroscopy confirmed that the orange complexes 6-8 were produced. The reddish-orange crystals of complexes 4 and 5 were exposed to hydrogen chloride vapor to yield the yellow products of complexes 1 and 2, respectively. PMID:26305775

  17. Optical and thermal properties of nickel(II) hydrazone complex for recordable blu-ray storage

    NASA Astrophysics Data System (ADS)

    Chen, Zhimin; Wu, Yiqun; Gu, Donghong; Gan, Fuxi

    2009-08-01

    A nickel(II) hydrazone complex was synthesized in order to obtain a suitable optical recording medium for the new generation recordable blu-ray disk. Smooth thin films of the nickel(II) hydrazone complex were prepared by using the spin-coating method. Absorption and reflectance spectra of the thin films were evaluated in the wavelength 300-700 nm. Thermal properties of the nickel(II) complex were investigated by thermogravimetry (TG) and differential scanning calorimetry (DSC). Optical constants (complex refractive indices N=n+ik) and thickness of the thin film, prepared on single-crystal silicon substrate, were investigated on a rotating analyzer-polarizer scanning ellipsometer in the wavelength 285-705 nm. In addition, in order to examine its possible use as a blu-ray recording medium, the spin-coated film of the nickel(II) complex was prepared on K9 glass substrate with a silver reflective layer, and was studied by static optical recording testing system with a 406.7 nm laser. It is found that the absorption spectra of the thin film has an strong absorption band in the wavelength region 360-420 nm and a moderate absorbance at the 405 nm side, which indicates that the absorption of the film is well matched with the laser wavelength of the 405 nm. The reflectance spectra show that a high reflectivity of the thin film at 405 nm wavelength can be obtained by an optimum film thickness and an appropriate metal reflective layer. The thin film of the nickel(II) complex gives a high n value of 1.62 and a low k value of 0.33, corresponding to the wavelength of the blue laser of 405 nm. Measurements of the thermal properties show that the nickel(II) complex holds a high thermal stability (~ 300 °C) and a sharp weight loss which are helpful to fabricate a small and sharp recording mark edge. The results of the static optical recording test, using the nickel(II) complex thin film as the recording layer, demonstrate that high reflectivity contrast (>50 %) can be obtained at

  18. Stability of esmolol hydrochloride in intravenous solutions.

    PubMed

    Baaske, D M; Dykstra, S D; Wagenknecht, D M; Karnatz, N N

    1994-11-01

    The stability of esmolol hydrochloride in a variety of i.v. solutions was studied. Solutions of esmolol hydrochloride 10 mg/mL were prepared separately in 0.45% sodium chloride injection, 0.9% sodium chloride injection, 5% dextrose injection, 5% dextrose and 0.45% sodium chloride injection, 5% dextrose and 0.9% sodium chloride injection, 5% dextrose with lactated Ringer's injection, lactated Ringer's injection, 5% sodium bicarbonate injection, and 5% dextrose injection with potassium chloride 40 meq/L. One glass and one polyvinyl chloride container of each solution (except glass only in the case of the solution in 5% sodium bicarbonate injection) were stored in the dark at 5 degrees C, under ambient room light at 23-27 degrees C, in the dark at 40 degrees C, and under intense light at 25-30 degrees C. At storage intervals up to 168 hours, samples were tested for esmolol hydrochloride concentration by high-performance liquid chromatography. Optical density and pH were also measured. Esmolol hydrochloride was stable in the various i.v. fluids for at least 168 hours when stored at 5 degrees C or 23-27 degrees C, for at least 24 hours when stored under intense light, and, with one exception, for at least 48 hours when stored at 40 degrees C. When mixed with 5% sodium bicarbonate injection, the drug was stable for only about 24 hours at 40 degrees C. There were no substantial changes in optical density or pH. The type of container had no effect on stability. With one exception, esmolol hydrochloride was stable in all the i.v. solutions under all the conditions tested. PMID:7856582

  19. Potassium N-Iodo p-Toluenesulfonamide (TsNIK, Iodamine-T): A New Reagent for the Oxidation of Hydrazones to Diazo Compounds

    PubMed Central

    Nicolle, Simon M; Moody, Christopher J

    2014-01-01

    A new reagent for the oxidation of hydrazones to diazo compounds is described. N-Iodo p-toluenesulfonamide (TsNIK, iodamine-T) allows the preparation of α-diazoesters, α-diazoamides, α-diazoketones and α-diazophosphonates in good yield and in high purity after a simple extractive work-up. α-Diazoesters were also obtained in high yield from the corresponding ketones through a one-pot process of hydrazone formation/oxidation. PMID:24615944

  20. Synthesis and evaluation of antioxidant phenolic diaryl hydrazones as potent antiangiogenic agents in atherosclerosis.

    PubMed

    Vanucci-Bacqué, Corinne; Camare, Caroline; Carayon, Chantal; Bernis, Corinne; Baltas, Michel; Nègre-Salvayre, Anne; Bedos-Belval, Florence

    2016-08-15

    A series of bis-hydrazones derived from diaryl and diaryl ether hydroxybenzaldehyde frames 1 and 2 have been synthesized as potential antioxidant and antiangiogenic agents, two properties required to limit atherogenesis and cardiovascular events. These compounds were evaluated for their ability to neutralize free radical formation, to block endothelial cell-induced low-density lipoprotein oxidation (monitored by the formation of TBARS), an essential step in atherogenesis, and subsequent toxicity, to prevent angiogenesis evoked by low oxidized LDL concentration (monitored by the formation of capillary tubes on Matrigel) and to inhibit intracellular ROS increase involved in the angiogenic signaling. A structure/activity study has been carried out and finally allowed to select the phenolic diaryl ether hydralazine derivative 2a, sharing all these protective properties, as a promising hit for further development. PMID:27288181

  1. Synthesis and antituberculosis activity of indole-pyridine derived hydrazides, hydrazide-hydrazones, and thiosemicarbazones.

    PubMed

    Velezheva, Valeriya; Brennan, Patrick; Ivanov, Pavel; Kornienko, Albert; Lyubimov, Sergey; Kazarian, Konstantin; Nikonenko, Boris; Majorov, Konstantin; Apt, Alexander

    2016-02-01

    We describe the design, synthesis, and in vitro antimycobacterial activity of a series of novel simple hybrid hydrazides and hydrazide-hydrazones combining indole and pyridine nuclei. The compounds are derivatives of 1-acetylindoxyl or substituted indole-3-carboxaldehydes tethered via a hydrazine group by simple C-N or double C=N bonds with 3- and 4-pyridines, 1-oxide 3- and 4-pyridine carbohydrazides. The most active of 15 compounds showed MICs values against an INH-sensitive strain of Mycobacterium tuberculosis H37Rv equal to that of INH (0.05-2 μg/mL). Five compounds demonstrated appreciable activity against the INH-resistant M. tuberculosis CN-40 clinical isolate (MICs: 2-5 μg/mL), providing justification for further in vivo studies. PMID:26725953

  2. Synthesis and anticandidal evaluation of new benzothiazole derivatives with hydrazone moiety.

    PubMed

    Yurttaş, Leyla; Kaplancıklı, Zafer Asım; Göger, Gamze; Demirci, Fatih

    2016-10-01

    In this study, we have performed the synthesis of new N'-(arylidene)-4-[(benzothiazol-2-yl)thio]butanoylhydrazide derivatives (3a-s) bearing azole moiety and hydrazone group in a lipophilic structural framework. The target compounds were prepared by a three step synthetic procedure starting from 2-mercaptobenzothiazole. The structures of the target compounds were elucidated by IR, (1)H NMR, (13)C NMR spectra and elemental analysis. The antifungal activity of the obtained compounds has been determined against a number of clinic and fluconazole-resistant Candida strains by using microdilution method. Compounds (3a-3s) exhibited anticandidal activity in different ratios varying between the range of MIC: 50 and 200 µg/mL. PMID:26247354

  3. Bulk synthesis of exfoliated two-dimensional polymers using hydrazone-linked covalent organic frameworks.

    PubMed

    Bunck, David N; Dichtel, William R

    2013-10-01

    Two-dimensional (2D) polymers assemble organic subunits into covalently linked, high-aspect-ratio networks with long-range order. Despite recent advances in 2D polymerization, scalable and general methods to access few- and single-layer materials are limited. Here we exfoliate a hydrazone-linked covalent organic framework (COF) to yield bulk quantities of few-layer two-dimensional (2D) polymers. Immersing the COF powder in several laboratory solvents exfoliates and disperses thin COF-43 samples, which maintain their characteristic periodic hexagonal structure. This phenomenon was characterized using infrared spectroscopy, dynamic light scattering, atomic force microscopy, transmission electron microscopy, and selected area electron diffraction. 2D COFs with reduced interlayer interaction energies offer a new means to access high-aspect-ratio 2D polymers whose structure may be designed using established principles of COF synthesis. PMID:24053107

  4. Synthesis, characterization and anticancer evaluation of novel tri-arm star shaped 1,3,5-triazine hydrazones

    NASA Astrophysics Data System (ADS)

    Machakanur, Shrinath S.; Patil, Basavaraj R.; Badiger, Dayananda S.; Bakale, Raghavendra P.; Gudasi, Kalagouda B.; Annie Bligh, S. W.

    2012-03-01

    A series of novel trisubstituted triazine hydrazones [N3C3(sbnd OC6H4-p-CHdbnd Nsbnd NHsbnd C(O)sbnd C6H4-p-X)3] (X = H, Br, Cl, F, OH, OCH3, CH3, NO2, NH2) were prepared by a three-fold condensation reaction of 2,4,6-tris(4-formylphenoxy)-1,3,5-triazine with p-substituted benzoic acid hydrazides [NH2sbnd NHsbnd C(O)sbnd C6H4-p-X] with excellent yields. The structures were confirmed by elemental analysis, FT-IR, 1H, 13C, 2D-HSQC NMR and mass spectrometry (MALDI-TOF). These derivatives bearing hydrolysable hydrazone linkages were evaluated for their invitro antiproliferative activity against the human liver carcinoma cell line (HepG2) and human cervix carcinoma cell line (HeLa).

  5. Phenylazoindole dyes 3: Determination of azo-hydrazone tautomers of new phenylazoindole dyes in solution and solid state

    NASA Astrophysics Data System (ADS)

    Babür, Banu; Seferoğlu, Nurgül; Aktan, Ebru; Hökelek, Tuncer; Şahin, Ertan; Seferoğlu, Zeynel

    2015-02-01

    A new two series of phenylazo indole dyes was synthesized and the structures of the dyes were confirmed by UV-vis, FT-IR, HRMS and 1H/13C NMR spectroscopic techniques. Five of these dyes (I, I‧, II‧, III and III‧) were also characterized in solid state by using single crystal X-ray diffraction studies besides other spectroscopic techniques. The geometries of the azo and hydrazone tautomeric forms of the dyes were optimized by using Density Functional Theory (DFT). In addition, the effects of the donor and acceptor groups on the azo and hydrazone forms of the dyes were evaluated experimentally and theoretically. The results indicate that the phenylazoindole dyes derived from 2-phenyl indole as coupling component exist as azo form in solution, gas phase and solid state.

  6. Study on fluorescence characteristics of duloxetine hydrochloride

    NASA Astrophysics Data System (ADS)

    Liu, Xiangping; Du, Yingxiang; Wu, Xiulan

    2008-12-01

    The fluorescence characteristics of duloxetine hydrochloride are studied in this paper. The fluorescence emission spectra of duloxetine demonstrate that intramolecular charge-transfer takes place between thiophene ring and napthalenyloxy group upon irradiation. The effects of excitation light, solvent system, variation of solution pH value, metal ions and vitamin C on the fluorescence spectra of duloxetine hydrochloride are elucidated, respectively. A spectrofluorometric method of quantitative determination of duloxetine in dosage form is reported for the first time, the linear range is 7.14 × 10 -8 mol/L to 1.43 × 10 -5 mol/L, the linear correlation coefficient r is equal to 0.9997, and the detection limit is 3.5 × 10 -8 mol/L. The accuracy and the precision are satisfactory.

  7. Flow injection potentiometric determination of pipazethate hydrochloride.

    PubMed

    Abdel-Ghani, N T; Shoukry, A F; el Nashar, R M

    2001-01-01

    New plastic membrane electrodes for pipazethate hydrochloride based on pipazethatium phosphotungstate, pipazethatium phosphomolybdate and a mixture of the two were prepared. The electrodes were fully characterized in terms of composition, life span, pH and temperature and were then applied to the potentiometric determination of the pipazethate ion in its pure state and pharmaceutical preparations under batch and flow injection conditions. The selectivity of the electrodes towards many inorganic cations, sugars and amino acids was also tested. PMID:11205518

  8. New Organocatalyst Scaffolds with High Activity in Promoting Hydrazone and Oxime Formation at Neutral pH

    PubMed Central

    2015-01-01

    The discovery of two new classes of catalysts for hydrazone and oxime formation in water at neutral pH, namely 2-aminophenols and 2-(aminomethyl)benzimidazoles, is reported. Kinetics studies in aqueous solutions at pH 7.4 revealed rate enhancements up to 7-fold greater than with classic aniline catalysis. 2-(Aminomethyl)benzimidazoles were found to be effective catalysts with otherwise challenging aryl ketone substrates. PMID:25545888

  9. Spectrophotometric, difference spectroscopic, and high-performance liquid chromatographic methods for the determination of cefixime in pharmaceutical formulations.

    PubMed

    Shah, Paresh B; Pundarikakshudu, Kilambi

    2006-01-01

    Three simple and sensitive spectrophotometric, difference spectroscopic, and liquid chromatographic (LC) methods are described for the determination of cefixime. The first method is based on the oxidative coupling reaction of cefixime with 3-methyl-2-benzothiazolinon hydrazone HCI in presence of ferric chloride. The absorbance of reaction product was measured at the maximum absorbance wavelength (wavelength(max)), 630 nm. The difference spectroscopic method is based on the measurement of absorbance of cefixime at the absorbance maximum, 268 nm, and minimum, 237 nm. The measured value was the amplitude of maxima and minima between 2 equimolar solutions of the analyte in different chemical forms, which exhibited different spectral characteristics. The conditions were optimized, and Beer's law was obeyed for cefixime at 1 to 16 microg/mL and 10 to 50 microg/mL, respectively. The third method, high-performance LC, was developed for the determination of cefixime using 50 mM potassium dihydrogen phosphate (pH 3.0)-methanol (78 + 22, v/v) as the mobile phase and measuring the response at wavelength(max) 286 nm. The analysis was performed on a Lichrospher RPC18 column. The calibration curve was obtained for cefixime at 5 to 250 microg/mL, and the mean recovery was 99.71 +/- 0.01%. The methods were validated according to the guidelines of the U.S. Pharmacopoeia and also assessed by applying the standard addition technique. The results obtained in the analysis of dosage forms agreed well with the contents stated on the labels. PMID:16915834

  10. 21 CFR 520.2345a - Tetracycline hydrochloride capsules.

    Code of Federal Regulations, 2011 CFR

    2011-04-01

    ... organisms sensitive to tetracycline hydrochloride, such as bacterial gastroenteritis due to E. coli and urinary tract infections due to Staphylococcus spp. and E. coli. (3) Limitations. Federal law...

  11. 21 CFR 520.2345a - Tetracycline hydrochloride capsules.

    Code of Federal Regulations, 2010 CFR

    2010-04-01

    ... organisms sensitive to tetracycline hydrochloride, such as bacterial gastroenteritis due to E. coli and urinary tract infections due to Staphylococcus spp. and E. coli. (3) Limitations. Federal law...

  12. 21 CFR 520.2345a - Tetracycline hydrochloride capsules.

    Code of Federal Regulations, 2013 CFR

    2013-04-01

    ... organisms sensitive to tetracycline hydrochloride, such as bacterial gastroenteritis due to E. coli and urinary tract infections due to Staphylococcus spp. and E. coli. (3) Limitations. Federal law...

  13. 21 CFR 520.2345a - Tetracycline hydrochloride capsules.

    Code of Federal Regulations, 2014 CFR

    2014-04-01

    ... organisms sensitive to tetracycline hydrochloride, such as bacterial gastroenteritis due to E. coli and urinary tract infections due to Staphylococcus spp. and E. coli. (3) Limitations. Federal law...

  14. 21 CFR 520.2345a - Tetracycline hydrochloride capsules.

    Code of Federal Regulations, 2012 CFR

    2012-04-01

    ... organisms sensitive to tetracycline hydrochloride, such as bacterial gastroenteritis due to E. coli and urinary tract infections due to Staphylococcus spp. and E. coli. (3) Limitations. Federal law...

  15. Synthesis, crystal structures and spectroscopic properties of triazine-based hydrazone derivatives; a comparative experimental-theoretical study.

    PubMed

    Arshad, Muhammad Nadeem; Bibi, Aisha; Mahmood, Tariq; Asiri, Abdullah M; Ayub, Khurshid

    2015-01-01

    We report here a comparative theoretical and experimental study of four triazine-based hydrazone derivatives. The hydrazones are synthesized by a three step process from commercially available benzil and thiosemicarbazide. The structures of all compounds were determined by using the UV-Vis., FT-IR, NMR (1H and 13C) spectroscopic techniques and finally confirmed unequivocally by single crystal X-ray diffraction analysis. Experimental geometric parameters and spectroscopic properties of the triazine based hydrazones are compared with those obtained from density functional theory (DFT) studies. The model developed here comprises of geometry optimization at B3LYP/6-31G (d, p) level of DFT. Optimized geometric parameters of all four compounds showed excellent correlations with the results obtained from X-ray diffraction studies. The vibrational spectra show nice correlations with the experimental IR spectra. Moreover, the simulated absorption spectra also agree well with experimental results (within 10-20 nm). The molecular electrostatic potential (MEP) mapped over the entire stabilized geometries of the compounds indicated their chemical reactivates. Furthermore, frontier molecular orbital (electronic properties) and first hyperpolarizability (nonlinear optical response) were also computed at the B3LYP/6-31G (d, p) level of theory. PMID:25854752

  16. Effect of Ractopamine Hydrochloride and Zilpaterol Hydrochloride on tenderness of longissimus steaks of Bos Taurus steers

    Technology Transfer Automated Retrieval System (TEKTRAN)

    Objectives: Three experiments were conducted to determine 1) the interaction of ractopamine hydrochloride (RH) inclusion rate (0 or 300 mg·hd-1·d-1 for last 30 to 34 d before harvest) and dietary protein level (13.5 or 17.5% CP) on LM slice shear force (SSF) at 14 d postmortem (Exp. 1); 2) the inter...

  17. 21 CFR 522.2474 - Tolazoline hydrochloride injection.

    Code of Federal Regulations, 2013 CFR

    2013-04-01

    ... 21 Food and Drugs 6 2013-04-01 2013-04-01 false Tolazoline hydrochloride injection. 522.2474 Section 522.2474 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES... solution contains tolazoline hydrochloride equivalent to 100 milligrams of base activity. (b) Sponsor....

  18. 21 CFR 522.2474 - Tolazoline hydrochloride injection.

    Code of Federal Regulations, 2010 CFR

    2010-04-01

    ... 21 Food and Drugs 6 2010-04-01 2010-04-01 false Tolazoline hydrochloride injection. 522.2474 Section 522.2474 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES... solution contains tolazoline hydrochloride equivalent to 100 milligrams of base activity. (b) Sponsor....

  19. 21 CFR 522.2474 - Tolazoline hydrochloride injection.

    Code of Federal Regulations, 2012 CFR

    2012-04-01

    ... 21 Food and Drugs 6 2012-04-01 2012-04-01 false Tolazoline hydrochloride injection. 522.2474 Section 522.2474 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES... solution contains tolazoline hydrochloride equivalent to 100 milligrams of base activity. (b) Sponsor....

  20. 21 CFR 522.2474 - Tolazoline hydrochloride injection.

    Code of Federal Regulations, 2011 CFR

    2011-04-01

    ... 21 Food and Drugs 6 2011-04-01 2011-04-01 false Tolazoline hydrochloride injection. 522.2474 Section 522.2474 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES... solution contains tolazoline hydrochloride equivalent to 100 milligrams of base activity. (b) Sponsor....

  1. 40 CFR 180.276 - Formetanate hydrochloride; tolerances for residues.

    Code of Federal Regulations, 2010 CFR

    2010-07-01

    ..., wet pomace 1.5 Grapefruit 1.5 Lemon 0.60 Lime 0.03 Nectarine 0.40 Orange 1.5 Peach 0.40 Pear 0.50... established for residues of the insecticide formetanate hydrochloride (m- amino ]phenyl methylcarbamate... for residues of the insecticide formetanate hydrochloride (m- amino ]phenyl...

  2. 21 CFR 522.536 - Detomidine hydrochloride injection.

    Code of Federal Regulations, 2011 CFR

    2011-04-01

    ... 21 Food and Drugs 6 2011-04-01 2011-04-01 false Detomidine hydrochloride injection. 522.536 Section 522.536 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL DRUGS, FEEDS, AND RELATED PRODUCTS IMPLANTATION OR INJECTABLE DOSAGE FORM NEW ANIMAL DRUGS § 522.536 Detomidine hydrochloride...

  3. 21 CFR 522.1222 - Ketamine hydrochloride injectable dosage forms.

    Code of Federal Regulations, 2011 CFR

    2011-04-01

    ... 21 Food and Drugs 6 2011-04-01 2011-04-01 false Ketamine hydrochloride injectable dosage forms. 522.1222 Section 522.1222 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN... ANIMAL DRUGS § 522.1222 Ketamine hydrochloride injectable dosage forms....

  4. 21 CFR 522.1222 - Ketamine hydrochloride injectable dosage forms.

    Code of Federal Regulations, 2013 CFR

    2013-04-01

    ... 21 Food and Drugs 6 2013-04-01 2013-04-01 false Ketamine hydrochloride injectable dosage forms. 522.1222 Section 522.1222 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN... ANIMAL DRUGS § 522.1222 Ketamine hydrochloride injectable dosage forms....

  5. 21 CFR 522.1222 - Ketamine hydrochloride injectable dosage forms.

    Code of Federal Regulations, 2012 CFR

    2012-04-01

    ... 21 Food and Drugs 6 2012-04-01 2012-04-01 false Ketamine hydrochloride injectable dosage forms. 522.1222 Section 522.1222 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN... ANIMAL DRUGS § 522.1222 Ketamine hydrochloride injectable dosage forms....

  6. 40 CFR 721.4460 - Amidinothiopropionic acid hydrochloride.

    Code of Federal Regulations, 2013 CFR

    2013-07-01

    ... 40 Protection of Environment 32 2013-07-01 2013-07-01 false Amidinothiopropionic acid... Specific Chemical Substances § 721.4460 Amidinothiopropionic acid hydrochloride. (a) Chemical substance and... amidinothiopropionic acid hydrochloride (PMN P-91-102) is subject to reporting under this section for the...

  7. 21 CFR 522.1222 - Ketamine hydrochloride injectable dosage forms.

    Code of Federal Regulations, 2010 CFR

    2010-04-01

    ... 21 Food and Drugs 6 2010-04-01 2010-04-01 false Ketamine hydrochloride injectable dosage forms. 522.1222 Section 522.1222 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN... ANIMAL DRUGS § 522.1222 Ketamine hydrochloride injectable dosage forms....

  8. 21 CFR 520.1263c - Lincomycin hydrochloride soluble powder.

    Code of Federal Regulations, 2010 CFR

    2010-04-01

    ... 21 Food and Drugs 6 2010-04-01 2010-04-01 false Lincomycin hydrochloride soluble powder. 520.1263c Section 520.1263c Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES... Lincomycin hydrochloride soluble powder. (a) Specifications. Each gram of soluble powder contains...

  9. 21 CFR 520.1263c - Lincomycin hydrochloride soluble powder.

    Code of Federal Regulations, 2011 CFR

    2011-04-01

    ... 21 Food and Drugs 6 2011-04-01 2011-04-01 false Lincomycin hydrochloride soluble powder. 520.1263c Section 520.1263c Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES... Lincomycin hydrochloride soluble powder. (a) Specifications. Each gram of soluble powder contains...

  10. 21 CFR 520.1263c - Lincomycin hydrochloride soluble powder.

    Code of Federal Regulations, 2012 CFR

    2012-04-01

    ... 21 Food and Drugs 6 2012-04-01 2012-04-01 false Lincomycin hydrochloride soluble powder. 520.1263c Section 520.1263c Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL DRUGS, FEEDS, AND RELATED PRODUCTS ORAL DOSAGE FORM NEW ANIMAL DRUGS § 520.1263c Lincomycin hydrochloride soluble powder....

  11. 21 CFR 520.2098 - Selegiline hydrochloride tablets.

    Code of Federal Regulations, 2010 CFR

    2010-04-01

    ... 21 Food and Drugs 6 2010-04-01 2010-04-01 false Selegiline hydrochloride tablets. 520.2098 Section 520.2098 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES... hydrochloride tablets. (a) Specifications. Each tablet contains either 2, 5, 10, 15, or 30 milligrams...

  12. 21 CFR 520.2098 - Selegiline hydrochloride tablets.

    Code of Federal Regulations, 2012 CFR

    2012-04-01

    ... 21 Food and Drugs 6 2012-04-01 2012-04-01 false Selegiline hydrochloride tablets. 520.2098 Section 520.2098 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES... hydrochloride tablets. (a) Specifications. Each tablet contains either 2, 5, 10, 15, or 30 milligrams...

  13. 21 CFR 520.1242e - Levamisole hydrochloride effervescent tablets.

    Code of Federal Regulations, 2013 CFR

    2013-04-01

    ... 21 Food and Drugs 6 2013-04-01 2013-04-01 false Levamisole hydrochloride effervescent tablets. 520....1242e Levamisole hydrochloride effervescent tablets. (a) Specifications. Each tablet contains 907... water from pigs before treatment is not necessary. Add one tablet for each 21/2 gallons of water;...

  14. 21 CFR 520.2582 - Triflupromazine hydrochloride tablets.

    Code of Federal Regulations, 2013 CFR

    2013-04-01

    ... 21 Food and Drugs 6 2013-04-01 2013-04-01 false Triflupromazine hydrochloride tablets. 520.2582 Section 520.2582 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES... Triflupromazine hydrochloride tablets. (a) Specifications. Each tablet contains either 10 milligrams or...

  15. 21 CFR 520.1242e - Levamisole hydrochloride effervescent tablets.

    Code of Federal Regulations, 2012 CFR

    2012-04-01

    ... 21 Food and Drugs 6 2012-04-01 2012-04-01 false Levamisole hydrochloride effervescent tablets. 520....1242e Levamisole hydrochloride effervescent tablets. (a) Specifications. Each tablet contains 907... water from pigs before treatment is not necessary. Add one tablet for each 21/2 gallons of water;...

  16. 21 CFR 520.863 - Ethylisobutrazine hydrochloride tablets.

    Code of Federal Regulations, 2010 CFR

    2010-04-01

    ... 21 Food and Drugs 6 2010-04-01 2010-04-01 false Ethylisobutrazine hydrochloride tablets. 520.863 Section 520.863 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES... Ethylisobutrazine hydrochloride tablets. (a) Specifications. Each tablet contains either 10 milligrams or...

  17. 21 CFR 520.863 - Ethylisobutrazine hydrochloride tablets.

    Code of Federal Regulations, 2012 CFR

    2012-04-01

    ... 21 Food and Drugs 6 2012-04-01 2012-04-01 false Ethylisobutrazine hydrochloride tablets. 520.863 Section 520.863 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES... Ethylisobutrazine hydrochloride tablets. (a) Specifications. Each tablet contains either 10 milligrams or...

  18. 21 CFR 520.863 - Ethylisobutrazine hydrochloride tablets.

    Code of Federal Regulations, 2013 CFR

    2013-04-01

    ... 21 Food and Drugs 6 2013-04-01 2013-04-01 false Ethylisobutrazine hydrochloride tablets. 520.863 Section 520.863 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES... Ethylisobutrazine hydrochloride tablets. (a) Specifications. Each tablet contains either 10 milligrams or...

  19. 21 CFR 520.2098 - Selegiline hydrochloride tablets.

    Code of Federal Regulations, 2014 CFR

    2014-04-01

    ... 21 Food and Drugs 6 2014-04-01 2014-04-01 false Selegiline hydrochloride tablets. 520.2098 Section 520.2098 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES... hydrochloride tablets. (a) Specifications. Each tablet contains either 2, 5, 10, 15, or 30 milligrams...

  20. 21 CFR 520.2098 - Selegiline hydrochloride tablets.

    Code of Federal Regulations, 2011 CFR

    2011-04-01

    ... 21 Food and Drugs 6 2011-04-01 2011-04-01 false Selegiline hydrochloride tablets. 520.2098 Section 520.2098 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES... hydrochloride tablets. (a) Specifications. Each tablet contains either 2, 5, 10, 15, or 30 milligrams...

  1. 21 CFR 520.863 - Ethylisobutrazine hydrochloride tablets.

    Code of Federal Regulations, 2014 CFR

    2014-04-01

    ... 21 Food and Drugs 6 2014-04-01 2014-04-01 false Ethylisobutrazine hydrochloride tablets. 520.863 Section 520.863 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES... Ethylisobutrazine hydrochloride tablets. (a) Specifications. Each tablet contains either 10 milligrams or...

  2. 21 CFR 520.2582 - Triflupromazine hydrochloride tablets.

    Code of Federal Regulations, 2012 CFR

    2012-04-01

    ... 21 Food and Drugs 6 2012-04-01 2012-04-01 false Triflupromazine hydrochloride tablets. 520.2582 Section 520.2582 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES... Triflupromazine hydrochloride tablets. (a) Specifications. Each tablet contains either 10 milligrams or...

  3. 21 CFR 520.863 - Ethylisobutrazine hydrochloride tablets.

    Code of Federal Regulations, 2011 CFR

    2011-04-01

    ... 21 Food and Drugs 6 2011-04-01 2011-04-01 false Ethylisobutrazine hydrochloride tablets. 520.863 Section 520.863 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES... Ethylisobutrazine hydrochloride tablets. (a) Specifications. Each tablet contains either 10 milligrams or...

  4. 21 CFR 520.2098 - Selegiline hydrochloride tablets.

    Code of Federal Regulations, 2013 CFR

    2013-04-01

    ... 21 Food and Drugs 6 2013-04-01 2013-04-01 false Selegiline hydrochloride tablets. 520.2098 Section 520.2098 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES... hydrochloride tablets. (a) Specifications. Each tablet contains either 2, 5, 10, 15, or 30 milligrams...

  5. 21 CFR 520.2582 - Triflupromazine hydrochloride tablets.

    Code of Federal Regulations, 2014 CFR

    2014-04-01

    ... 21 Food and Drugs 6 2014-04-01 2014-04-01 false Triflupromazine hydrochloride tablets. 520.2582 Section 520.2582 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES... Triflupromazine hydrochloride tablets. (a) Specifications. Each tablet contains either 10 milligrams or...

  6. Synthesis, characterization, investigation of biological activity and theoretical studies of hydrazone compounds containing choloroacetyl group

    NASA Astrophysics Data System (ADS)

    Cukurovali, Alaaddin; Yilmaz, Engin

    2014-10-01

    In this study, three new hydrazide-hydrazone derivative compounds which contain choloroacetyl group have been synthesized and characterized. In the characterization, spectral techniques such as IR, 1H NMR, 13C NMR and UV-Vis spectroscopy techniques were used. Antibacterial effects of the synthesized compounds were investigated against Staphylococcus aureus ATCC 29213, Enterococcus faecalis ATCC 29212, Escherichia coli ATCC 25922 and Pseudomonas aeruginosa ATCC 27853. In the theoretical calculations Gaussian 09 software was used with the DFT/6-311+(d,p) basis set. Experimental X-ray analysis of compounds has not been studied. Theoretical bond lengths of synthesized compounds were compared with experimental bond lengths of a similar compound. Theoretical and experimental bond lengths are in good agreement with R2: 0.896, 0.899 and 0.900 for compounds 1, 2, and 3, respectively. For antibacterial activity, the most effective one was found to be N‧-(4-bromobenzylidene)-2-chloro-N-(4-(3-methyl-3-phenylcyclobutyl)-thiazol-2-yl) acetohydrazide against P.aeroginaosa ATTC 27853, among the studied compounds.

  7. Catalytic N-radical cascade reaction of hydrazones by oxidative deprotonation electron transfer and TEMPO mediation.

    PubMed

    Hu, Xiao-Qiang; Qi, Xiaotian; Chen, Jia-Rong; Zhao, Quan-Qing; Wei, Qiang; Lan, Yu; Xiao, Wen-Jing

    2016-01-01

    Compared with the popularity of various C-centred radicals, the N-centred radicals remain largely unexplored in catalytic radical cascade reactions because of a lack of convenient methods for their generation. Known methods for their generation typically require the use of N-functionalized precursors or various toxic, potentially explosive or unstable radical initiators. Recently, visible-light photocatalysis has emerged as an attractive tool for the catalytic formation of N-centred radicals, but the pre-incorporation of a photolabile groups at the nitrogen atom largely limited the reaction scope. Here, we present a visible-light photocatalytic oxidative deprotonation electron transfer/2,2,6,6-tetramethylpiperidine-1-oxyl (TEMPO)-mediation strategy for catalytic N-radical cascade reaction of unsaturated hydrazones. This mild protocol provides a broadly applicable synthesis of 1,6-dihydropyradazines with complete regioselectivity and good yields. The 1,6-dihydropyradazines can be easily transformed into diazinium salts that showed promising in vitro antifungal activities against fungal pathogens. DFT calculations are conducted to explain the mechanism. PMID:27048886

  8. Synthesis, growth and characterization of a new promising organic nonlinear optical crystal: 4-Nitrophenyl hydrazone.

    PubMed

    Hemaraju, B C; Ahlam, M A; Pushpa, N; Mahadevan, K M; Gnana Prakash, A P

    2015-12-01

    4-Nitrophenyl hydrazone single crystals were grown by slow evaporation of solvent method using acetone as a solvent. The grown crystals were subjected to various characterizations such as X-ray diffraction studies, UV-visible studies, thermogravimetric analysis and differential thermal analysis (TGA/DTA) and second harmonic generation (SHG). The cell parameters were calculated by using single crystal XRD measurement and the crystal system was found as orthorhombic with non-centro-symmetric space group Pca21. The crystallinity of the grown crystal was confirmed by powder X-ray diffraction analysis. The Fourier transform infrared (FTIR) and nuclear magnetic resonance (NMR) studies confirmed the presence of functional groups in the sample. The optical transmittance spectrum shows that the crystal is transparent in the visible wavelength range. The scanning electron microscopy (SEM) was used to study the surface morphology of the grown crystal. The chemical composition of the grown crystal was confirmed by energy dispersive X-ray (EDX) analysis. The TGA/DTA results showed that the material is stable up to 146°C. The NLO property of the crystal was confirmed by Kurtz and Perry method and SHG conversion efficiency is 15.39 times when compared to KDP crystal. PMID:26184469

  9. Catalytic N-radical cascade reaction of hydrazones by oxidative deprotonation electron transfer and TEMPO mediation

    PubMed Central

    Hu, Xiao-Qiang; Qi, Xiaotian; Chen, Jia-Rong; Zhao, Quan-Qing; Wei, Qiang; Lan, Yu; Xiao, Wen-Jing

    2016-01-01

    Compared with the popularity of various C-centred radicals, the N-centred radicals remain largely unexplored in catalytic radical cascade reactions because of a lack of convenient methods for their generation. Known methods for their generation typically require the use of N-functionalized precursors or various toxic, potentially explosive or unstable radical initiators. Recently, visible-light photocatalysis has emerged as an attractive tool for the catalytic formation of N-centred radicals, but the pre-incorporation of a photolabile groups at the nitrogen atom largely limited the reaction scope. Here, we present a visible-light photocatalytic oxidative deprotonation electron transfer/2,2,6,6-tetramethylpiperidine-1-oxyl (TEMPO)-mediation strategy for catalytic N-radical cascade reaction of unsaturated hydrazones. This mild protocol provides a broadly applicable synthesis of 1,6-dihydropyradazines with complete regioselectivity and good yields. The 1,6-dihydropyradazines can be easily transformed into diazinium salts that showed promising in vitro antifungal activities against fungal pathogens. DFT calculations are conducted to explain the mechanism. PMID:27048886

  10. Z-Group ketone chain transfer agents for RAFT polymer nanoparticle modification via hydrazone conjugation

    PubMed Central

    Bandyopadhyay, Saibal; Xia, Xin; Maiseiyeu, Andrei; Mihai, Georgeta; Rajagopalan, Sanjay

    2012-01-01

    A ketal-containing trithiocarbonyl compound has been synthesized and characterized as a chain transfer agent (CTA) in Reversible Addition Fragmentation Transfer (RAFT) polymerization. The ketal functionality does not interfere with RAFT polymerization of acrylate monomers, which proceeds as previously reported to yield macro-CTA polymers and block co-polymers. Post-polymerization ketal cleavage revealed ketone functionality at the polar terminus of an amphiphilic block co-polymer. Hydrazone-formation was facile in both organic solution as well as in aqueous buffer where polymer nanoparticle assemblies were formed, indicating a conjugation/end-functionalization yield of 40–50%. Conjugation was verified with fluorescein, biotin and Gd-DOTA derivatives, and though the trithiocarbonate linkage is hydrolytically labile, we observed stable conjugation for several days at pH 7.4. and 37°C. As expected, streptavidin binding to biotinylated polymer micelles was observed, and size-change based relaxivity increases were observed when Gd-DOTA hydrazide was conjugated to polymer micelles. Cell-uptake of fluorescently labeled polymer micelles was also readily tracked by FACS and fluorescence microscopy. These polymer derivatives demonstrate a range of potential theranostic/biotechnological applications for this conveniently accessible keto-CTA, which include ligand-based nanoparticle targeting and fluorescent/MR nanoparticle contrast agents. PMID:23148126

  11. Switching mechanisms and role of entropy in chemically controlled hydrazone-based switches

    NASA Astrophysics Data System (ADS)

    Derian, Rene; Stich, Ivan

    2015-03-01

    Chemically controlled synthetic rotary switches are important as they resemble rotary motors found in nature. In order to elucidate the recent experiments, using hybrid QM/MM methods we have studied chemically controlled hydrazone-based switches in a strongly polar solvent. The experiments indicate a controlled E -->Z-H+ switching by addition of acid and thermal backward isomerization. We have studied the Z -->E switching mechanisms and the role of entropy. We find use of explicit MM solvent crucial for understanding the huge dipole moments (>10D) in the Z conformation and significantly smaller (~5D) in the E conformation and at the transition state, pointing toward very different ordering in those states. Furthermore, the internal and free energy surfaces from thermodynamic integration are qualitatively very different with the free energy surface exhibiting much smaller energy differences between E and Z. In addition, the solvent causes a pronounced shift (~30°) in the position of the Z states from internal and free energies. Both finding highlight the role of the entropy in the switching process and help a quantitative understanding of the switching in the solvent. Supported by APVV-0207-11 and VEGA (2/0007/12) projects.

  12. Dark Hydrazone Fluorescence Labeling Agents Enable Imaging of Cellular Aldehydic Load.

    PubMed

    Yuen, Lik Hang; Saxena, Nivedita S; Park, Hyun Shin; Weinberg, Kenneth; Kool, Eric T

    2016-08-19

    Aldehydes are key intermediates in many cellular processes, from endogenous metabolic pathways like glycolysis to undesired exogenously induced processes such as lipid peroxidation and DNA interstrand cross-linking. Alkyl aldehydes are well documented to be cytotoxic, affecting the functions of DNA and protein, and their levels are tightly regulated by the oxidative enzyme ALDH2. Mutations in this enzyme are associated with cardiac damage, diseases such as Fanconi anemia (FA), and cancer. Many attempts have been made to identify and quantify the overall level of these alkyl aldehydes inside cells, yet there are few practical methods available to detect and monitor these volatile aldehydes in real time. Here, we describe a multicolor fluorogenic hydrazone transfer ("DarkZone") system to label alkyl aldehydes, yielding up to 30-fold light-up response in vitro. A cell-permeant DarkZone dye design was applied to detect small-molecule aldehydes in the cellular environment. The new dye design also enabled the monitoring of cellular acetaldehyde production from ethanol over time by flow cytometry, demonstrating the utility of the DarkZone dyes for measuring and imaging the aldehydic load related to human disease. PMID:27326450

  13. Synthesis, characterization and studies on the nonlinear optical parameters of hydrazones

    NASA Astrophysics Data System (ADS)

    Naseema, K.; Sujith, K. V.; Manjunatha, K. B.; Kalluraya, Balakrishna; Umesh, G.; Rao, Vijayalakshmi

    2010-07-01

    Three hydrazones, 2-(4-methylphenoxy)- N'-[(1E)-(4-nitrophenyl)methylene]acetohydrazide (compound-1), 2-(4-methylphenoxy)- N'-[(1E)-(4-methylphenyl)methylene]acetohydrazide ((compound-2) and N'-{(1E)-[4-(dimethylamino)phenyl]methylene}-2-(4-ethylphenoxy) acetohydrazide(compound-3) were synthesized and their third order nonlinear optical properties were investigated using a single beam z-scan technique with nanosecond laser pulses at 532 nm. Open aperture data obtained from the three compounds indicates two photon absorption at this wavelength. The nonlinear refractive index n2, the nonlinear absorption coefficient β, the magnitude of the effective third order susceptibility χ(3), the second order hyperpolarizability γh and the coupling factor ρ have been estimated. The values obtained are comparable with the values obtained for 4-methoxy chalcone derivatives and dibenzylidene acetone derivatives. Among the compounds studied, compounds-1 and 3 exhibited the better optical power limiting behaviour at 532 nm. Our studies suggest that compounds-1, 2 and 3 are potential candidates for optical device applications such as optical limiters and optical switches.

  14. Radiation induced conductivity of polycarbonate doped with different concentrations of aromatic hydrazone DEH

    NASA Astrophysics Data System (ADS)

    Vladimir, Saenko; Novikov, Lev; Tyutnev, Andrey

    Radiation induced conductivity (RIC) of polymers widely used on present-day spacecraft plays is an important factor affecting their charging by the hot plasma of the Earth’s magnetosphere. As a result, researchers pay special attention to laboratory investigations of RIC in polymers excited by 10 -100 keV electrons prevailing in the hot magnetospheric plasma, including auroral radiation. Due to fluctuating fluxes of plasma electrons and especially of auroral electrons, it is very important to know how RIC depends on time. In our report we present RIC results observed in polycarbonate (PC) molecularly doped with aromatic hydrazone DEH (10 to 30 mas. percent) under continuous irradiation with 50 keV electrons. It has been found that RIC behavior in this material differs markedly from what we observed earlier in most of the polymers. After beginning of the stepwise irradiation, the RIC of PC+DEH rises fast to the quasistationary level but unlike common polymers, does not fall by an order of magnitude, instead it starts to increase further thus causing the accumulating space charge to decrease. This fact combined with the confirmed high radiation and temperature tolerance allows us to recommend this material for application on the spacecraft outer surface and specifically, as a thermal blanket.

  15. Experimental and theoretical studies on methanesulfonic acid 1-methylhydrazide: Antimicrobial activities of its sulfonyl hydrazone derivatives

    NASA Astrophysics Data System (ADS)

    Özbek, Neslihan; Alyar, Saliha; Karacan, Nurcan

    2009-12-01

    Methanesulfonic acid 1-methylhydrazide ( msmh) and its sulfonyl hydrazone derivatives, salicylaldehyde- N-methylmethanesulfonylhydrazone ( salmsmh) and 2-hydroxy-1-naphthaldehyde- N-methylmethanesulfonylhydrazone ( nafmsmh) were synthesized and characterized by using FT-IR, 1H NMR, 13C NMR, LC-MS and elemental analysis. Conformation analysis of msmh based on DFT/B3LYP/6-311G(d) method was performed. 1H and 13C shielding tensors of msmh for the most stable conformer were calculated with GIAO/DFT/B3LYP/6-311++G(2d, 2p) methods in vacuo and various solvents such as DMSO, THF, acetonitrile, methanol and aqueous solution. The harmonic vibrational wavenumbers for the most stable conformer were calculated using at B3LYP/6-311G(d) level. Antimicrobial activity of the compounds was also screened against Gram-positive bacteria ( Staphylococcus aureus ATCC 25923, Bacillus cereus RSKK 863) and Gram-negative bacteria ( Escherichia coli ATCC 11230, Salmonella enterititis ATCC 40376, Pseudomonos aeruginosa ATCC 28753) by both disc diffusion and micro dilution methods.

  16. Biting deterrence and insecticidal activity of hydrazide–hydrazones and their corresponding 3-acetyl-2,5-disubstituted-2,3-dihydro-1,3,4-oxadiazoles against Aedes aegypti

    Technology Transfer Automated Retrieval System (TEKTRAN)

    BACKGROUND: Hydrazones are important compounds for drug design and they have also good insecticidal activity. In this study, A series of hydrazide–hydrazones (1-10) and 3-acetyl-2,5-disubstituted-2,3-dihydro-1,3,4-oxadiazoles (11-20) were investigated for their biting deterrent and insecticidal act...

  17. Luminescent properties of a di-hydrazone derived from the antituberculosis agent isoniazid: Potentiality as an emitting layer constituent for OLED fabrication

    NASA Astrophysics Data System (ADS)

    Moraes, Rafaela S.; Aderne, Rian E.; Cremona, Marco; Rey, Nicolás A.

    2016-02-01

    Hydrazones constitute a class of compounds presenting azomethine R‧R″Nsbnd Ndbnd CHsbnd R hydrogens, which show diverse properties and a wide range of applications. A hydrazone derived from the antituberculosis drug isoniazid, namely, N,N‧-diisonicotinoyl-2-hydroxy-5-methylisophthalaldehyde hydrazone (DMD) was synthesized and chemically characterized. Its luminescent properties were also investigated, as well as the possibility of using this compound as a constituent of the emitting layer for the fabrication of OLEDs. Co-deposited devices were fabricated using the organic molecule BSBF as matrix and DMD as dopant. All the devices presented a broad electroluminescence band, in which it was possible to recognize the DMD emission along with emissions of some of the other organic layers. The best results were obtained with 35% DMD doping, achieving a luminance of about 35 cd/m2.

  18. Extending the Scope of the B(C6 F5 )3 -Catalyzed C=N Bond Reduction: Hydrogenation of Oxime Ethers and Hydrazones.

    PubMed

    Mohr, Jens; Porwal, Digvijay; Chatterjee, Indranil; Oestreich, Martin

    2015-12-01

    The B(C6 F5 )3 -catalyzed hydrogenation is applied to aldoxime triisopropylsilyl ethers and hydrazones bearing an easily removable phthaloyl protective group. The CN reduction of aldehyde-derived substrates (oxime ethers and hydrazones) is enabled by using 1,4-dioxane as the solvent known to participate as the Lewis-basic component in FLP-type heterolytic dihydrogen splitting. More basic ketone-derived hydrazones act as Lewis bases themselves in the FLP-type dihydrogen activation and are therefore successfully hydrogenated in nondonating toluene. The difference in reactivity between aldehyde- and ketone-derived substrates is also reflected in the required catalyst loading and dihydrogen pressure. PMID:26489785

  19. Relative predominance of azo and hydrazone tautomers of 4-carboxyl-2,6-dinitrophenylazohydroxynaphthalenes in binary solvent mixtures

    NASA Astrophysics Data System (ADS)

    Adegoke, Olajire A.

    2011-12-01

    Azo-hydrazone tautomerism is a phenomenon that occurs in azo dyes possessing substituents conjugated to the azo linkage which has labile proton that can be exchanged intramolecularly. Thus the predominance of one tautomer over another is a function of many factors among which are solvent polarity, solvent type, solute-solvent interactions and the structure of the dye molecule itself. The 4-carboxyl-2,6-dinitrophenylazohydroxynaphthalenes, previously shown to exhibit azo-hydrazone tautomerism, were studied for the relative predominance of one form over another based on interaction at the microenvironment of binary solvent mixtures containing DMF and non-hydrogen bonding (CCl 4), hydrogen bond donor (toluene, chloroform), hydrogen bond acceptor (acetonitrile, acetone) and the alcohols; ethanol and methanol as solvent pairs. The three dyes gave two main bands in the 50:50 mixture of DMF with these solvents consisting of a high energy band at 250-382 nm while the low energy bands for the dyes occurred at 415-485 nm. Spectral shifts in the binary solvent mixtures were related to the solvent dipolarity, basicity of the less polar component relative to DMF, substituent type, molar transition energy, formation constant for the hydrogen-bonding solvated complexes and the standard free energy change for hydrogen bonding with DMF. The relative predominance of the hydrazone tautomer bears a direct relationship to the basicity of the solvent, presence of hydrogen bond donor substituent and was associated with high molar transition energies and low formation constant. The microenvironment surrounding the dye molecules played a major role in the stability of one tautomer relative to the other.

  20. Identification of polymorphism in ethylone hydrochloride: synthesis and characterization.

    PubMed

    Maheux, Chad R; Alarcon, Idralyn Q; Copeland, Catherine R; Cameron, T Stanley; Linden, Anthony; Grossert, J Stuart

    2016-08-01

    Ethylone, a synthetic cathinone with psychoactive properties, is a designer drug which has appeared on the recreational drug market in recent years. Since 2012, illicit shipments of ethylone hydrochloride have been intercepted with increasing frequency at the Canadian border. Analysis has revealed that ethylone hydrochloride exists as two distinct polymorphs. In addition, several minor impurities were detected in some seized exhibits. In this study, the two conformational polymorphs of ethylone hydrochloride have been synthesized and fully characterized by FTIR, FT-Raman, powder XRD, GC-MS, ESI-MS/MS and NMR ((13) C CPMAS, (1) H, (13) C). The two polymorphs can be distinguished by vibrational spectroscopy, solid-state nuclear magnetic resonance spectroscopy and X-ray diffraction. The FTIR data are applied to the identification of both polymorphs of ethylone hydrochloride (mixed with methylone hydrochloride) in a laboratory submission labelled as 'Ocean Snow Ultra'. The data presented in this study will assist forensic scientists in the differentiation of the two ethylone hydrochloride polymorphs. This report, alongside our recent article on the single crystal X-ray structure of a second polymorph of this synthetic cathinone, is the first to confirm polymorphism in ethylone hydrochloride. © 2015 Canada Border Services Agency. Drug Testing and Analysis published by John Wiley & Sons, Ltd. © 2015 Canada Border Services Agency. Drug Testing and Analysis published by John Wiley & Sons, Ltd. PMID:26344849

  1. Radical Addition of Hydrazones by α-Bromo Ketones To Prepare 1,3,5-Trisubstituted Pyrazoles via Visible Light Catalysis.

    PubMed

    Fan, Xiu-Wei; Lei, Tao; Zhou, Chao; Meng, Qing-Yuan; Chen, Bin; Tung, Chen-Ho; Wu, Li-Zhu

    2016-08-19

    A novel efficient tandem reaction of hydrazones and α-bromo ketones is reported for the preparation of 1,3,5-trisubstituted pyrazoles by visible light catalysis. In this system, the monosubstituted hydrazones show wonderful reaction activity with alkyl radicals, generated from α-bromo ketones. A radical addition followed by intramolecular cyclization affords the important pyrazole skeleton in good to excellent yields. This efficient strategy under mild conditions with wide group tolerance provides a potential approach to the 1,3,5-trisubstituted pyrazoles. PMID:27362866

  2. Comparison of boron-assisted oxime and hydrazone formations leads to the discovery of a fluorogenic variant.

    PubMed

    Stress, Cedric J; Schmidt, Pascal J; Gillingham, Dennis G

    2016-06-28

    We use kinetic data, photophysical properties, and mechanistic analyses to compare recently developed high-rate constant oxime and hydrazone formations. We show that when Schiff base formation between aldehydes and arylhydrazines is carried out with an appropriately positioned boron atom, then aromatic B-N heterocycles form irreversibly. These consist of an extended aromatic structure amenable to the tailoring of specific properties such as reaction rate and fluorescence. The reactions work best in neutral aqueous buffer and can be designed to be fluorogenic - properties which are particularly interesting in bioconjugation. PMID:26876694

  3. Enantioselective Rhodium(I) Donor Carbenoid-Mediated Cascade Triggered by a Base-Free Decomposition of Arylsulfonyl Hydrazones.

    PubMed

    Torres, Òscar; Parella, Teodor; Solà, Miquel; Roglans, Anna; Pla-Quintana, Anna

    2015-11-01

    The reaction of diyne arylsulfonyl hydrazone substrates under rhodium(I)/BINAP catalysis gives access to sulfonated azacyclic frameworks in a highly enantioselective manner. This new cascade process considerably increases the molecular complexity by generating two C-C bonds, one C-S bond, and one C-H bond. Theoretical calculations, competitive experiments, and deuterium labeling have jointly been used to propose a mechanism that accounts for the reaction. The mechanism involves the formation of vinyl rhodium carbenoids, hydride migratory insertion, and intermolecular stereoselective nucleophilic attack. The last two steps are the key to the stereoselectivity of the process. PMID:26397988

  4. Synthesis, Biological Evaluation and Molecular Docking Study of Hydrazone-Containing Pyridinium Salts as Cholinesterase Inhibitors.

    PubMed

    Parlar, Sulunay; Bayraktar, Gulsah; Tarikogullari, Ayse Hande; Alptüzün, Vildan; Erciyas, Ercin

    2016-01-01

    A series of pyridinium salts bearing alkylphenyl groups at 1 position and hydrazone structure at 4 position of the pyridinium ring were synthesized and evaluated for the inhibition of both acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) enzymes. The cholinesterase (ChE) inhibitory activity studies were carried out by using the Ellman's colorimetric method. All compounds displayed considerable AChE and BuChE inhibitory activity and some of the compounds manifested remarkable anti-AChE activity compared to the reference compound, galantamine. Among the title compounds, the series including benzofuran aromatic ring exhibited the best inhibitory activity both on AChE and BuChE enzymes. Compound 3b, 4-[2-(1-(benzofuran-2-yl)ethylidene)hydrazinyl]-1-(3-phenylpropyl)pyridinium bromide, was the most active compound with IC50 value of 0.23 (0.24) µM against enantiomeric excess (ee)AChE (human (h)AChE) while compound 3a, 4-[2-(1-(benzofuran-2-yl)ethylidene)hydrazinyl]-1-phenethylpyridinium bromide, was the most active compound with IC50 value of 0.95 µM against BuChE. Moreover, 3a and b exhibited higher activity than the reference compound galantamine (eeAChE (hAChE) IC50 0.43 (0.52) µM; BuChE IC50 14.92 µM). Molecular docking studies were carried out on 3b having highest inhibitory activity against AChE. PMID:27581632

  5. Syntheses, crystal structure, Hirshfeld surfaces, fluorescence properties, and DFT analysis of benzoic acid hydrazone Schiff bases.

    PubMed

    Alam, Mohammad Sayed; Lee, Dong-Ung

    2015-06-15

    Two hydrazone Schiff base analogues, namely, (E)-N'-(4-hydroxy-3-methoxybenzylidene)benzohydrazide (3a) and (E)-N'-(4-methoxybenzylidene)benzohydrazide (3b), were synthesized using a mild, efficient method and characterized by (1)H NMR, mass spectrometry, elemental analysis, and single-crystal X-ray diffraction. X-ray analysis of a single crystal of 3a revealed a tetragonal, space group I4(1)/a structure, with an E-configuration around the azomethine (C8N2) double bond. In this structure, the NH and OH groups act as proton donors and the >CO and N groups as proton acceptors, and these facilitate hydrogen bond formation in the crystal state. Plausible intermolecular interactions were studied using 3D Hirshfeld surfaces and related 2D fingerprint plots. The optimized geometry, vibrational frequencies, Mulliken charge distribution, molecular electrostatic potential (MEP) maps, frontier molecular orbitals (FMOs), and associated energies of the ground state and the first single excited state were calculated using density functional theory (DFT) and time-dependant DFT calculations using the B3LYP/6-311G method. Vibrational frequencies calculated in the gaseous phase compared with experimental values measured in the solid state and showed good agreement with each other. The chemical reactivities of 3a and 3b were predicted by mapping MEP surface over optimized geometries and comparing these with MEP map generated over crystal structures. Mulliken charge distribution analysis and MEP map of 3a and 3b revealed that N(1), O(1), O(2) and O(3) atoms could act as electron donors and coordinate with metals and that these represented the most suitable sites for electrophilic attack. In fluorescence spectra, the absorption and emission spectra of 3a and 3b were similar in different polar solvents with few exceptions. In addition, both compounds exhibited dual emission spectra in acetone due to keto-enol tautomerism induced by photoexcitation. PMID:25804368

  6. Bivalent transition metal complexes of ONO donor hydrazone ligand: Synthesis, structural characterization and antimicrobial activity.

    PubMed

    Bhaskar, Ravindra; Salunkhe, Nilesh; Yaul, Amit; Aswar, Anand

    2015-12-01

    Mononuclear transition metal complexes of Mn(II), Co(II), Ni(II), Cu(II), Zn(II) and Cd(II) with a new hydrazone ligand derived from pyrazine-2-carbohydrazide and 2-hydroxyacetophenone have been synthesized. The isolated complexes were characterized by elemental analysis, spectral and analytical methods including elemental analyses, IR, diffuse reflectance, (1)H-NMR, mass spectra, molar conductance, magnetic moment, ESR, XRD, TG and SEM analysis. From the elemental analyses data, the stoichiometry of the complexes was found to be 1:1 (metal:ligand) having the general formulae [M(HL)(Cl)(H2O)2], [M=Mn(II), Co(II), Ni(II) and Cu(II)] and [M(L)(H2O)], [M=Zn(II) and Cd(II)]. The molar conductance values indicate the nonelectrolytic nature of metal complexes. The IR spectral data suggest that the ligand behaves as tridentate moiety with ONO donor atoms sequence towards central metal ion. The Mn(II), Co(II), Ni(II) and Cu(II) complexes have been assigned a monomeric octahedral geometry whereas tetrahedral to Zn(II) and Cd(II) complexes. The antibacterial and antifungal activities of the ligand and its metal complexes were studied against bacterial species Escherichia coli, Pseudomonas aeruginosa, Staphylococcus aureus, Bacillus subtilis, Enterococcus faecalis and Streptococcus pyogenes and fungi Candida albicans, Aspergillus niger and Aspergillus clavatus. The activity data show that the metal complexes have a promising biological activity comparable with the parent ligand against all bacterial and fungal species. PMID:26163785

  7. Syntheses, crystal structure, Hirshfeld surfaces, fluorescence properties, and DFT analysis of benzoic acid hydrazone Schiff bases

    NASA Astrophysics Data System (ADS)

    Alam, Mohammad Sayed; Lee, Dong-Ung

    2015-06-01

    Two hydrazone Schiff base analogues, namely, (E)-N‧-(4-hydroxy-3-methoxybenzylidene)benzohydrazide (3a) and (E)-N‧-(4-methoxybenzylidene)benzohydrazide (3b), were synthesized using a mild, efficient method and characterized by 1H NMR, mass spectrometry, elemental analysis, and single-crystal X-ray diffraction. X-ray analysis of a single crystal of 3a revealed a tetragonal, space group I4(1)/a structure, with an E-configuration around the azomethine (sbnd C8dbnd N2sbnd) double bond. In this structure, the sbnd NHsbnd and sbnd OH groups act as proton donors and the >Cdbnd O and sbnd Ndbnd groups as proton acceptors, and these facilitate hydrogen bond formation in the crystal state. Plausible intermolecular interactions were studied using 3D Hirshfeld surfaces and related 2D fingerprint plots. The optimized geometry, vibrational frequencies, Mulliken charge distribution, molecular electrostatic potential (MEP) maps, frontier molecular orbitals (FMOs), and associated energies of the ground state and the first single excited state were calculated using density functional theory (DFT) and time-dependant DFT calculations using the B3LYP/6-311G method. Vibrational frequencies calculated in the gaseous phase compared with experimental values measured in the solid state and showed good agreement with each other. The chemical reactivities of 3a and 3b were predicted by mapping MEP surface over optimized geometries and comparing these with MEP map generated over crystal structures. Mulliken charge distribution analysis and MEP map of 3a and 3b revealed that N(1), O(1), O(2) and O(3) atoms could act as electron donors and coordinate with metals and that these represented the most suitable sites for electrophilic attack. In fluorescence spectra, the absorption and emission spectra of 3a and 3b were similar in different polar solvents with few exceptions. In addition, both compounds exhibited dual emission spectra in acetone due to keto-enol tautomerism induced by

  8. Stability of admixture containing morphine sulfate, bupivacaine hydrochloride, and clonidine hydrochloride in an implantable infusion system.

    PubMed

    Classen, Ashley M; Wimbish, Gary H; Kupiec, Thomas C

    2004-12-01

    Intrathecal infusion is often performed using drug combinations. This study was conducted to evaluate the stability of the admixture of morphine sulfate, bupivacaine hydrochloride, and clonidine hydrochloride when used in an implantable pump under simulated clinical use conditions. SynchroMed implantable pumps were filled with an admixture and incubated at 37 degrees C for a period of 90 days. Drug admixture stored in glass vials at 4 degrees C and at 37 degrees C served as controls. Samples which included pump reservoir and catheter delivered aliquots were collected every 30 days and analyzed for drug concentrations using a stability-indicating HPLC method. All drugs contained in the admixture were stable and the original concentrations remained greater than 96%. Over 90 days, and with the pump at the simulated body temperature of 37 degrees C, there were no evident heat catalyzed or device catalyzed reactions. PMID:15589086

  9. Simultaneous determination of pseudoephedrine hydrochloride and diphenhydramine hydrochloride in cough syrup by gas chromatography (GC).

    PubMed

    Raj, S V; Kapadia, S U; Argekar, A P

    1998-05-01

    A simple, rapid and precise gas chromatographic method has been developed for the simultaneous determination of pseudoephedrine hydrochloride and diphenhydramine hydrochloride in cough syrup, using a SS column of 10% OV 1 on chromosorb W-HP (80-100 mesh) and nitrogen as a carrier gas at a flow rate of 30 ml min(-1). The oven temperature was programmed at 135 degrees C for 1 min, with a rise of 10 degrees C min(-1) up to 250 degrees C (held for 5 min). The injector and detector port temperatures were maintained at 280 degrees C. Detection was carried out using Flame ionization detector. Guaphenesin was used as an internal standard. Results of assay and recovery studies were statistically evaluated for its accuracy and precision. PMID:18967146

  10. Simultaneous UV Spectrophotometric Estimation of Ambroxol Hydrochloride and Levocetirizine Dihydrochloride.

    PubMed

    Prabhu, S Lakshmana; Shirwaikar, A A; Shirwaikar, Annie; Kumar, C Dinesh; Kumar, G Aravind

    2008-01-01

    A novel, simple, sensitive and rapid spectrophotometric method has been developed for simultaneous estimation of ambroxol hydrochloride and levocetirizine dihydrochloride. The method involved solving simultaneous equations based on measurement of absorbance at two wavelengths 242 nm and 231 nm, the gamma max of ambroxol hydrochloride and levocetirizine dihydrochloride, respectively. Beer's law was obeyed in the concentration range 10-50 mug/ml and 8-24 mug/ml for ambroxol hydrochloride and levocetirizine dihydrochloride respectively. Results of the method were validated statistically and by recovery studies. PMID:20046721

  11. Simultaneous UV Spectrophotometric Estimation of Ambroxol Hydrochloride and Levocetirizine Dihydrochloride

    PubMed Central

    Prabhu, S. Lakshmana; Shirwaikar, A. A.; Shirwaikar, Annie; Kumar, C. Dinesh; Kumar, G. Aravind

    2008-01-01

    A novel, simple, sensitive and rapid spectrophotometric method has been developed for simultaneous estimation of ambroxol hydrochloride and levocetirizine dihydrochloride. The method involved solving simultaneous equations based on measurement of absorbance at two wavelengths 242 nm and 231 nm, the γ max of ambroxol hydrochloride and levocetirizine dihydrochloride, respectively. Beer's law was obeyed in the concentration range 10–50 μg/ml and 8–24 μg/ml for ambroxol hydrochloride and levocetirizine dihydrochloride respectively. Results of the method were validated statistically and by recovery studies. PMID:20046721

  12. Effect of ractopamine hydrochloride and zilpaterol hydrochloride on cardiac electrophysiologic and hematologic variables in finishing steers.

    PubMed

    Frese, Daniel A; Reinhardt, Christopher D; Bartle, Steven J; Rethorst, David N; Bawa, Bhupinder; Thomason, Justin D; Loneragan, Guy H; Thomson, Daniel U

    2016-09-15

    OBJECTIVE To investigate the effects of dietary supplementation with the β-adrenoceptor agonists ractopamine hydrochloride and zilpaterol hydrochloride on ECG and clinicopathologic variables of finishing beef steers. DESIGN Randomized controlled trial. ANIMALS 30 Angus steers. PROCEDURES Steers were grouped by body weight and randomly assigned to receive 1 of 3 diets for 23 days: a diet containing no additive (control diet) or a diet containing ractopamine hydrochloride (300 mg/steer/d) or zilpaterol hydrochloride (8.3 mg/kg [3.8 mg/lb] of feed on a dry-matter basis), beginning on day 0. Steers were instrumented with an ambulatory ECG monitor on days -2, 6, 13, and 23, and continuous recordings were obtained for 72, 24, 24, and 96 hours, respectively. At the time of instrumentation, blood samples were obtained for CBC and serum biochemical and blood lactate analysis. Electrocardiographic recordings were evaluated for mean heart rate and arrhythmia rates. RESULTS Steers fed zilpaterol or ractopamine had greater mean heart rates than those fed the control diet. Mean heart rates were within reference limits for all steers, with the exception of those in the ractopamine group on day 14, in which mean heart rate was high. No differences in arrhythmia rates were identified among the groups, nor were any differences identified when arrhythmias were classified as single, paired, or multiple (> 2) beats. CONCLUSIONS AND CLINICAL RELEVANCE Results suggested that dietary supplementation of cattle with ractopamine or zilpaterol at FDA-approved doses had no effect on arrhythmia rates but caused an increase in heart rate that remained within reference limits. PMID:27585105

  13. Spectrophotometric methods for the simultaneous analysis of meclezine hydrochloride and pyridoxine hydrochloride in bulk drug and pharmaceutical formulations.

    PubMed

    Arayne, M Saeed; Sultana, Najma; Siddiqui, Farhan Ahmed; Zuberi, M Hashim; Mirza, Agha Zeeshan

    2007-04-01

    Three new spectrophotometric procedures for the simultaneous determination of pyridoxine hydrochloride and meclezine hydrochloride are described. The first method depends on the application of simultaneous equation to resolve the interference due to spectral overlapping. The analytical signals were measured at 231 and 220 nm. Calibration graphs were established for 1 to 20 microGmL(-1) for pyridoxine hydrochloride and 0.5 to 10 microGmL(-1) for meclezine hydrochloride in binary mixture. In the second method, the determination of pyridoxine hydrochloride and meclezine hydrochloride was performed by measuring the absorbances at 290 and 235 nm in the simple absorbance spectra of their mixture. In third method a yellowish orange complex of pyridoxine hydrochloride was formed with ferric chloride, which absorbs in the visible region with lambda(max) at 445 nm. Calibration curve of complex formation range was conducted in between 20 to 250 microGmL(-1). These methods were validated with respect to accuracy, precision, linearity, limit of detection and quantification. Regression analysis of Beer's plot showed good correlation in a general concentration range of 1 to 20 microGml(-1) with correlation coefficient (r = 0.9999 and 0.9999; CV < 0.858) for pyridoxine hydrochloride, whereas meclezine hydrochloride concentration range 0.5 to 10 microGmL(-1) with correlation coefficient (r = 0.9998 and 0.9998; CV < 0.826). These methods can be readily applied, without any interference from the excipients. The suggested procedures were successfully applied to the determination of these compounds in synthetic mixtures and in pharmaceutical preparations, with high percentage of recovery, good accuracy and precision. PMID:17416572

  14. Submicron Organic Matter in a Peri-alpine, Ultra-oligotrphic Lake

    SciTech Connect

    Chanudet,V.; Filella, M.

    2007-01-01

    Combining organic carbon (OC) measurements with the classic MBTH (3-methyl-2-benzothiazolinone hydrochloride) method for carbohydrate determination and a new voltammetric method for the determination of refractory organic matter (ROM) made it possible, for the first time, to quantify the types, sources and fate of submicron organic matter present in an ultra-oligotrophic lake (Lake Brienz, Switzerland). The lake is extremely rich in suspended glacial flour in summer (glacier melting season). Measurements were taken from June 2004 to October 2005 from 1.2 {mu}m filtered samples. OC concentration remained extremely low throughout the year (below 1 mg C L{sup -1}). MBTH carbohydrate concentration was very low in the lake (0.06-0.43 mg C L{sup -1}) and in the two tributary rivers (0.06-0.25 mg C L{sup -1}). Lake carbohydrate concentration only correlated with phytoplanktonic biomass at the onset of the productivity period. The results suggest that differences in MBTH concentration may sometimes reflect differences in the nature of the carbohydrates rather than differences in carbon concentration. Extensive fibril formation was evidenced by transmission electron microscopy (TEM) observations. ROM concentration in the lake was also very low (0.1-0.2 mg C L{sup -1}). Significant variation in ROM riverine input was due to either annual occurrences (snow melting) or irregular episodes (floods). Melting snow was responsible for about 30% of the lake's annual ROM input. One box mass balance calculations showed that about 25% of ROM was lost within the lake. Evidence gleaned from TEM and STXM (scanning transmission X-ray microscopy) observations clearly indicates that this is mainly caused by ROM sedimentation after association with inorganic colloids.

  15. Stability of Revex, nalmefene hydrochloride injection.

    PubMed

    Brittain, H G; Lafferty, L; Bousserski, P; Diegnan, G; Lessor, R; Small, C; Pejaver, S

    1996-01-01

    The stability of Revex, nalmefene hydrochloride injection, has been studied at several temperatures for periods up to 36 months. The data were obtained using a HPLC method for the potency determination, and for the level of the sole degradation product (2,2'-bisnalmefene). These methods were found to be characterized by excellent precision, linearity, and accuracy over the analyte concentration ranges established. The stability data were found to be interpretable using first-order kinetics, and essentially comparable rate constants were calculated for both the potency loss and the formation of 2,2'-bisnalmefene. Applying the Arrhenius equation to these data, a rate constant of 0.00441 month-1 was deduced for the reactions taking place at 25 degrees C. This low value is consistent with the excellent stability exhibited by the product, and amply justifies its shelf life. PMID:8846056

  16. A novel and practical asymmetric synthesis of dapoxetine hydrochloride.

    PubMed

    Zhu, Yijun; Liu, Zhenren; Li, Hongyan; Ye, Deyong; Zhou, Weicheng

    2015-01-01

    A novel and practical asymmetric synthesis of dapoxetine hydrochloride by using the chiral auxiliary (S)-tert-butanesulfinamide was explored. The synthesis was concise, mild, and easy to perform. The overall yield and stereoselectivity were excellent. PMID:26734109

  17. 21 CFR 522.1642 - Oxymorphone hydrochloride injection.

    Code of Federal Regulations, 2011 CFR

    2011-04-01

    ... milligrams of oxymorphone hydrochloride per milliliter of aqueous solution containing 0.8 percent sodium chloride. (b) Sponsor. See No. 060951 in § 510.600(c) of this chapter. (c) Conditions of use. (1) The...

  18. 21 CFR 522.1642 - Oxymorphone hydrochloride injection.

    Code of Federal Regulations, 2012 CFR

    2012-04-01

    ... milligrams of oxymorphone hydrochloride per milliliter of aqueous solution containing 0.8 percent sodium chloride. (b) Sponsor. See No. 060951 in § 510.600(c) of this chapter. (c) Conditions of use. (1) The...

  19. 21 CFR 522.1642 - Oxymorphone hydrochloride injection.

    Code of Federal Regulations, 2010 CFR

    2010-04-01

    ... milligrams of oxymorphone hydrochloride per milliliter of aqueous solution containing 0.8 percent sodium chloride. (b) Sponsor. See No. 060951 in § 510.600(c) of this chapter. (c) Conditions of use. (1) The...

  20. A novel and practical asymmetric synthesis of dapoxetine hydrochloride

    PubMed Central

    Zhu, Yijun; Liu, Zhenren; Li, Hongyan

    2015-01-01

    Summary A novel and practical asymmetric synthesis of dapoxetine hydrochloride by using the chiral auxiliary (S)-tert-butanesulfinamide was explored. The synthesis was concise, mild, and easy to perform. The overall yield and stereoselectivity were excellent. PMID:26734109

  1. 21 CFR 522.1335 - Medetomidine hydrochloride injection.

    Code of Federal Regulations, 2012 CFR

    2012-04-01

    ... solution contains 1.0 milligram of medetomidine hydrochloride. (b) Sponsor. See 052483 in § 510.600(c) of... diseases, dogs in shock, dogs which are severly debilitated, or dogs which are stressed due to extreme...

  2. 21 CFR 520.1242e - Levamisole hydrochloride effervescent tablets.

    Code of Federal Regulations, 2014 CFR

    2014-04-01

    ...: (1) Amount. The equivalent of 8 milligrams of levamisole hydrochloride per kilogram of body weight... thoroughly. Allow 1 gallon of medicated water for each 100 pounds body weight of pigs to be treated. No...

  3. Synthesis, Biological Evaluation and 2D-QSAR Study of Halophenyl Bis-Hydrazones as Antimicrobial and Antitubercular Agents

    PubMed Central

    Abdel-Aziz, Hatem A.; Eldehna, Wagdy M.; Fares, Mohamed; Al-Rashood, Sara T. A.; Al-Rashood, Khalid A.; Abdel-Aziz, Marwa M.; Soliman, Dalia H.

    2015-01-01

    In continuation of our endeavor towards the development of potent and effective antimicrobial agents, three series of halophenyl bis-hydrazones (14a–n, 16a–d, 17a and 17b) were synthesized and evaluated for their potential antibacterial, antifungal and antimycobacterial activities. These efforts led to the identification of five molecules 14c, 14g, 16b, 17a and 17b (MIC range from 0.12 to 7.81 μg/mL) with broad antimicrobial activity against Mycobacterium tuberculosis; Aspergillus fumigates; Gram positive bacteria, Staphylococcus aureus, Streptococcus pneumonia, and Bacillis subtilis; and Gram negative bacteria, Salmonella typhimurium, Klebsiella pneumonia, and Escherichia coli. Three of the most active compounds, 16b, 17a and 17b, were also devoid of apparent cytotoxicity to lung cancer cell line A549. Amphotericin B and ciprofloxacin were used as references for antifungal and antibacterial screening, while isoniazid and pyrazinamide were used as references for antimycobacterial activity. Furthermore, three Quantitative Structure Activity Relationship (QSAR) models were built to explore the structural requirements controlling the different activities of the prepared bis-hydrazones. PMID:25903147

  4. Structural, spectroscopic and quantum chemical studies of acetyl hydrazone oxime and its palladium(II) and platinum(II) complexes

    NASA Astrophysics Data System (ADS)

    Kaya, Yunus; Icsel, Ceyda; Yilmaz, Veysel T.; Buyukgungor, Orhan

    2015-09-01

    Acetyl hydrazone oxime, [(1E,2E)-2-(hydroxyimino)-1-phenylethylidene]acetohydrazone (hipeahH2) and its palladium(II) and platinum(II) complexes, [M(hipeahH)2] (M = PdII and PtII), have been synthesized and characterized by elemental analysis, UV-vis IR, NMR and LC-MS techniques. X-ray diffraction analysis of [Pd(hipeahH)2] shows that the two hipeahH2 ligands are not equal; one of the ligands loses the hydrazone proton, while the other one loses the oxime proton, resulting in a different coordination behavior to form five- and six-membered chelate rings. The molecular geometries from X-ray experiments in the ground state were compared using the density functional theory (DFT) with the B3LYP method combined with the 6-311++G(d,p) basis set for the ligand and the LanL2DZ basis set for the complexes. Comprehensive theoretical and experimental structural studies on the molecule have been carried out by FT-IR, NMR and UV-vis spectrometry. In addition, the isomer studies of ligand and its complexes were made by DFT.

  5. Synthesis and Antimicrobial Evaluation of Some Novel Thiazole, Pyridone, Pyrazole, Chromene, Hydrazone Derivatives Bearing a Biologically Active Sulfonamide Moiety

    PubMed Central

    Darwish, Elham S.; Abdel Fattah, Azza M.; Attaby, Fawzy A.; Al-Shayea, Oqba N.

    2014-01-01

    This study aimed for the synthesis of new heterocyclic compounds incorporating sulfamoyl moiety suitable for use as antimicrobial agents via a versatile, readily accessible N-[4-(aminosulfonyl)phenyl]-2-cyanoacetamide (3). The 2-pyridone derivatives were obtained via reaction of cyanoacetamide with acetylacetone or arylidenes malononitrile. Cycloaddition reaction of cyanoacetamide with salicyaldehyde furnished chromene derivatives. Diazotization of 3 with the desired diazonium chloride gave the hydrazone derivatives 13a–e. Also, the reactivity of the hydrazone towards hydrazine hydrate to give Pyrazole derivatives was studied. In addition, treatment of 3 with elemental sulfur and phenyl isothiocyanate or malononitrile furnished thiazole and thiophene derivatives respectively. Reaction of 3 with phenyl isothiocyanate and KOH in DMF afforded the intermediate salt 17 which reacted in situ with 3-(2-bromoacetyl)-2H-chromen-2-one and methyl iodide afforded the thiazole and ketene N,S-acetal derivatives respectively. Finally, reaction of 3 with carbon disulfide and 1,3-dibromopropane afforded the N-[4-(aminosulfonyl) phenyl]-2-cyano-2-(1,3-dithian-2-ylidene)acetamide product 22. All newly synthesized compounds were elucidated by considering the data of both elemental and spectral analysis. The compounds were evaluated for both their in vitro antibacterial and antifungal activities and showed promising results. PMID:24445259

  6. Potential amoebicidal activity of hydrazone derivatives: synthesis, characterization, electrochemical behavior, theoretical study and evaluation of the biological activity.

    PubMed

    Toledano-Magaña, Yanis; García-Ramos, Juan Carlos; Navarro-Olivarria, Marisol; Flores-Alamo, Marcos; Manzanera-Estrada, Mayra; Ortiz-Frade, Luis; Galindo-Murillo, Rodrigo; Ruiz-Azuara, Lena; Meléndrez-Luevano, Ruth Ma; Cabrera-Vivas, Blanca M

    2015-01-01

    Four new hydrazones were synthesized by the condensation of the selected hydrazine and the appropriate nitrobenzaldehyde. A complete characterization was done employing 1H- and 13C-NMR, electrochemical techniques and theoretical studies. After the characterization and electrochemical analysis of each compound, amoebicidal activity was tested in vitro against the HM1:IMSS strain of Entamoeba histolytica. The results showed the influence of the nitrobenzene group and the hydrazone linkage on the amoebicidal activity. meta-Nitro substituted compound 2 presents a promising amoebicidal activity with an IC50 = 0.84 μM, which represents a 7-fold increase in cell growth inhibition potency with respect to metronidazole (IC50 = 6.3 μM). Compounds 1, 3, and 4 show decreased amoebicidal activity, with IC50 values of 7, 75 and 23 µM, respectively, as a function of the nitro group position on the aromatic ring. The observed differences in the biological activity could be explained not only by the redox potential of the molecules, but also by their capacity to participate in the formation of intra- and intermolecular hydrogen bonds. Redox potentials as well as the amoebicidal activity can be described with parameters obtained from the DFT analysis. PMID:26035095

  7. Comparative studies, synthesis, spectroscopic and characterization of N-methylisatin-3-Girard's T and P hydrazone complexes

    NASA Astrophysics Data System (ADS)

    Azhari, Shaker J.; Salah, Sabah; Farag, Rabei S.; Mostafa, Mohsen M.

    2015-02-01

    Different types of complexes derived from the reactions of N-methylisatin Girard's T hydrazone, N,N,N-trimethyl-2-[(2z)-2-(1-methyl-2-oxo-1,2-dihydro-3H-indole-3-ylidene) hydrazino]-2-oxo-ethan ammonium chloride (MIGT) and N-methylisatin Girard's P hydrazone, 1-{2-(2z)-2-[(1-methyl-2-oxo-1,2-dihydro-3H-indole-3-ylidene) hydrazino]-2-oxoethyl}pyridinium chloride (MIGP) with Fe3+, Al3+, Sb3+ and Sn2+ salts were synthesized. The isolated complexes were characterized by elemental analyses, molar conductivities, spectral (IR, UV-Vis., 1H NMR, mass), magnetic moments and thermal measurements. The values of conductance suggest that the complexes are conducting in polar solvents (EtOH, H2O and DMF). The IR spectra suggest that the ligands coordinate in a bidentate and/or tridentate manner via the carbonyl groups of both N-methylisatin and Girard's T and/or P and the (Cdbnd N) group. The solvents inside and outside the coordination sphere were determined by weight loss and TGA methods. The octahedral geometry of the complexes is confirmed using spectral, magnetic and DFT method from DMOL3 calculations. The ligands and their metal complexes were tested against different strains of bacteria and fungi.

  8. Pharmacological Evaluation and Preparation of Nonsteroidal Anti-Inflammatory Drugs Containing an N-Acyl Hydrazone Subunit

    PubMed Central

    de Melo, Thais Regina Ferreira; Chelucci, Rafael Consolin; Pires, Maria Elisa Lopes; Dutra, Luiz Antonio; Barbieri, Karina Pereira; Bosquesi, Priscila Longhin; Trossini, Gustavo Henrique Goulart; Chung, Man Chin; dos Santos, Jean Leandro

    2014-01-01

    A series of anti-inflammatory derivatives containing an N-acyl hydrazone subunit (4a–e) were synthesized and characterized. Docking studies were performed that suggest that compounds 4a–e bind to cyclooxygenase (COX)-1 and COX-2 isoforms, but with higher affinity for COX-2. The compounds display similar anti-inflammatory activities in vivo, although compound 4c is the most effective compound for inhibiting rat paw edema, with a reduction in the extent of inflammation of 35.9% and 52.8% at 2 and 4 h, respectively. The anti-inflammatory activity of N-acyl hydrazone derivatives was inferior to their respective parent drugs, except for compound 4c after 5 h. Ulcerogenic studies revealed that compounds 4a–e are less gastrotoxic than the respective parent drug. Compounds 4b–e demonstrated mucosal damage comparable to celecoxib. The in vivo analgesic activities of the compounds are higher than the respective parent drug for compounds 4a–b and 4d–e. Compound 4a was more active than dipyrone in reducing acetic-acid-induced abdominal constrictions. Our results indicate that compounds 4a–e are anti-inflammatory and analgesic compounds with reduced gastrotoxicity compared to their respective parent non-steroidal anti-inflammatory drugs. PMID:24714090

  9. Comparative studies, synthesis, spectroscopic and characterization of N-methylisatin-3-Girard's T and P hydrazone complexes.

    PubMed

    Azhari, Shaker J; Salah, Sabah; Farag, Rabei S; Mostafa, Mohsen M

    2014-11-01

    Different types of complexes derived from the reactions of N-methylisatin Girard's T hydrazone, N,N,N-trimethyl-2-[(2z)-2-(1-methyl-2-oxo-1,2-dihydro-3H-indole-3-ylidene) hydrazino]-2-oxo-ethan ammonium chloride (MIGT) and N-methylisatin Girard's P hydrazone, 1-{2-(2z)-2-[(1-methyl-2-oxo-1,2-dihydro-3H-indole-3-ylidene) hydrazino]-2-oxoethyl}pyridinium chloride (MIGP) with Fe(3+), Al(3+), Sb(3+) and Sn(2+) salts were synthesized. The isolated complexes were characterized by elemental analyses, molar conductivities, spectral (IR, UV-Vis., (1)H NMR, mass), magnetic moments and thermal measurements. The values of conductance suggest that the complexes are conducting in polar solvents (EtOH, H2O and DMF). The IR spectra suggest that the ligands coordinate in a bidentate and/or tridentate manner via the carbonyl groups of both N-methylisatin and Girard's T and/or P and the (CN) group. The solvents inside and outside the coordination sphere were determined by weight loss and TGA methods. The octahedral geometry of the complexes is confirmed using spectral, magnetic and DFT method from DMOL(3) calculations. The ligands and their metal complexes were tested against different strains of bacteria and fungi. PMID:25467685

  10. Highly efficient donor-acceptor hydrazone dyes-inorganic Si/TiO2 hybrid solar cells

    NASA Astrophysics Data System (ADS)

    Al-Sehemi, Abdullah G.; Irfan, Ahmad; Al-Melfi, Mohrah Abdullah M.

    2015-06-01

    We have synthesized the two donor-bridge-acceptor organic dyes (hydrazone dye 1 (HD1) and hydrazone dye 2 (HD2)) with the aim to enhance intra-molecular charge transfer then characterized by FTIR and NMR. The ground state geometries have been optimized at three different levels of theories, i.e., B3LYP/6-31G∗, B3LYP/6-31G∗∗ and Hartee-Fock HF/6-31G∗∗. The absorption spectra and oscillator strengths in different solvents have been computed and compared with the experimental data. The vibrational spectral assignments have been performed on the recorded FTIR spectra based on the theoretical predicted wavenumbers at three different levels of theories. The effect of different solvents (CHCl3, CH3CN and C2H5OH) has been studied on the absorption wavelengths. Furthermore, we have computed the ionization potentials, electron affinities and reorganization energies of studied compounds and shed light on the charge transport properties. The hetero-junction solar cell devices were fabricated by organic-inorganic hetero-junction (Si/TiO2/dye) then the efficiency has been measured by applying the incident power 30, 50 and 70 mW/cm2. The maximum efficiency 3.12% has been observed for HD1.

  11. Synthesis and biological activity of hydrazide hydrazones and their corresponding 3-acetyl-2,5-disubstituted-2,3-dihydro-1,3,4-oxadiazoles

    Technology Transfer Automated Retrieval System (TEKTRAN)

    Various new 3-acetyl-2,5-disubstituted-2,3-dihydro-1,3,4-oxadiazoles (11-20) were prepared by the reaction of aryl substituted hydrazones of 4-fluorobenzoic acid hydrazide (1-10) with acetic anhydride. The structures of the newly synthesized compounds 11-20, were confirmed by UV, IR and 1H NMR spec...

  12. CATALYST-FREE REACTIONS UNDER SOLVENT-FEE CONDITIONS: MICROWAVE-ASSISTED SYNTHESIS OF HETEROCYCLIC HYDRAZONES BELOW THE MELTING POINT OF NEAT REACTANTS: JOURNAL ARTICLE

    EPA Science Inventory

    NRMRL-CIN-1437 Jeselnik, M., Varma*, R.S., Polanc, S., and Kocevar, M. Catalyst-free Reactions under Solvent-fee Conditions: Microwave-assisted Synthesis of Heterocyclic Hydrazones below the Melting Point of Neat Reactants. Published in: Chemical Communications 18:1716-1717 (200...

  13. An Efficient Protocol for the Oxidative Hydrolysis of Ketone SAMP Hydrazones Employing SeO(2) and H(2)O(2) under Buffered (pH 7) Conditions.

    PubMed

    Smith, Amos B; Liu, Zhuqing; Simov, Vladimir

    2009-06-01

    An effective oxidative protocol for the liberation of ketones from SAMP hydrazones employing peroxyselenous acid under aqueous buffered conditions (pH 7) has been developed. The procedure proceeds without epimerization of adjacent stereocenters or dehydration, respectively, in representative SAMP alkylation and aldol reaction adducts. PMID:20657727

  14. Catalyst-free reactions under solvent-free conditions: microwave-assisted synthesis of heterocyclic hydrazones below the melting points of neat reactants.

    PubMed

    Jeselnik, M; Varma, R S; Polanc, S; Kocevar, M

    2001-09-21

    The reaction of neat 5- or 8-oxobenzopyran-2(1H)-ones, 1-3, with a variety of aromatic and heteroaromatic hydrazines, 4, is remarkably accelerated upon irradiation in a household microwave oven in the absence of any catalyst, solid support or solvent thus providing an environmentally friendly route to several heterocyclic hydrazones. PMID:12240280

  15. A Post Hoc Analysis of D-Threo-Methylphenidate Hydrochloride (Focalin) Versus D,l-Threo-Methylphenidate Hydrochloride (Ritalin)

    ERIC Educational Resources Information Center

    Weiss, Margaret; Wasdell, Michael; Patin, John

    2004-01-01

    Objective: To evaluate clinical measures of the benefit/risk ratio in a post hoc analysis of a clinical trial of d-threo-methylphenidate hydrochloride (d-MPH) and d,l-threo-methylphenidate hydrochloride (d,l-MPH). Method: Data from a phase III clinical trial was used to compare equimolar doses of d-MPH and d,l-MPH treatment for…

  16. Synthesis, leishmanicidal, trypanocidal and cytotoxic activity of quinoline-hydrazone hybrids.

    PubMed

    Coa, Juan Carlos; Castrillón, Wilson; Cardona, Wilson; Carda, Miguel; Ospina, Victoria; Muñoz, July Andrea; Vélez, Iván D; Robledo, Sara M

    2015-08-28

    Cutaneous leishmaniasis and Chagas disease are vector-borne parasitic disease causing serious risks to million people living in poverty-stricken areas. Both diseases are a major health problem in Latin America, and currently drugs for the effective treatment of these diseases have important concerns related with efficacy or toxicity than need to be addressed. We report herein the synthesis and biological activities (cytotoxicity, leishmanicidal and trypanocidal activities) of ten quinolone-hydrazone hybrids. The structure of the products was elucidated by spectrometric analyses. The synthesized compounds were evaluated against amastigotes forms of L. (V) panamensis which is the most prevalent Leishmania species in Colombia and Trypanosoma cruzi that is the major pathogenic species to humans; in turn, cytotoxicity was evaluated against human U-937 macrophages. Compounds 6b, 6c and 8 showed activity against L. (V) panamensis with EC50 of 6.5 ± 0.8 μg/mL (21.2 μM), 0.8 ± 0.0 μg/mL (2.6 μM) and 3.4 ± 0.6 μg/mL (11.1 μM), respectively, while compounds 6a and 6c had activity against T. cruzi. with EC50 values of 1.4 ± 0.3 μg/mL (4.8 μM) and 6.6 ± 0.3 μg/mL (4.6 μM), respectively. Even compound 6a showed better activity against T. cruzi than the standard drug benznidazole with EC50 = 10.5 ± 1.8 μg/mL (40.3 μM). Analysis of the results obtained against leishmaniasis indicates that antiparasite activity is related to the presence of 2-substituted quinoline (isoquinolinic core) and the hydroxyl group in positions 3 and 4 of the aromatic ring. Although the majority of these compounds were highly cytotoxic, the antiparasite activity was higher than cytotoxicity and therefore, they still have potential to be considered as hit molecules for leishmanicidal and trypanocidal drug development. PMID:26218652

  17. 77 FR 20987 - Oral Dosage Form New Animal Drugs; Change of Sponsor; Lincomycin Hydrochloride Soluble Powder...

    Federal Register 2010, 2011, 2012, 2013, 2014

    2012-04-09

    ... Sponsor; Lincomycin Hydrochloride Soluble Powder; Penicillin G Potassium in Drinking Water; Tetracycline Powder AGENCY: Food and Drug Administration, HHS. ACTION: Final rule; technical amendment. SUMMARY: The...; penicillin G potassium, USP; and tetracycline hydrochloride soluble powders administered in drinking...

  18. Stability of cefozopran hydrochloride in aqueous solutions.

    PubMed

    Zalewski, Przemysław; Skibiński, Robert; Paczkowska, Magdalena; Garbacki, Piotr; Talaczyńska, Alicja; Cielecka-Piontek, Judyta; Jelińska, Anna

    2016-01-01

    The influence of pH on the stability of cefozopran hydrochloride (CZH) was investigated in the pH range of 0.44-13.00. Six degradation products were identified with a hybrid ESI-Q-TOF mass spectrometer. The degradation of CZH as a result of hydrolysis was a pseudo-first-order reaction. As general acid-base hydrolysis of CZH was not occurred in the solutions of hydrochloric acid, sodium hydroxide, acetate, borate and phosphate buffers, kobs = kpH because specific acid-base catalysis was observed. Specific acid-base catalysis of CZH consisted of the following reactions: hydrolysis of CZH catalyzed by hydrogen ions (kH+), hydrolysis of dications (k1H2O), monocations (k2H2O) and zwitter ions (k3H2O) and hydrolysis of zwitter ions (k1OH-) and monoanions (k2OH-) of CZH catalyzed by hydroxide ions. The total rate of the reaction was equal to the sum of partial reactions: [Formula: see text]. CZH similarly like other fourth generation cephalosporin was most stable at slightly acidic and neutral pH and less stable in alkaline pH. The cleavage of the β-lactam ring resulting from a nucleophilic attack on the carbonyl carbon in the β-lactam moiety is the preferred degradation pathway of β-lactam antibiotics in aqueous solutions. PMID:26079426

  19. Nalbuphine hydrochloride dependence in anabolic steroid users.

    PubMed

    Wines, J D; Gruber, A J; Pope, H G; Lukas, S E

    1999-01-01

    Nalbuphine hydrochloride, a nonscheduled opioid agonist/antagonist analgesic, is currently approved for the treatment of pain. Recently, nalbuphine dependence was reported in three anabolic steroid users in Britain. To further document this phenomenon, we conducted interviews on eleven subjects who reported nalbuphine use. Eight subjects were clinically dependent on nalbuphine, and seven of the subjects who were asked about tolerance and withdrawal with nalbuphine acknowledged these symptoms. Eight subjects, who had never used drugs intravenously before, reported using nalbuphine by this route. Nalbuphine-related morbidity was extensive and included medical complications and psychiatric symptoms. Nalbuphine users also exhibited a high rate of comorbid Axis I disorders, including other substance misuse. Virtually all subjects described widespread nalbuphine use in the gymnasiums they frequented. These observations, together with the recent increase in nalbuphine-related articles in the lay press, suggest that nalbuphine may represent a new drug of abuse among athletes, especially those using anabolic steroids, and that nalbuphine's scheduling status may need to be re-evaluated. PMID:10365196

  20. Sapropterin Hydrochloride: Enzyme Enhancement Therapy for Phenylketonuria

    PubMed Central

    Lachmann, Robin

    2011-01-01

    Phenylketonuria (PKU) is an inherited disorder of amino acid metabolism caused by deficiency of the enzyme phenylalanine hydroxylase (PAH). Historically PKU was a common genetic cause of severe learning difficulties and developmental delay, but with the introduction of newborn screening and early dietary management, it has become a treatable disease and people born with PKU should now have IQs and achievements similar to their peers. Dietary treatment, however, involves lifestyle changes that pervade most aspects of daily life for an individual and their family. A simple pharmacological treatment for PKU would have a great appeal. Sapropterin hydrochloride is a synthetic form of tetrahydrobiopterin, the cofactor for PAH. A proportion of mutant PAH enzymes show enhanced activity in the presence of pharmacological doses of sapropterin and, for some patients with milder forms of PKU, sapropterin can effectively lower plasma phenylalanine levels. This article discusses the potential place for sapropterin in the management of PKU and how this expensive orphan drug is being integrated into patient care in different healthcare systems. PMID:23148178

  1. Immobilizing wild mountain lions (Felis concolor) with ketamine hydrochloride and xylazine hydrochloride.

    PubMed

    Logan, K A; Thorne, E T; Irwin, L L; Skinner, R

    1986-01-01

    A mixture of 120 mg ketamine hydrochloride (KHCL)/20 mg xylazine hydrochloride (XHCL)/ml was used to immobilize 37 wild mountain lions (Felis concolor) 46 times. Observations were recorded during 37 trials that included kittens, adult females, and adult males. Dosages were based on 11 mg KHCL and 1.8 mg XHCL/kg estimated body weight. Actual doses for 24 lions requiring a single injection for immobilization ranged from 4.7-15.8 mg KHCL/kg and 0.8-2.6 mg XHCL/kg. Induction, duration, and recovery times did not differ (P greater than 0.05) between the sex and age classes. Two kittens were overdosed with the drug combination, but the effects were not life threatening. Eleven other lions, nine of which were initially underdosed, required additional injections of the drug combination for safe handling. Immobilization was characterized initially by semi-consciousness, open eyelids, pupillary dilation, and muscle rigidity. Later, most lions appeared unconscious, muscles relaxed, and breathing slowed considerably. No convulsions or hypersalivation occurred. The KHCL/XHCL mixture given at approximately 11 mg KHCL and 1.8 mg XHCL/kg body weight proved useful for immobilizing wild mountain lions for research purposes. Suggestions for case of immobilized cats are included. PMID:3951066

  2. Synthesis of novel hydrazone and azole functionalized pyrazolo[3,4-b]pyridine derivatives as promising anticancer agents.

    PubMed

    Nagender, P; Naresh Kumar, R; Malla Reddy, G; Krishna Swaroop, D; Poornachandra, Y; Ganesh Kumar, C; Narsaiah, B

    2016-09-15

    A series of novel pyrazolo[3,4-b]pyridine based target compounds were synthesized starting from the key intermediate ethyl 2-(3-amino-6-(trifluoromethyl)-1H-pyrazolo[3,4-b]pyridin-1-yl)acetate 5 on reaction with hydrazine hydrate followed by reaction with different aldehydes, acid chlorides and isothiocyanates to form hydrazones 7, oxadiazoles 8, 1,2,4 triazoles 10 and thiadiazoles 11 respectively in high yield. All the final compounds were screened for anticancer activity against four human cancer cell lines. Among them, 1,2,4 triazole derivatives showed promising activity and compound 10d is identified as a lead molecule. PMID:27528432

  3. Structure-activity studies in the development of a hydrazone based inhibitor of adipose-triglyceride lipase (ATGL).

    PubMed

    Mayer, Nicole; Schweiger, Martina; Melcher, Michaela-Christina; Fledelius, Christian; Zechner, Rudolf; Zimmermann, Robert; Breinbauer, Rolf

    2015-06-15

    Adipose triglyceride lipase (ATGL) catalyzes the degradation of cellular triacylglycerol stores and strongly determines the concentration of circulating fatty acids (FAs). High serum FA levels are causally linked to the development of insulin resistance and impaired glucose tolerance, which eventually progresses to overt type 2 diabetes. ATGL-specific inhibitors could be used to lower circulating FAs, which can counteract the development of insulin resistance. In this article, we report about structure-activity relationship (SAR) studies of small molecule inhibitors of ATGL based on a hydrazone chemotype. The SAR indicated that the binding pocket of ATGL requests rather linear compounds without bulky substituents. The best inhibitor showed an IC50=10μM in an assay with COS7-cell lysate overexpressing murine ATGL. PMID:25778769

  4. New series of aromatic/ five-membered heteroaromatic butanesulfonyl hydrazones as potent biological agents: Synthesis, physicochemical and electronic properties

    NASA Astrophysics Data System (ADS)

    Hamurcu, Fatma; Mamaş, Serhat; Ozdemir, Ummuhan Ozmen; Gündüzalp, Ayla Balaban; Senturk, Ozan Sanlı

    2016-08-01

    The aromatic/five-membered heteroaromatic butanesulfonylhydrazone derivatives; 5-bromosalicylaldehydebutanesulfonylhydrazone(1), 2-hydroxy-1-naphthaldehydebutane sulfonylhydrazone(2), indole-3-carboxaldehydebutanesulfonylhydrazone (3), 2-acetylfuran- carboxyaldehydebutanesulfonylhydrazone(4), 2-acetylthiophenecarboxyaldehydebutane- sulfonylhydrazone(5) and 2-acetyl-5-chlorothiophenecarboxyaldehydebutanesulfonyl hydrazone (6) were synthesized by the reaction of butane sulfonic acid hydrazide with aldehydes/ketones and characterized by using elemental analysis, 1H NMR, 13C NMR and FT-IR technique. Their geometric parameters and electronic properties consist of global reactivity descriptors were also determined by theoretical methods. The electrochemical behavior of the butanesulfonylhydrazones were investigated by using cyclic voltammetry (CV), controlled potential electrolysis and chronoamperometry (CA) techniques. The number of electrons transferred (n), diffusion coefficient (D) and standard heterogeneous rate constants (ks) were determined by electrochemical methods.

  5. Semisynthesis and quantitative structure-activity relationship (QSAR) study of some cholesterol-based hydrazone derivatives as insecticidal agents.

    PubMed

    Yang, Chun; Shao, Yonghua; Zhi, Xiaoyan; Huan, Qu; Yu, Xiang; Yao, Xiaojun; Xu, Hui

    2013-09-01

    In continuation of our program aimed at the discovery and development of natural-product-based insecticidal agents, four series of novel cholesterol-based hydrazone derivatives were synthesized, and their insecticidal activity was tested against the pre-third-instar larvae of oriental armyworm, Mythimna separata (Walker) in vivo at 1mg/mL. All the derivatives showed the better insecticidal activity than their precursor cholesterol. Quantitative structure-activity relationship (QSAR) model demonstrated that six descriptors such as RDF085v, Mor06u, Mor11u, Dv, HATS0v and H-046, are likely to influence the insecticidal activity of these compounds. Among them, two important ones are the Mor06u and RDF085v. PMID:23891182

  6. Toward the Development of Specific G-Quadruplex Binders: Synthesis, Biophysical, and Biological Studies of New Hydrazone Derivatives.

    PubMed

    Amato, Jussara; Morigi, Rita; Pagano, Bruno; Pagano, Alessia; Ohnmacht, Stephan; De Magis, Alessio; Tiang, Yee-Peng; Capranico, Giovanni; Locatelli, Alessandra; Graziadio, Alessandra; Leoni, Alberto; Rambaldi, Mirella; Novellino, Ettore; Neidle, Stephen; Randazzo, Antonio

    2016-06-23

    G-Quadruplex-binding compounds are currently perceived as possible anticancer therapeutics. Here, starting from a promising lead, a small series of novel hydrazone-based compounds were synthesized and evaluated as G-quadruplex binders. The in vitro G-quadruplex-binding properties of the synthesized compounds were investigated employing both human telomeric and oncogene promoter G-quadruplexes with different folding topologies as targets. The present investigation led to the identification of potent G-quadruplex stabilizers with high selectivity over duplex DNA and preference for one G-quadruplex topology over others. Among them, selected derivatives have been shown to trap G-quadruplex structures in the nucleus of cancer cells. Interestingly, this behavior correlates with efficient cytotoxic activity in human osteosarcoma and colon carcinoma cells. PMID:27223049

  7. On the roles of close shell interactions in the structure of acyl-substituted hydrazones: An experimental and theoretical approach

    NASA Astrophysics Data System (ADS)

    Saeed, Aamer; Ifzan Arshad, M.; Bolte, Michael; Fantoni, Adolfo C.; Delgado Espinoza, Zuly Y.; Erben, Mauricio F.

    2016-03-01

    The 2-(phenyl-hydrazono)-succinic acid dimethyl ester compound was synthesized by reacting phenylhydrazine with dimethylacetylene dicarboxylate at room temperature and characterized by elemental analysis, infrared, Raman, 1H and 13C NMR spectroscopies and mass spectrometry. Its solid state structure was determined by X-ray diffraction methods. The X-ray structure determination corroborates that the molecule is present in the crystal as the hydrazone tautomer, probably favored by a strong intramolecular N-H···Odbnd C hydrogen bond occurring between the carbonyl (-Cdbnd O) and the hydrazone -Cdbnd N-NH- groups. A substantial fragment of the molecular skeleton is planar due to an extended π-bonding delocalization. The topological analysis of the electron densities (Atom in Molecule, AIM) allows characterization of intramolecular N-H···O interaction, that can be classified as a resonant assisted hydrogen bond (RAHB). Moreover, the Natural Bond Orbital population analysis confirms that a strong hyperconjugative lpO1 → σ*(N2-H) remote interaction between the C2dbnd O1 and N2-H groups takes place. Periodic system electron density and topological analysis have been applied to characterize the intermolecular interactions in the crystal. Weak intermolecular interactions determine the crystal packing, and the prevalence of non-directional dispersive contributions are inferred on topological grounds. The IR spectrum of the crystalline compound was investigated by means of density functional theory calculations carried out with periodic boundary conditions on the crystal, showing excellent agreement between theory and the experiments. The vibrational assignment is complemented with the analysis of the Raman spectrum.

  8. Synthesis of novel flavone hydrazones: in-vitro evaluation of α-glucosidase inhibition, QSAR analysis and docking studies.

    PubMed

    Imran, Syahrul; Taha, Muhammad; Ismail, Nor Hadiani; Kashif, Syed Muhammad; Rahim, Fazal; Jamil, Waqas; Hariono, Maywan; Yusuf, Muhammad; Wahab, Habibah

    2015-11-13

    Thirty derivatives of flavone hydrazone (5-34) had been synthesized through a five-step reaction and screened for their α-glucosidase inhibition activity. Chalcone 1 was synthesized through aldol condensation then subjected through oxidative cyclization, esterification, and condensation reaction to afford the final products. The result for baker's yeast α-glucosidase (EC 3.2.1.20) inhibition assay showed that all compounds are active with reference to the IC50 value of the acarbose (standard drug) except for compound 3. Increase in activity observed for compounds 2 to 34 clearly highlights the importance of flavone, hydrazide and hydrazone linkage in suppressing the activity of α-glucosidase. Additional functional group on N-benzylidene moiety further enhances the activity significantly. Compound 5 (15.4 ± 0.22 μM), a 2,4,6-trihydroxy substituted compound, is the most active compound in the series. Other compounds which were found to be active are those having chlorine, fluorine, and nitro substituents. Compounds with methoxy, pyridine, and methyl substituents are weakly active. Further studies showed that they are not active in inhibiting histone deacetylase activity and do not possess any cytotoxic properties. QSAR model was being developed to further identify the structural requirements contributing to the activity. Using Discovery Studio (DS) 2.5, various 2D descriptors were being used to develop the model. The QSAR model is able to predict the pIC50 and could be used as a prediction tool for compounds having the same skeletal framework. Molecular docking was done for all compounds using homology model of α-glucosidase to identify important binding modes responsible for inhibition activity. PMID:26491979

  9. On the roles of close shell interactions in the structure of acyl-substituted hydrazones: An experimental and theoretical approach.

    PubMed

    Saeed, Aamer; Ifzan Arshad, M; Bolte, Michael; Fantoni, Adolfo C; Delgado Espinoza, Zuly Y; Erben, Mauricio F

    2016-03-15

    The 2-(phenyl-hydrazono)-succinic acid dimethyl ester compound was synthesized by reacting phenylhydrazine with dimethylacetylene dicarboxylate at room temperature and characterized by elemental analysis, infrared, Raman, (1)H and (13)C NMR spectroscopies and mass spectrometry. Its solid state structure was determined by X-ray diffraction methods. The X-ray structure determination corroborates that the molecule is present in the crystal as the hydrazone tautomer, probably favored by a strong intramolecular N-H···O=C hydrogen bond occurring between the carbonyl (-C=O) and the hydrazone -C=N-NH- groups. A substantial fragment of the molecular skeleton is planar due to an extended π-bonding delocalization. The topological analysis of the electron densities (Atom in Molecule, AIM) allows characterization of intramolecular N-H···O interaction, that can be classified as a resonant assisted hydrogen bond (RAHB). Moreover, the Natural Bond Orbital population analysis confirms that a strong hyperconjugative lpO1→σ*(N2-H) remote interaction between the C2=O1 and N2-H groups takes place. Periodic system electron density and topological analysis have been applied to characterize the intermolecular interactions in the crystal. Weak intermolecular interactions determine the crystal packing, and the prevalence of non-directional dispersive contributions are inferred on topological grounds. The IR spectrum of the crystalline compound was investigated by means of density functional theory calculations carried out with periodic boundary conditions on the crystal, showing excellent agreement between theory and the experiments. The vibrational assignment is complemented with the analysis of the Raman spectrum. PMID:26761413

  10. Compatibility of cholecalciferol, haloperidol, imipramine hydrochloride, levodopa/carbidopa, lorazepam, minocycline hydrochloride, tacrolimus monohydrate, terbinafine, tramadol hydrochloride and valsartan in SyrSpend SF PH4 oral suspensions.

    PubMed

    Polonini, H C; Silva, S L; Cunha, C N; Brandão, M A F; Ferreira, A O

    2016-04-01

    A challenge with compounding oral liquid formulations is the limited availability of data to support the physical, chemical and microbiological stability of the formulation. This poses a patient safety concern and a risk for medication errors. The objective of this study was to evaluate the compatibility of the following active pharmaceutical ingredients (APIs) in 10 oral suspensions, using SyrSpend SF PH4 (liquid) as the suspending vehicle: cholecalciferol 50,000 IU/mL, haloperidol 0.5 mg/mL, imipramine hydrochloride 5.0 mg/mL, levodopa/carbidopa 5.0/1.25 mg/mL, lorazepam 1.0 mg/mL, minocycline hydrochloride 10.0 mg/mL, tacrolimus monohydrate 1.0 mg/mL, terbinafine 25.0 mg/mL, tramadol hydrochloride 10.0 mg/mL and valsartan 4.0 mg/mL. The suspensions were stored both refrigerated (2 - 8 degrees C) and at controlled room temperature (20 - 25 degrees C). This is the first stability study for these APIs in SyrSpend SF PH4 (liquid). Further, the stability of haloperidol,ilmipramine hydrochloride, minocycline, and valsartan in oral suspension has not been previously reported in the literature. Compatibility was assessed by measuring percent recovery at varying time points throughout a 90 days period. Quantification of the APIs was performed by high performance liquid chromatography (HPLC-UV). Given the percentage of recovery of the APIs within the suspensions, the beyond-use date of the final preparations was found to be at least 90 days for most suspensions both refrigerated and at room temperature. Exceptions were: Minocycline hydrochloride at both storage temperatures (60 days), levodopa/carbidopa at room temperature (30 days), and lorazepam at room temperature (60 days). This suggests that compounded suspensions of APIs from different pharmacological classes in SyrSpend SF PH4 (liquid) are stable. PMID:27209697

  11. Acute dermal toxicity of guanidine hydrochloride in rabbits. Report for 18 May-1 August 1984

    SciTech Connect

    Hiatt, G.F.; Sanso, S.K.; Korte, D.W.

    1989-12-01

    The acute dermal toxicity of guanidine hydrochloride was evaluated in five male and five female New Zealand White rabbits. Guanidine hydrochloride (2 g/kg) was applied topically to the clipped dorsal skin surface for 24 hours. No compound-related deaths or clinical signs were observed; however, guanidine hydrochloride did produce dermal irritation, necrosis, and eschar formation under conditions of the study.

  12. 21 CFR 524.1662a - Oxytetracycline hydrochloride and hydrocortisone spray.

    Code of Federal Regulations, 2010 CFR

    2010-04-01

    ... 21 Food and Drugs 6 2010-04-01 2010-04-01 false Oxytetracycline hydrochloride and hydrocortisone... NEW ANIMAL DRUGS § 524.1662a Oxytetracycline hydrochloride and hydrocortisone spray. (a) Specifications. Each 3-ounce unit of oxytetracycline hydrochloride and hydrocortisone spray contains...

  13. Validated Colorimetric Assay of Clonidine Hydrochloride from Pharmaceutical Preparations.

    PubMed

    Corciova, Andreia

    2016-01-01

    Clonidine hydrochloride is an antihypertensive agent used for migraine prophylaxis, attention deficit hyperactivity disorder, menopausal flushing and Tourette syndrome. The quantity of the active substance in pharmaceutical preparations must be within specific limits, in agreement with the respective label claim. Therefore, the aim of this study was to establish the conditions for two spectrophotometric methods for clonidine determination, based on the formation of the ion pair complex between clonidine hydrochloride and thymol blue/bromophenol blue. A Jasco UV-Vis 530 spectrophotometer was used for the analysis and the maxim absorbance was measured at 418 nm/448 nm against blank solution. After validation, the methods were used for quantification of clonidine hydrochloride in two commercial samples (tablets). The recovery of active substance varies between 98.06 and 100.13 % without interferences from the excipients. PMID:27610155

  14. Temperature-dependent THz vibrational spectra of clenbuterol hydrochloride

    NASA Astrophysics Data System (ADS)

    Yang, YuPing; Lei, XiangYun; Yue, Ai; Zhang, Zhenwei

    2013-04-01

    Using the high-resolution Terahertz Time-domain spectroscopy (THz-TDS) and the standard sample pellet technique, the far-infrared vibrational spectra of clenbuterol hydrochloride (CH), a β 2-adrenergic agonist for decreasing fat deposition and enhancing protein accretion, were measured in temperature range of 77-295 K. Between 0.2 and 3.6 THz (6.6-120.0 cm-1), seven highly resolved spectral features, strong line-narrowing and a frequency blue-shift were observed with cooling. However, ractopamine hydrochloride, with some structural and pharmacological similarities to clenbuterol hydrochloride, showed no spectral features, indicating high sensitivity and strong specificity of THz-TDS. These results could be used for the rapid and nondestructive CH residual detection in food safety control.

  15. Colestipol hydrochloride prophylaxis of diarrhea during pelvic radiotherapy

    SciTech Connect

    Stryker, J.A.; Chung, C.K.; Layser, J.D.

    1983-02-01

    Thirty-three patients were randomized prior to pelvic radiotherapy to receive the bile acid-sequestering resin colestipol hydrochloride, 5 grams qid, during the entire time of their therapy or diphenoxylate hydrochloride and atropine sulfate 2.5-20 mg per day (control) if they experienced diarrhea. The colestipol patients also took diphenoxylate if they had diarrhea. The patients in the colestipol group often experienced nausea, vomiting, and abdominal cramps and 8 were forced to discontinue the drug. There was no difference in the weekly stool frequency between the colestipol and the control patients but the colestipol patients who took at least 50% of the prescribed dose required fewer diphenoxylate tablets than the controls. The data suggest that colestipol hydrochloride is not of value in preventing radiation-induced diarrhea because of the side effects associated with the drug, but the theory on which the use of bile acid-sequestering agents is based may be correct.

  16. Validated Colorimetric Assay of Clonidine Hydrochloride from Pharmaceutical Preparations

    PubMed Central

    Corciova, Andreia

    2016-01-01

    Clonidine hydrochloride is an antihypertensive agent used for migraine prophylaxis, attention deficit hyperactivity disorder, menopausal flushing and Tourette syndrome. The quantity of the active substance in pharmaceutical preparations must be within specific limits, in agreement with the respective label claim. Therefore, the aim of this study was to establish the conditions for two spectrophotometric methods for clonidine determination, based on the formation of the ion pair complex between clonidine hydrochloride and thymol blue/bromophenol blue. A Jasco UV-Vis 530 spectrophotometer was used for the analysis and the maxim absorbance was measured at 418 nm/448 nm against blank solution. After validation, the methods were used for quantification of clonidine hydrochloride in two commercial samples (tablets). The recovery of active substance varies between 98.06 and 100.13 % without interferences from the excipients. PMID:27610155

  17. Propranolol hydrochloride release behaviour of crosslinked chitosan membranes.

    PubMed

    Thacharodi, D; Rao, K P

    1993-01-01

    Chitosan membranes of 20 microns thickness were prepared by a solvent evaporation technique and crosslinked with different concentrations of glutaraldehyde to obtain membranes of various degrees of crosslinking. These membranes were characterized by thermogravimetric (TG) analysis, differential scanning calorimetry (DSC) and tensile strength studies. The effect of crosslinking on the permeability of membranes to propranolol hydrochloride was evaluated by permeation studies conducted in static glass diffusion cells. A decrease in the thermal stability of chitosan membranes due to crosslinking was observed. The tensile strength of the membranes was improved by crosslinking. The introduction of crosslink points within the membrane reduced its permeability to propranolol hydrochloride as evidenced by decreased permeability and diffusion coefficients. Permeability studies revealed the operation of a pore mechanism in the transport of hydrophilic agents such as propranolol hydrochloride through chitosan and crosslinked chitosan membranes. PMID:7764115

  18. Stability of ondansetron hydrochloride and 12 medications in plastic syringes.

    PubMed

    Stewart, J T; Warren, F W; King, D T; Venkateshwaran, T G; Fox, J L

    1998-12-15

    The stability and compatibility of ondansetron hydrochloride with neostigmine methylsulfate, naloxone hydrochloride, midazolam hydrochloride, fentanyl citrate, alfentanil hydrochloride, atropine sulfate, morphine sulfate, meperidine hydrochloride, propofol, droperidol, metoclopramide monohydrochloride, and glycopyrrolate were studied. Ondansetron 1.33 or 1.0 mg/mL was combined with 0.9% sodium chloride injection and each of the 12 drugs in duplicate in plastic syringes (or glass for propofol). The syringes were stored at 21.8-23.4 or 4 degrees C in the dark, except for those containing propofol, which were stored at ambient temperature. Samples were removed at 0, 4, 8, and 24 hours for analysis by high-performance liquid chromatography and pH measurement; the propofol-containing samples were removed at 0, 1, 2, and 4 hours. Syringes were visually assessed for color and clarity, and particulate content was measured with a particle counter at the end of the study period. All solutions containing ondansetron retained more than 90% of their initial ondansetron concentration. Solutions containing each of the other drugs except droperidol retained more than 90% of their initial concentration of these drugs. The solutions containing droperidol retained more than 90% of their initial droperidol concentration for up to eight hours at ambient temperature but precipitated quickly at 4 degrees C. In combinations of ondansetron 1.33 or 1.0 mg/mL and 10 of 12 drugs, all drugs were stable for 24 hours in plastic syringes at 23 and 4 degrees C; ondansetron hydrochloride 1.0 mg/mL and propofol 1.0 and 5.0 mg/mL in admixtures were stable for 4 hours, and droperidol on its own and combined with ondansetron 1.0 mg/mL was stable for no more than 8 hours at ambient temperature. PMID:9872702

  19. PREDICTIVE PHARMACOKINETICS OF TRAMADOL HYDROCHLORIDE FLOATING TABLETS.

    PubMed

    Wang, Jianming; Zhang, Yanzhen; Guo, Zhiling; Tao, Qingwen; Wang, Yongjun; Zhou, Wei; Ma, Xiao; Li, Zhihong

    2016-01-01

    The purpose of this study was to propose the effectiveness of convolution approach to predict pharmacokinetics of tramadol hydrochloride floating tablets, prepared by using various ratios of carbopol, HPMC K100M, and Hibiscus rosa Sinensis as excipient. The in vitro dissolution test was conducted using paddle method in 900 mL of HCl buffer with pH 1.2 to simulate the gastric condition. The stirring speed of paddles was set at 70 rpm. Temperature of dissolution medium was adjusted at 37 ± 5 °C. At predetermined time points, 5 mL of dissolution samples were taken with a replacement of same volume using fresh medium. The obtained samples were analyzed at 271 nm using UV visible spectrophotometer. The values of predicted pharmacokinetic parameters like Cmax (maximum blood drug level), Tmax (time required to attain maximum blood drug level), and AUC (area under blood drug concentration curve) ranged between 80.8 ± 3.2-119.6 ± 4.7 ng/mL, 11.4 ± 0.2-12.2 ± 0.2 h, and 1430.5 ± 209.5-1970.6 ± 287.4 ng.h/mL, respectively. This certainly is a desired feature required at the formulation development step, where the formulator requires the development of a formulation using desired in vivo features on the basis of only accessible in vitro data. It can be concluded from the results that convolution method is a practical method for the prediction of drug concentration in blood and for quality control. PMID:27476294

  20. Medium effects on fluorescence of ciprofloxacin hydrochloride

    NASA Astrophysics Data System (ADS)

    Yang, Rui; Fu, Yan; Li, Long-Di; Liu, Jia-Ming

    2003-10-01

    The medium (pH, organic solvents, cyclodextrin (CD) or surfactants) effects on the fluorescence of ciprofloxacin hydrochloride (CPFX·HCl) were studied in detail. It is found that the three acid constants of ciprofloxacin (CPFX) are near to each other. Therefore the relation curve between pH and fluorescence intensity has no strident change and keeps relative stable in the pH range of 2-7. When pH was in the range of 5.5-6.0, the fluorescence intensity of CPFX reached the max. The kind and amount of organic solvent added to the luminescent system have various effects. Ethanol quenched fluorescence and the fluorescence excitation wavelength is red shift at first and then blue shift. Acetone has complicated effects on the fluorescence properties of CPFX·HCl solution. The experiment result shows that acetone is really a quencher when its volume content in the system is from 0 to 20%, but when its content is 90%, the signal intensity is unexpectedly one and a half times as much as that of no acetone. This means that there is a strong interaction between the acetone and CPFX; CPFX·H + could be included into the γ-CD but the capping effect is not notable. The effect of cationic surfactant cetyltrimethylammonium bromide and non-ionic surfactant TX-100 and TX-80 on CPFX fluorescence was unimpressive, but the anionic surfactant's effect is aberrant. The fluorescence intensity of CPFX·HCl solution experiences three stages of increasing, decreasing and increasing in turn, as sodium dodecyl sulfate is adding gradually. But for sodium lauryl sulfonate, there are only two stages of decreasing and increasing with the concentration increasing. It is problematic to illustrate clearly the effect mechanism of acetone and anionic surfactant at present. Undoubtedly, the experimental results in this paper should be useful in practice works and the research is worth studying still further.

  1. Degradation of Verapamil hydrochloride in water by gliding arc discharge.

    PubMed

    Krishna, Syam; Maslani, Alan; Izdebski, Tomasz; Horakova, Marta; Klementova, Sarka; Spatenka, Petr

    2016-06-01

    This study investigated the influence of gliding arc plasma discharge on the degradation of Verapamil hydrochloride in water. The plasma discharge was characterized by means of optical emission spectroscopy. Spectra of various atomic and molecular species were observed. Aqueous solution of Verapamil hydrochloride was exposed to gliding arc discharge operated in continuous discharge at atmospheric pressure and room temperature. The identification of Verapamil, the degradation mechanisms of Verapamil and its transformation products were performed using liquid chromatography - mass spectrometry (HPLC-MS). Experimental results indicate that the atmospheric pressure gliding arc plasma treatment has noticeable effects on Verapamil with satisfactory degradation efficiency. Plausible mechanisms of the degradation were discussed. PMID:26953731

  2. Field application of Telazol (tiletamine hydrochloride and zolazepam hydrochloride) to immobilize wild red howler monkeys (Alouatta seniculus) in Venezuela.

    PubMed

    Agoramoorthy, G; Rudran, R

    1994-07-01

    Telazol (TEL) (tiletamine hydrochloride and zolazepam hydrochloride combination) was used to immobilize 50 wild red howler monkeys (Alouatta seniculus) in Venezuela between October 1989 and February 1991. The mean (+/- SD) dosages of TEL used for adult males and adult females were 22.4 (+/- 7.3) mg/kg and 22.5 (+/- 5.0) mg/kg, respectively. Juveniles of both sexes received a mean dose of 30.5 (+/- 5.6) mg/kg. The induction time for TEL ranged from 1 to 6.2 min. Thirteen animals were given an additional dosage of ketamine hydrochloride manually when they recovered from the first injection of TEL. Total recovery times ranged from 39 to 308 min. There were no apparent side effects to the fetuses of two pregnant females. PMID:7933286

  3. Formulation and Evaluation of Multilayered Tablets of Pioglitazone Hydrochloride and Metformin Hydrochloride

    PubMed Central

    Chowdary, Y. Ankamma; Raparla, Ramakrishna; Madhuri, Muramshetty

    2014-01-01

    In the treatment of type 2 diabetes mellitus a continuous therapy is required which is a more complex one. As in these patients there may be a defect in both insulin secretion and insulin action exists. Hence, the treatment depends on the pathophysiology and the disease state. In the present study, multilayered tablets of pioglitazone hydrochloride 15 mg and metformin hydrochloride 500 mg were prepared in an attempt for combination therapy for the treatment of type 2 diabetes mellitus. Pioglitazone HCl was formulated as immediate release layer to show immediate action by direct compression method using combination of superdisintegrants, namely, crospovidone and avicel PH 102. Crospovidone at 20% concentration showed good drug release profile at 2 hrs. Metformin HCl was formulated as controlled release layer to prolong the drug action by incorporating hydrophilic polymers such as HPMC K4M by direct compression method and guar gum by wet granulation method in order to sustain the drug release from the tablets and maintain its integrity so as to provide a suitable formulation. The multilayered tablets were prepared after carrying out the optimization of immediate release layer and were evaluated for various precompression and postcompression parameters. Formulation F13 showed 99.97% of pioglitazone release at 2 hrs in 0.1 N HCl and metformin showed 98.81% drug release at 10 hrs of dissolution in 6.8 pH phosphate buffer. The developed formulation is equivalent to innovator product in view of in vitro drug release profile. The results of all these evaluation tests are within the standards. The procedure followed for the formulation of these tablets was found to be reproducible and all the formulations were stable after accelerated stability studies. Hence, multilayered tablets of pioglitazone HCl and metformin HCl can be a better alternative way to conventional dosage forms. PMID:26556204

  4. Formulation and Evaluation of Multilayered Tablets of Pioglitazone Hydrochloride and Metformin Hydrochloride.

    PubMed

    Chowdary, Y Ankamma; Raparla, Ramakrishna; Madhuri, Muramshetty

    2014-01-01

    In the treatment of type 2 diabetes mellitus a continuous therapy is required which is a more complex one. As in these patients there may be a defect in both insulin secretion and insulin action exists. Hence, the treatment depends on the pathophysiology and the disease state. In the present study, multilayered tablets of pioglitazone hydrochloride 15 mg and metformin hydrochloride 500 mg were prepared in an attempt for combination therapy for the treatment of type 2 diabetes mellitus. Pioglitazone HCl was formulated as immediate release layer to show immediate action by direct compression method using combination of superdisintegrants, namely, crospovidone and avicel PH 102. Crospovidone at 20% concentration showed good drug release profile at 2 hrs. Metformin HCl was formulated as controlled release layer to prolong the drug action by incorporating hydrophilic polymers such as HPMC K4M by direct compression method and guar gum by wet granulation method in order to sustain the drug release from the tablets and maintain its integrity so as to provide a suitable formulation. The multilayered tablets were prepared after carrying out the optimization of immediate release layer and were evaluated for various precompression and postcompression parameters. Formulation F13 showed 99.97% of pioglitazone release at 2 hrs in 0.1 N HCl and metformin showed 98.81% drug release at 10 hrs of dissolution in 6.8 pH phosphate buffer. The developed formulation is equivalent to innovator product in view of in vitro drug release profile. The results of all these evaluation tests are within the standards. The procedure followed for the formulation of these tablets was found to be reproducible and all the formulations were stable after accelerated stability studies. Hence, multilayered tablets of pioglitazone HCl and metformin HCl can be a better alternative way to conventional dosage forms. PMID:26556204

  5. Synthesis of o-(Dimethylamino)aryl Ketones, Acridones, Acridinium Salts, and 1H-Indazoles by the Reaction of Hydrazones and Arynes

    PubMed Central

    Dubrovskiy, Anton V.; Larock, Richard C.

    2012-01-01

    A novel, efficient route to biologically and pharmaceutically important o-(dimethylamino)aryl ketones, acridones, acridinium salts, and 1H-indazoles has been developed starting from readily available hydrazones of aldehydes and o-(trimethylsilyl)aryl triflates. The reaction proceeds through arynes under mild conditions, tolerates a wide range of functional groups, and provides the final products in good to excellent yields. PMID:23206164

  6. Synthesis and Biological Evaluation of New Hydrazone Derivatives of Quinoline and Their Cu(II) and Zn(II) Complexes against Mycobacterium tuberculosis

    PubMed Central

    Mandewale, Mustapha C.; Thorat, Bapu; Shelke, Dnyaneshwar; Yamgar, Ramesh

    2015-01-01

    A new series of quinoline hydrazone derivatives and their metal complexes have been synthesized and their biological properties have been evaluated against Mycobacterium tuberculosis (H37 RV strain). Most of the newly synthesized compounds displayed 100% inhibitory activity at a concentration of 6.25–25 μg/mL, against Mycobacterium tuberculosis. Fluorescence properties of all the synthesized compounds have been studied. PMID:26759537

  7. Synthesis, structure and study of azo-hydrazone tautomeric equilibrium of 1,3-dimethyl-5-(arylazo)-6-amino-uracil derivatives

    NASA Astrophysics Data System (ADS)

    Debnath, Diptanu; Roy, Subhadip; Li, Bing-Han; Lin, Chia-Her; Misra, Tarun Kumar

    2015-04-01

    Azo dyes, 1,3-dimethyl-5-(arylazo)-6-aminouracil (aryl = -C6H5 (1), -p-CH3C6H4 (2), -p-ClC6H4 (3), -p-NO2C6H4 (4)) were prepared and characterized by UV-vis, FT-IR, 1H NMR, 13C NMR spectroscopic techniques and single crystal X-ray crystallographic analysis. In the light of spectroscopic analysis it evidences that of the tautomeric forms, the azo-enamine-keto (A) form is the predominant form in the solid state whereas in different solvents it is the hydrazone-imine-keto (B) form. The study also reveals that the hydrazone-imine-keto (B) form exists in an equilibrium mixture with its anionic form in various organic solvents. The solvatochromic and photophysical properties of the dyes in various solvents with different hydrogen bonding parameter were investigated. The dyes exhibit positive solvatochromic property on moving from polar protic to polar aprotic solvents. They are fluorescent active molecules and exhibit high intense fluorescent peak in some solvents like DMSO and DMF. It has been demonstrated that the anionic form of the hydrazone-imine form is responsible for the high intense fluorescent peak. In addition, the acid-base equilibrium in between neutral and anionic form of hydrazone-imine form in buffer solution of varying pH was investigated and evaluated the pKa values of the dyes by making the use of UV-vis spectroscopic methods. The determined acid dissociation constant (pKa) values increase according to the sequence of 2 > 1 > 3 > 4.

  8. 21 CFR 524.1982 - Proparacaine hydrochloride ophthalmic solution.

    Code of Federal Regulations, 2012 CFR

    2012-04-01

    ... 21 Food and Drugs 6 2012-04-01 2012-04-01 false Proparacaine hydrochloride ophthalmic solution. 524.1982 Section 524.1982 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL DRUGS, FEEDS, AND RELATED PRODUCTS OPHTHALMIC AND TOPICAL DOSAGE FORM NEW ANIMAL DRUGS § 524.1982...

  9. Amides and Hydrazides from Amine and Hydrazine Hydrochlorides.

    ERIC Educational Resources Information Center

    Shama, Sami A.; Tran, Thuan L.

    1978-01-01

    This safe and efficient procedure for the synthesis of N-substituted amides and hydrazides is a modification of the Schotten-Bausmann procedure in which the amine or hydrazide is replaced by the corresponding hydrochloride salt, and the use of alkali is eliminated. (Author/BB)

  10. 21 CFR 522.1335 - Medetomidine hydrochloride injection.

    Code of Federal Regulations, 2013 CFR

    2013-04-01

    ... 21 Food and Drugs 6 2013-04-01 2013-04-01 false Medetomidine hydrochloride injection. 522.1335 Section 522.1335 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL DRUGS, FEEDS, AND RELATED PRODUCTS IMPLANTATION OR INJECTABLE DOSAGE FORM NEW ANIMAL DRUGS § 522.1335 Medetomidine...

  11. 21 CFR 522.1465 - Naltrexone hydrochloride injection.

    Code of Federal Regulations, 2010 CFR

    2010-04-01

    ... 21 Food and Drugs 6 2010-04-01 2010-04-01 false Naltrexone hydrochloride injection. 522.1465 Section 522.1465 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL DRUGS, FEEDS, AND RELATED PRODUCTS IMPLANTATION OR INJECTABLE DOSAGE FORM NEW ANIMAL DRUGS § 522.1465 Naltrexone...

  12. 21 CFR 522.863 - Ethylisobutrazine hydrochloride injection.

    Code of Federal Regulations, 2010 CFR

    2010-04-01

    ... 21 Food and Drugs 6 2010-04-01 2010-04-01 false Ethylisobutrazine hydrochloride injection. 522.863 Section 522.863 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL DRUGS, FEEDS, AND RELATED PRODUCTS IMPLANTATION OR INJECTABLE DOSAGE FORM NEW ANIMAL...

  13. Cradle-to-gate life cycle inventory of vancomycin hydrochloride.

    PubMed

    Ponder, Celia; Overcash, Michael

    2010-02-15

    A life cycle analysis on the cradle-to-gate production of vancomycin hydrochloride, which begins at natural resource extraction and spans through factory (gate) production, not only shows all inputs, outputs, and energy usage to manufacture the product and all related supply chain chemicals, but can highlight where process changes would have the greatest impact on raw material and energy consumption and emissions. Vancomycin hydrochloride is produced by a low-yield fermentation process that accounts for 47% of the total cradle-to-gate energy. The fermentation step consumes the most raw materials and energy cradle-to-gate. Over 75% of the total cradle-to-gate energy consumption is due to steam use; sterilization within fermentation is the largest user of steam. Aeration and agitation in the fermentation vessels use 65% of the cradle-to-gate electrical energy. To reduce raw materials, energy consumption, and the associated environmental footprint of producing vancomycin hydrochloride, other sterilization methods, fermentation media, nutrient sources, or synthetic manufacture should be investigated. The reported vancomycin hydrochloride life cycle inventory is a part of a larger life cycle study of the environmental consequences of the introduction of biocide-coated medical textiles for the prevention of MRSA (methicillin-resistant Staphylococcus aureus) nosocomial infections. PMID:19942254

  14. 21 CFR 522.2615 - Tripelennamine hydrochloride injection.

    Code of Federal Regulations, 2010 CFR

    2010-04-01

    ... 21 Food and Drugs 6 2010-04-01 2010-04-01 false Tripelennamine hydrochloride injection. 522.2615 Section 522.2615 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL DRUGS, FEEDS, AND RELATED PRODUCTS IMPLANTATION OR INJECTABLE DOSAGE FORM NEW ANIMAL...

  15. 21 CFR 522.1462 - Naloxone hydrochloride injection.

    Code of Federal Regulations, 2010 CFR

    2010-04-01

    ... 21 Food and Drugs 6 2010-04-01 2010-04-01 false Naloxone hydrochloride injection. 522.1462 Section 522.1462 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL DRUGS, FEEDS, AND RELATED PRODUCTS IMPLANTATION OR INJECTABLE DOSAGE FORM NEW ANIMAL...

  16. 21 CFR 522.2002 - Propiopromazine hydrochloride injection.

    Code of Federal Regulations, 2010 CFR

    2010-04-01

    ... 21 Food and Drugs 6 2010-04-01 2010-04-01 false Propiopromazine hydrochloride injection. 522.2002 Section 522.2002 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL DRUGS, FEEDS, AND RELATED PRODUCTS IMPLANTATION OR INJECTABLE DOSAGE FORM NEW ANIMAL DRUGS § 522.2002...

  17. Chemical Immobilization of Sloth Bears (Melursus ursinus) with Ketamine Hydrochloride and Xylazine Hydrochloride: Hematology and Serum Biochemical Values

    PubMed Central

    Veeraselvam, M.; Sridhar, R.; Perumal, P.; Jayathangaraj, M. G.

    2014-01-01

    The present study was conducted to define the physiological responses of captive sloth bears immobilized with ketamine hydrochloride and xylazine hydrochloride and to determine and compare the values of hematology and serum biochemical parameters between sexes. A total of 15 sloth bears were immobilized using combination of ketamine hydrochloride and xylazine hydrochloride drugs at the dose rate of 5.0 milligram (mg) per kg body weight and 2.0 mg per kg body weight, respectively. The use of combination of these drugs was found satisfactory for the chemical immobilization of captive sloth bears. There were no significant differences observed in induction time and recovery time and physiological parameters such as heart rate, respiratory rate, and rectal temperature between sexes. Health related parameters comprising hematological values like packed cell volume (PCV), hemoglobin (Hb), red blood cell count (RBC), erythrocyte indices, and so forth and biochemical values like total protein, blood urea nitrogen (BUN), creatinine, alkaline amino-transferase (ALT), aspartate amino-transferase (AST), and so forth were estimated in 11 (5 males and 6 females) apparently healthy bears. Comparison between sexes revealed significant difference in PCV (P < 0.05) and mean corpuscular hemoglobin concentration (MCHC) (P < 0.05). The study might help to evaluate health profiles of sloth bears for appropriate line treatment. PMID:24876990

  18. Effect of thiamine hydrochloride, pyridoxine hydrochloride and calcium-d-pantothenate on the patulin content of apple juice concentrate.

    PubMed

    Yazici, Serafettin; Velioglu, Y Sedat

    2002-08-01

    Thiamine hydrochloride, pyridoxine hydrochloride and calcium-d-pantothenate were applied apple juice concentrates (AJC) at various doses in order to reduce the patulin content. AJC samples containing high levels of patulin were stored at 22 +/- 2 degrees C and 4 degrees C for 6 months after vitamins were added. Patulin was fully degraded at the end of a 6-month period in samples stored at 22 +/- 2 degrees C, on the other hand, other quality parameters diminished significantly. Without any considerable reduction on other quality parameters, applications of 1000 and 2500 mg/kg calcium-d-pantothenate resulted in reduction of patulin of 73.6 and 94.3%, respectively, however, 42.1% of patulin reduction was observed in the control sample of AJC stored for 1 month at 22 +/- 2 degrees C. Addition of thiamine hydrochloride (1000 mg/kg), pyrodoxine hydrochloride (625 or 875 mg/kg) and calcium-d-pantothenate (1000 or 2500 mg/kg) into the samples and storage at 4 degrees C for 6 months yielded 55.5 to 67.7% of patulin reduction which was only 35.8% for the control while the other quality parameters were protected adequately. PMID:12224421

  19. Novel hydrazone moiety-bearing aminopyrimidines as selective inhibitors of epidermal growth factor receptor T790M mutant.

    PubMed

    Qin, Mingze; Wang, Tingting; Xu, Boxuan; Ma, Zonghui; Jiang, Nan; Xie, Hongbo; Gong, Ping; Zhao, Yanfang

    2015-11-01

    The epidermal growth factor receptor (EGFR) T790M mutant is found in approximately 50% of clinically acquired resistance to gefitinib among patients with non-small cell lung cancer (NSCLC). Here, a series of novel aminopyrimidines bearing a hydrazone moiety were identified as potent and selective EGFR inhibitors. Compounds 14a, 15g, and 15i potently inhibited all EGFR mutants including EGFR T790M/L858R, EGFR T790M/delE746_A750, and EGFR T790M while they showed weak effects on the wild type (WT) EGFR. In addition, these compounds effectively suppressed proliferation of gefitinib-resistant H1975 (EGFR T790M/L858R) cells but were less potent against A549 (WT EGFR and k-Ras mutation) and HT-29 (non-special gene type) cells, showing a high safety index. Therefore, 14a, 15g, and 15i might be promising candidates to overcome drug resistance mediated by the EGFR T790M mutant. PMID:26451770

  20. Synthesis, structure, infrared and fluorescence spectra of new rare earth complexes with 6-hydroxy chromone-3-carbaldehyde benzoyl hydrazone

    NASA Astrophysics Data System (ADS)

    Wang, Bao-Dui; Yang, Zheng-Yin; Zhang, Ding-Wa; Wang, Yan

    2006-01-01

    A novel 6-hydroxy chromone-3-carbaldehyde benzoyl hydrazone ligand and its four complexes, [LnL2(NO3)2]NO3 [Ln = Eu(1), Sm(2), Tb(3), Dy(4)], were synthesized. The complexes were characterized by the elemental analyses, molar conductivity and IR spectra. The crystal and molecular structure of Sm(III) complex was determined by single-crystal X-ray diffraction: crystallized in the triclinic system, space group P-1, Z = 1, a = 11.037(4) Å, b = 14.770(5) Å, c = 15.032(7) Å, α = 60.583(4), β = 75.528(7), γ = 88.999(4), R1 = 0.0349. The fluorescence properties of complexes in the solid state and in the organic solvent were studied in detail, respectively. Under the excitation of ultraviolet light, strong red fluorescence of solid europium complex was observed. But the green fluorescence of solid terbium complex was not observed. These observations show that the ligand favor energy transfers to the emitting energy level of Eu3+. Some factors that influence the fluorescent intensity were also discussed.

  1. Synthesis, characterization, cytotoxicity and antiangiogenic activity of copper(II) complexes with 1-adamantoyl hydrazone bearing pyridine rings.

    PubMed

    Rodić, Marko V; Leovac, Vukadin M; Jovanović, Ljiljana S; Spasojević, Vojislav; Joksović, Milan D; Stanojković, Tatjana; Matić, Ivana Z; Vojinović-Ješić, Ljiljana S; Marković, Violeta

    2016-06-10

    Three novel copper complexes with tridentate N2O ligand di(2-pyridil) ketone 1-adamantoyl hydrazone (Addpy) of the formula [Cu(II)2Cu(I)2(Addpy)2Br2(μ-Br4)] (1), catena-poly[CuCl(μ-Addpy)(μ-Cl)CuCl2]n (2) and [Cu(Addpy)(NCS)2] (3) were synthesized. Complexes are characterized by X-ray crystallography, spectral (UV-Vis, FTIR), electrochemical (CV) analyses, and magnetochemical measurements. Investigation of anticancer potential of Cu(II) complexes, mode of cell death, apoptosis, and inhibition of angiogenesis were performed. All tested malignant cell lines (HeLa, LS174, A549, K562, and MDA-MB-231) showed high sensitivity to the examined Cu(II) complexes. It has been shown that the complexes induce apoptosis in the caspase 3-dependent manner, whereas the anti-angiogenic effects of 1, 2, and 3 have been confirmed in EA.hy926 cells using a tube formation assay. PMID:27084495

  2. Structure investigation of three hydrazones Schiff's bases by spectroscopic, thermal and molecular orbital calculations and their biological activities

    NASA Astrophysics Data System (ADS)

    Belal, Arafa A. M.; Zayed, M. A.; El-Desawy, M.; Rakha, Sh. M. A. H.

    2015-03-01

    Three Schiff's bases AI (2(1-hydrazonoethyl)phenol), AII (2, 4-dibromo 6-(hydrazonomethyl)phenol) and AIII (2(hydrazonomethyl)phenol) were prepared as new hydrazone compounds via condensation reactions with molar ratio (1:1) of reactants. Firstly by reaction of 2-hydroxy acetophenone solution and hydrazine hydrate; it gives AI. Secondly condensation between 3,5-dibromo-salicylaldehyde and hydrazine hydrate gives AII. Thirdly condensation between salicylaldehyde and hydrazine hydrate gives AIII. The structures of AI-AIII were characterized by elemental analysis (EA), mass (MS), FT-IR and 1H NMR spectra, and thermal analyses (TG, DTG, and DTA). The activation thermodynamic parameters, such as, ΔE∗, ΔH∗, ΔS∗ and ΔG∗ were calculated from the TG curves using Coats-Redfern method. It is important to investigate their molecular structures to know the active groups and weak bond responsible for their biological activities. Consequently in the present work, the obtained thermal (TA) and mass (MS) practical results are confirmed by semi-empirical MO-calculations (MOCS) using PM3 procedure. Their biological activities have been tested in vitro against Escherichia coli, Proteus vulgaris, Bacillissubtilies and Staphylococcus aurous bacteria in order to assess their anti-microbial potential.

  3. Isoniazid is not a lead compound for its pyridyl ring derivatives, isonicotinoyl amides, hydrazides, and hydrazones: a critical review.

    PubMed

    Scior, T; Garcés-Eisele, S J

    2006-01-01

    The relationships between structure, disintegration and antituberculotic in vitro activity were studied for over 200 derivatives of isonicotinic acid hydrazide (isoniazid, INH). Conclusive evidence reflects that many compounds do not withstand the in vitro conditions. A pH dependant partial hydrolysis to INH occurs in the case of hydrazones, in analogy to well-known benzoic acid esters. Hydrazides and amides are cleaved into isonicotinic acid. In general, antimycobacterial potencies drop against INH except for two outliers probably with additional unspecific toxicity of their residues. Analyzing the complexity and heterogeneity of molecular events, trends linked to hydrolysis are found when structural features are clustered. Hammett sigma constants correlate to pK(a) values possessing a twofold descriptive meaning: (i) the cardinal increase of partial positive charge of the reaction center towards nucleophilic water attack and (ii) the ionization crucial for mycobacterial cell permeation through porins or lipid barriers. We review the literature concluding that many so-called "novel leads" are nothing else than precursors of an INH-based scaffold. In addition, INH ring-substitution or analogous backbones never achieve the efficiency of INH, itself a prodrug, which accumulates in Mycobacterium tuberculosis in form of its intrabacterial active principle(s) to which it is an optimal transport vehicle, evidencing that INH is not a promising lead compound at all. PMID:16918349

  4. Structural diversity in mercury(II) coordination complexes with asymmetrical hydrazone-based ligands derived from pyridine

    NASA Astrophysics Data System (ADS)

    Masoumi, Asad; Servati Gargari, Masoumeh; Mahmoudi, Ghodrat; Miroslaw, Barbara; Therrien, Bruno; Abedi, Marjan; Hazendonk, Paul

    2015-05-01

    Three novel Hg(II) complexes 1-3 of asymmetrical hydrazone-pyridine based ligands, L1-L3, with distinct coordination structures have been prepared and characterized by a single crystal X-ray diffraction, elemental and thermal analysis, and IR spectroscopy. The complexes form either discrete units with one (1) or two (2) organic ligands, or one-dimensional polymers (3). Hence the ligands can be regarded as chelating (1), mono-dentate (2) or bridging (3) agents. The mercury center is essentially neutralized in each complex by two iodide anions. The coordination in complexes 2 and 3 adopts deformed tetrahedral shapes. In contrast the Hg(II) cation in complex 1 binds three coplanar ligating atoms (O,N,N) and, as with pincer ligands, its coordination polyhedron is supplemented with two I- anions in apical positions. The structural diversity in these complexes is strongly influenced by the position of N atom in pyridine derived moieties. The crystal structure is stabilized by N/O-H⋯N/O/I hydrogen bonds and π⋯π interactions.

  5. Coordination diversity of new mononuclear ONS hydrazone with transition metals: Synthesis, characterization, molecular modeling and antimicrobial studies

    NASA Astrophysics Data System (ADS)

    Adly, Omima M. I.; Taha, A.

    2013-04-01

    The mononuclear hydrazone ligand, H2L, a condensation product of 4-amino-6-methyl-3-thioxo-3,4-dihydro-1,2,4-triazin-5(2H)-one with 2-hydroxy-1-naphthaldehyde and its metal chelates of Cu(II), Ni(II), Co(II), Zn(II), Cd(II), VO(IV) and UO2(VI) ions were synthesized and characterized using elemental analyses, spectral, magnetic and molar conductance studies as well as thermal gravimetric analysis (TGA). The physico-chemical studies support that the ligand acts as mono- or dibasic tridentate ONS donor toward metal ions forming a mononuclear square planar, tetrahedral, square pyramidal and octahedral geometrical arrangements except UO2(VI) complex in which the metal ion is octa-coordinated. The ligand field parameters, Dq, B and β values, in the case of the cobalt and nickel complexes are calculated. The kinetics of the thermal decomposition for some metal complexes studied and their thermodynamic parameters were reported. Structural parameters of the ligand and its metal chelates have been calculated and correlated with the experimental data. The ligand and its metal chelates were screened for their antimicrobial activity against Staphylococcus aureus and Bacillus subtilis as Gram-positive bacteria, Escherichia coli and Salmonella typhimurium as Gram-negative bacteria and Candida albicans as fungus strain.

  6. The Cytotoxicity of Benzaldehyde Nitrogen Mustard-2-Pyridine Carboxylic Acid Hydrazone Being Involved in Topoisomerase IIα Inhibition

    PubMed Central

    Fu, Yun; Zhou, Sufeng; Liu, Youxun; Yang, Yingli; Sun, Xingzhi; Li, Changzheng

    2014-01-01

    The antitumor property of iron chelators and aromatic nitrogen mustard derivatives has been well documented. Combination of the two pharmacophores in one molecule in drug designation is worth to be explored. We reported previously the syntheses and preliminary cytotoxicity evaluation of benzaldehyde nitrogen mustard pyridine carboxyl acid hydrazones (BNMPH) as extended study, more tumor cell lines (IC50 for HepG2: 26.1 ± 3.5 μM , HCT-116: 57.5 ± 5.3 μM, K562: 48.2 ± 4.0 μM, and PC-12: 19.4 ± 2.2 μM) were used to investigate its cytotoxicity and potential mechanism. In vitro experimental data showed that the BNMPH chelating Fe2+ caused a large number of ROS formations which led to DNA cleavage, and this was further supported by comet assay, implying that ROS might be involved in the cytotoxicity of BNMPH. The ROS induced changes of apoptosis related genes, but the TFR1 and NDRG1 metastatic genes were not obviously regulated, prompting that BNMPH might not be able to deprive Fe2+ of ribonucleotide reductase. The BNMPH induced S phase arrest was different from that of iron chelators (G1) and alkylating agents (G2). BNMPH also exhibited its inhibition of human topoisomerase IIα. Those revealed that the cytotoxic mechanism of the BNMPH could stem from both the topoisomerase II inhibition, ROS generation and DNA alkylation. PMID:24995306

  7. Growth and characterization of benzaldehyde 4-nitro phenyl hydrazone (BPH) single crystal: A proficient second order nonlinear optical material

    NASA Astrophysics Data System (ADS)

    Saravanan, M.; Abraham Rajasekar, S.

    2016-04-01

    The crystals (benzaldehyde 4-nitro phenyl hydrazone (BPH)) appropriate for NLO appliance were grown by the slow cooling method. The solubility and metastable zone width measurement of BPH specimen was studied. The material crystallizes in the monoclinic crystal system with noncentrosymmetric space group of Cc. The optical precision in the whole visible region was found to be excellent for non-linear optical claim. Excellence of the grown crystal is ascertained by the HRXRD and etching studies. Laser Damage Threshold and Photoluminescence studies designate that the grown crystal contains less imperfection. The mechanical behaviour of BPH sample at different temperatures was investigated to determine the hardness stability of the grown specimen. The piezoelectric temperament and the relative Second Harmonic Generation (for diverse particle sizes) of the material were also studied. The dielectric studies were executed at varied temperatures and frequencies to investigate the electrical properties. Photoconductivity measurement enumerates consummate of inducing dipoles due to strong incident radiation and also divulge the nonlinear behaviour of the material. The third order nonlinear optical properties of BPH crystals were deliberate by Z-scan method.

  8. Synthesis of Tolmetin Hydrazide-Hydrazones and Discovery of a Potent Apoptosis Inducer in Colon Cancer Cells.

    PubMed

    Küçükgüzel, Ş Güniz; Koç, Derya; Çıkla-Süzgün, Pelin; Özsavcı, Derya; Bingöl-Özakpınar, Özlem; Mega-Tiber, Pınar; Orun, Oya; Erzincan, Pınar; Sağ-Erdem, Safiye; Şahin, Fikrettin

    2015-10-01

    Tolmetin hydrazide and a novel series of tolmetin hydrazide-hydrazones 4a-l were synthesized in this study. The structures of the new compounds were determined by spectral (FT-IR, (1)H NMR) methods. N'-[(2,6-Dichlorophenyl)methylidene]-2-[1-methyl-5-(4-methylbenzoyl)-1H-pyrrol-2-yl]acetohydrazide (4g) was evaluated in vitro using the MTT colorimetric method against the colon cancer cell lines HCT-116 (ATCC, CCL-247) and HT-29 (ATCC, HTB-38) to determine growth inhibition and cell viability at different doses. Compound 4g exhibited anti-cancer activity with an IC50 value of 76 μM against colon cancer line HT-29 (ATCC, HTB-38) and did not display cytotoxicity toward control NIH3T3 mouse embryonic fibroblast cells compared to tolmetin. In addition, this compound was evaluated for caspase-3, caspase-8, caspase-9, and annexin-V activation in the apoptotic pathway, which plays a key role in the treatment of cancer. We demonstrated that the anti-cancer activity of this compound was due to the activation of caspase-8 and caspase-9 involved in the apoptotic pathway. In addition, in this study, we investigated the catalytical effect of COX on the HT-29 cancer line, the apoptotic mechanism, and the moleculer binding of tolmetin and compound 4g on the COX enzyme active site. PMID:26287512

  9. Rare earth complexes with 3-carbaldehyde chromone-(benzoyl) hydrazone: synthesis, characterization, DNA binding studies and antioxidant activity.

    PubMed

    Li, Yong; Yang, Zheng-Yin

    2010-01-01

    A new ligand, 3-carbaldehyde chromone-(benzoyl) hydrazone (L), was prepared by condensation of 3-carbaldehyde chromone with benzoyl hydrazine. Its four rare earth complexes have been prepared and characterized on the basis of elemental analyses, molar conductivities, mass spectra, (1)H NMR spectra, UV-vis spectra, fluorescence studies and IR spectra. The Sm(III) complex exhibits red fluorescence under UV light and the fluorescent properties of Sm(III) complex in solid state and different solutions were investigated. In addition, the DNA binding properties of the ligand and its complexes have been investigated by electronic absorption spectroscopy, fluorescence spectra, ethidium bromide displacement experiments, iodide quenching experiments, salt effect and viscosity measurements. Experimental results suggest that all the compounds can bind to DNA via an intercalation binding mode. Furthermore, the antioxidant activities of the ligand and its complexes were determined by superoxide and hydroxyl radical scavenging methods in vitro. The rare earth complexes were found to possess potent antioxidant activities that are better than those of the ligand alone. PMID:19856083

  10. Synthesis, characterization, DNA binding properties, fluorescence studies and antioxidant activity of transition metal complexes with hesperetin-2-hydroxy benzoyl hydrazone.

    PubMed

    Li, Yong; Yang, Zheng-Yin; Wang, Ming-Fang

    2010-07-01

    A novel Schiff-base ligand (H(5)L), hesperetin-2-hydroxy benzoyl hydrazone, and its copper (II), zinc (II) and nickel (II) complexes (M.H(3)L) [M(II) = Cu, Zn, Ni], have been synthesized and characterized. The ligand and Zn (II) complex exhibit green and blue fluorescence under UV light and the fluorescent properties of the ligand and Zn (II) complex in solid state and different solutions were investigated. In addition, DNA binding properties of the ligand and its metal complexes have been investigated by electronic absorption spectroscopy, fluorescence spectra, ethidium bromide displacement experiments, iodide quenching experiments, salt effect and viscosity measurements. Results suggest that all the compounds bind to DNA via an intercalation binding mode. Furthermore, the antioxidant activity of the ligand and its metal complexes was determined by superoxide and hydroxyl radical scavenging methods in vitro. The metal complexes were found to possess potent antioxidant activity and be better than the free ligand alone and some standard antioxidants like vitamin C and mannitol. PMID:20352308

  11. Synthesis, structure, spectral, thermal and first-order molecular hyperpolarizability of 4-benzoylpyridine isonicotinyl hydrazone monohydrate single crystals.

    PubMed

    Meenatchi, V; Muthu, K; Rajasekar, M; Meenakshisundaram, S P

    2014-04-24

    Single crystals of 4-benzoylpyridine isonicotinyl hydrazone monohydrate were grown by slow evaporation solution growth technique from ethanol at room temperature. It belongs to triclinic system with space group P1¯ and the cell parameters are, a=8.9250(2) Å, b=9.1540(2) Å, c=10.87500(10) Å and V=797.88(3) Å(3). Powder XRD closely resembles with that of simulated pattern from single crystal XRD. The characteristic functional groups present in the molecule are confirmed by FT-IR and FT-Raman analyses. The crystal is transparent in the visible region having a lower optical cut-off at ∼420 nm and the band gap energies are estimated by the application of Kubelka-Munk algorithm. Thermal analysis by TG/DTA indicates the stability of the material. The scanning electron microscopy studies reveal the surface morphology of the as-grown crystal. Mass spectrometry provides information pertaining to the structure and molecular weight of the compound. Theoretical calculations were performed using Hartree-Fock method with 6-31G(d,p) as the basis set for to derive the optimized geometry, dipole moment and first-order molecular hyperpolarizality (β) values. PMID:24508881

  12. Structure investigation of three hydrazones Schiff's bases by spectroscopic, thermal and molecular orbital calculations and their biological activities.

    PubMed

    Belal, Arafa A M; Zayed, M A; El-Desawy, M; Rakha, Sh M A H

    2015-03-01

    Three Schiff's bases AI (2(1-hydrazonoethyl)phenol), AII (2, 4-dibromo 6-(hydrazonomethyl)phenol) and AIII (2(hydrazonomethyl)phenol) were prepared as new hydrazone compounds via condensation reactions with molar ratio (1:1) of reactants. Firstly by reaction of 2-hydroxy acetophenone solution and hydrazine hydrate; it gives AI. Secondly condensation between 3,5-dibromo-salicylaldehyde and hydrazine hydrate gives AII. Thirdly condensation between salicylaldehyde and hydrazine hydrate gives AIII. The structures of AI-AIII were characterized by elemental analysis (EA), mass (MS), FT-IR and (1)H NMR spectra, and thermal analyses (TG, DTG, and DTA). The activation thermodynamic parameters, such as, ΔE(∗), ΔH(∗), ΔS(∗) and ΔG(∗) were calculated from the TG curves using Coats-Redfern method. It is important to investigate their molecular structures to know the active groups and weak bond responsible for their biological activities. Consequently in the present work, the obtained thermal (TA) and mass (MS) practical results are confirmed by semi-empirical MO-calculations (MOCS) using PM3 procedure. Their biological activities have been tested in vitro against Escherichia coli, Proteus vulgaris, Bacillissubtilies and Staphylococcus aurous bacteria in order to assess their anti-microbial potential. PMID:25437844

  13. HIV-1 Reverse Transcriptase Structure with RNase H Inhibitor dihydroxy benzoyl naphthyl Hydrazone Bound at a Novel Site

    SciTech Connect

    Himmel,D.; Sarafianos, S.; Dharmasena, S.; Hossain, M.; McCoy-Simandle, K.; Ilina, T.; Clark, A.; Knight, J.; Julias, J.; et al.

    2007-01-01

    The rapid emergence of drug-resistant variants of human immunodeficiency virus, type 1 (HIV-1), has limited the efficacy of anti-acquired immune deficiency syndrome (AIDS) treatments, and new lead compounds that target novel binding sites are needed. We have determined the 3.15 {angstrom} resolution crystal structure of HIV-1 reverse transcriptase (RT) complexed with dihydroxy benzoyl naphthyl hydrazone (DHBNH), an HIV-1 RT RNase H (RNH) inhibitor (RNHI). DHBNH is effective against a variety of drug-resistant HIV-1 RT mutants. While DHBNH has little effect on most aspects of RT-catalyzed DNA synthesis, at relatively high concentrations it does inhibit the initiation of RNA-primed DNA synthesis. Although primarily an RNHI, DHBNH binds >50 {angstrom} away from the RNH active site, at a novel site near both the polymerase active site and the non-nucleoside RT inhibitor (NNRTI) binding pocket. When DHBNH binds, both Tyr181 and Tyr188 remain in the conformations seen in unliganded HIV-1 RT. DHBNH interacts with conserved residues (Asp186, Trp229) and has substantial interactions with the backbones of several less well-conserved residues. On the basis of this structure, we designed substituted DHBNH derivatives that interact with the NNRTI-binding pocket. These compounds inhibit both the polymerase and RNH activities of RT.

  14. Fundamentals of ionic conductivity relaxation gained from study of procaine hydrochloride and procainamide hydrochloride at ambient and elevated pressure

    NASA Astrophysics Data System (ADS)

    Wojnarowska, Z.; Swiety-Pospiech, A.; Grzybowska, K.; Hawelek, L.; Paluch, M.; Ngai, K. L.

    2012-04-01

    The pharmaceuticals, procaine hydrochloride and procainamide hydrochloride, are glass-forming as well as ionically conducting materials. We have made dielectric measurements at ambient and elevated pressures to characterize the dynamics of the ion conductivity relaxation in these pharmaceuticals, and calorimetric measurements for the structural relaxation. Perhaps due to their special chemical and physical structures, novel features are found in the ionic conductivity relaxation of these pharmaceuticals. Data of conductivity relaxation in most ionic conductors when represented by the electric loss modulus usually show a single resolved peak in the electric modulus loss M″(f ) spectra. However, in procaine hydrochloride and procainamide hydrochloride we find in addition another resolved loss peak at higher frequencies over a temperature range spanning across Tg. The situation is analogous to many non-ionic glass-formers showing the presence of the structural α-relaxation together with the Johari-Goldstein (JG) β-relaxation. Naturally the analogy leads us to name the slower and faster processes resolved in procaine hydrochloride and procainamide hydrochloride as the primary α-conductivity relaxation and the secondary β-conductivity relaxation, respectively. The analogy of the β-conductivity relaxation in procaine HCl and procainamide HCl with JG β-relaxation in non-ionic glass-formers goes further by the finding that the β-conductivity is strongly related to the α-conductivity relaxation at temperatures above and below Tg. At elevated pressure but compensated by raising temperature to maintain α-conductivity relaxation time constant, the data show invariance of the ratio between the β- and the α-conductivity relaxation times to changes of thermodynamic condition. This property indicates that the β-conductivity relaxation has fundamental importance and is indispensable as the precursor of the α-conductivity relaxation, analogous to the relation found

  15. Growth and characterization of thiosemicarbazide hydrochloride: A semiorganic NLO material

    NASA Astrophysics Data System (ADS)

    Santhakumari, R.; Ramamurthi, K.; Babu, R. Ramesh; Evans, Helen Stoeckli; Bhagavannarayana, G.; Hema, R.

    2011-11-01

    Thiosemicarbazide hydrochloride (TSCHCL) was synthesized by mixing thiosemicarbazide and hydrochloride in 1:1 molar ratio in double distilled water. Single crystals of TSCHCL were grown by slow evaporation at room temperature and were characterized by single crystal X-ray diffraction study to determine the molecular structure and by FT-IR, 1H and 13C NMR spectral analyses to confirm the synthesized compound. Thermogravimetric and differential thermal analyses reveal the thermal stability of the crystal. The transmission spectrum of TSCHCL showed that the crystal is transparent in the wavelength range 380-1100 nm. High resolution X-ray diffractometry (HRXRD) was employed to evaluate the perfection of the grown crystal. Mechanical properties of the grown crystal were studied using Vickers microhardness test. Second harmonic generation efficiency of the powdered TSCHCL was tested using Nd:YAG laser and is ˜1.5 times that of potassium dihydrogen orthophosphate.

  16. Buspirone hydrochloride in the treatment of an atypical paraphilia.

    PubMed

    Fedoroff, J P

    1992-08-01

    A case report involving buspirone hydrochloride in the successful treatment of a patient with an atypical paraphilia and transvestic fetishism is presented. Treatment outcome was assessed by the patient's self-report as well as by retrospective examination of detailed notes about paraphilia fantasies which unknown to the therapists, had been kept by the patient. Preliminary evidence indicates that buspirone appears to effectively treat some paraphilias. PMID:1497477

  17. Tetracycline hydrochloride: A potential clinical drug for radioprotection.

    PubMed

    Alok, Amit; Chaudhury, N K

    2016-02-01

    Radiation exposure in planned scenario necessarily requires radioprotector for protection against radiation injuries in tissues and organs. A large number of potential radioprotectors have been investigated but no approved radioprotector is available. Hence, in quest for radioprotector, repurposing of clinical drug is an approach which aims at finding the radioprotective potential of known drugs so that in case of untoward accident the knowledge could be translated to drug usage. In this study, we have investigated the radical scavenging properties of tetracycline pertaining to radioprotection. Our study suggests that tetracycline hydrochloride efficiently scavenges free radicals in ABTS (2,2'-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid), DPPH (2,2-diphenyl-1-picrylhydrazyl) and FRAP (ferric reducing antioxidant power) assays. Hydroxyl radical scavenging assay has demonstrated its ability to scavenge gamma radiation induced free radicals by lowering the formation of malondialdehyde. Radiation causes damage to macromolecules and hence the protection offered by tetracycline hydrochloride to DNA and protein shows its radioprotective potential. Plasmid DNA relaxation study with pBR322 has shown that tetracycline hydrochloride confers dose modification factor (DMF) of 2 and 4 at 100 μM and 250 μM concentration respectively. Tetracycline hydrochloride has also protected bovine serum albumin (BSA) from radiation induced degradation. The ex vivo studies for lipid peroxidation and mitochondrial membrane potential further substantiate our findings. The whole body animal survival study has shown the drug to offer 20% protection at a lethal radiation dose of 9 Gy. This study demonstrates the radioprotective potential of the drug by providing some insight into ex vivo and in vivo efficacy. PMID:26763761

  18. [D-Ala2,D-Leu5]-enkephalin hydrochloride.

    PubMed

    Deschamps, J R; George, C; Flippen-Anderson, J L

    1996-06-15

    The title compound, L-tyrosyl-D-alanyl-glycyl-L-phenyl-alanyl-D-leucine hydrochloride (C29H40N5O7+. Cl-), co-crystallizes with 2-butanone (C4H8O). The structure determination reveals a slightly distorted type I' beta-bend conformation stabilized by one intramolecular hydrogen bond. This conformation is similar to that observed for other [Leu]-enkephalin analogues. PMID:8766899

  19. A novel kind of TSV slurry with guanidine hydrochloride

    NASA Astrophysics Data System (ADS)

    Jiao, Hong; Yuling, Liu; Baoguo, Zhang; Xinhuan, Niu; Liying, Han

    2015-10-01

    The effect of a novel alkaline TSV (through-silicon-via) slurry with guanidine hydrochloride (GH) on CMP (chemical mechanical polishing) was investigated. The novel alkaline TSV slurry was free of any inhibitors. During the polishing process, the guanidine hydrochloride serves as an effective surface-complexing agent for TSV CMP applications, the removal rate of barrier (Ti) can be chemically controlled through tuned selectivity with respect to the removal rate of copper and dielectric, which is helpful to modifying the dishing and gaining an excellent topography performance in TSV manufacturing. In this paper, we mainly studied the working mechanism of the components of slurry and the skillful application guanidine hydrochloride in the TSV slurry. Project supported by the Major National Science and Technology Special Projects (No. 2009ZX02308), the Fund Project of Hebei Provincial Department of Education, China (No. QN2014208), the Natural Science Foundation of Hebei Province, China (No. E2013202247), and Colleges and Universities Scientific research project of Hebei Province, China (No. Z2014088).

  20. Kinetic spectrophotometric determination of tramadol hydrochloride in pharmaceutical formulation.

    PubMed

    Abdellatef, Hisham E

    2002-07-31

    Two simple and sensitive kinetic methods for the determination of tramadol hydrochloride are described. The first method is based upon a kinetic investigation of the oxidation reaction of the drug with alkaline potassium permanganate at room temperature for a fixed time at 20 min. The absorbance of the colored manganate ions was measured at 610 nm. The second method is based on the reaction of tramadol hydrochloride with 4-chloro-7-nitrobenzofurazan (NBD-Cl) in presence of 0.1 M sodium bicarbonate. The spectrophotometric measurements were recorded by measuring the absorbance at 467 nm, at fixed time at 25 min on thermostated water bath at 90+/-1 degrees C. All variables affecting the development of the colour have been investigated and the conditions were optimised. The absorbance concentration plots in both methods were rectilinear over the range 5-25 and 50-250 microg ml(-1), for the first and second methods, respectively. The two methods have been applied successfully to commercial capsule and ampoule dosage form. The results obtained are compared statistically with those given by the reference spectrophotometric method. The determination of tramadol hydrochloride by the fixed concentration and rate constant methods is feasible with the calibration equations obtained, but the fixed time method proves to be more applicable. PMID:12093516

  1. Synthesis, characterization and biological activities of Cu(II), Co(II), Mn(II), Fe(II), and UO2(VI) complexes with a new Schiff Base hydrazone: O-hydroxyacetophenone-7-chloro-4-quinoline hydrazone.

    PubMed

    Al-Shaalan, Nora H

    2011-01-01

    The Schiff base hydrazone ligand HL was prepared by the condensation reaction of 7-chloro-4-quinoline with o-hydroxyacetophenone. The ligand behaves either as monobasic bidentate or dibasic tridentate and contain ONN coordination sites. This was accounted for be the presence in the ligand of a phenolic azomethine and imine groups. It reacts with Cu(II), Ni(II), Co(II), Mn(II), UO(2) (VI) and Fe(II) to form either mono- or binuclear complexes. The ligand and its metal complexes were characterized by elemental analyses, IR, NMR, Mass, and UV-Visible spectra. The magnetic moments and electrical conductance of the complexes were also determined. The Co(II), Ni(II) and UO(2) (VI) complexes are mononuclear and coordinated to NO sites of two ligand molecules. The Cu(II) complex has a square-planar geometry distorted towards tetrahedral, the Ni(II) complex is octahedral while the UO(2) (VI) complex has its favoured heptacoordination. The Co(II), Mn(II) complexes and also other Ni(II) and Fe(III) complexes, which were obtained in the presence of Li(OH) as deprotonating agent, are binuclear and coordinated via the NNNO sites of two ligand molecules. All the binuclear complexes have octahedral geometries and their magnetic moments are quite low compared to the calculated value for two metal ions complexes and thus antiferromagnetic interactions between the two adjacent metal ions. The ligand HL and metal complexes were tested against a strain of Gram +ve bacteria (Staphylococcus aureus), Gram -ve bacteria (Escherichia coli), and fungi (Candida albicans). The tested compounds exhibited high antibacterial activities. PMID:21996717

  2. Development of a microfluidic paper-based analytical device for the determination of salivary aldehydes.

    PubMed

    Ramdzan, Adlin N; Almeida, M Inês G S; McCullough, Michael J; Kolev, Spas D

    2016-05-01

    A low cost, disposable and easy to use microfluidic paper-based analytical device (μPAD) was developed for simple and non-invasive determination of total aldehydes in saliva with a potential to be used in epidemiological studies to assess oral cancer risk. The μPAD is based on the colour reaction between aldehydes (e.g. acetaldehyde, formaldehyde), 3-methyl-2-benzothiazolinone hydrazone (MBTH) and iron(III) to form an intense blue coloured formazan dye. The newly developed μPAD has a 3D design with two overlapping paper layers. The first layer comprises 15 circular detection zones (8 mm in diameter), each impregnated with 8 μL of MBTH, while the second layer contains 15 reagent zones (4 mm in diameter). Two μL of iron(III) chloride are added to each one of the second layer zones after the addition of sample to the detection zones in the first layer. All hydrophilic zones of the μPAD are defined by wax printing using a commercial wax printer. Due to the 2-step nature of the analytical reaction, the two paper layers are separated by a cellulose acetate interleaving sheet to allow for the reaction between the aldehydes in the saliva sample with MBTH to proceed first with the formation of an azine, followed by a blue coloured reaction between the azine and the oxidized by iron(III) form of MBTH, produced after the removal of the interleaving sheet. After obtaining a high resolution image of the detection side zone of the device using a flatbed scanner, the intensity of the blue colour within each detection zone is measured with Image J software. Under optimal conditions, the μPAD is characterised by a working range of 20.4-114.0 μM, limit of detection of 6.1 μM, and repeatability, expressed as RSD, of less than 12.7% (n = 5). There is no statistically significant difference at the 95% confidence level between the results obtained by the μPAD and the reference method (Student's t-test: 0.090 < 0.38). The optimized μPAD is stable for more than 41 days

  3. Stability indicating methods for assay of mequitazine in presence of its degradate.

    PubMed

    El-Ragehy, N A; Badawey, A M; El Khateeb, S Z

    2002-06-20

    Six procedures have been suggested for the determination of the antihistaminic agent, mequitazine, in the presence of its degradate. Mequitazine, having a phenothiazine group, undergoes peroxide oxidation and the corresponding sulphone is produced. Its identity was confirmed by IR and MS. The first procedure is based on determination of mequitazine by HPLC with UV detection at 256 nm. The mobile phase used is acetonitrile, ortho phosphoric acid (50:50) using caffeine as an internal standard. Linearity range is 1.00-9.00 microg/ml. The second determination is a densitometric procedure based on the determination of mequitazine in the presence of its degradate at 256 nm using the mobile phase, chloroform:methanol:ammonia (50:18:3). Linearity range is 1.25-7.50 microg per spot. The third procedure is spectrophotometric, where a mixture of mequitazine and its degradate are resolved by first derivative ratio spectra. Linear calibration graphs of first derivative values at wavelengths 210.2, 247 and 259.8 nm are obtained. On carrying out measurements at the three mentioned wavelengths, the linearity range is found to be 1.00-10.00 microg/ml. The fourth procedure is based on first derivative spectrophotometry, where D(1) measurements are carried out at 290 nm. Linearity range is 1.00-10.00 microg/ml. The fifth procedure is based on the reaction of mequitazine with 3-methyl-2-benzothiazolinone hydrazone (MBTH) in the presence of ferric chloride. A stable violet colored oxidative coupling product is formed, which is measured spectrophotometrically at 685 nm. The optimum experimental parameters for the reaction have been studied and assigned. Linearity range is 1.00-16.00 microg/ml. The sixth procedure is based on the reaction of mequitazine in the presence of its degradate with 2,6-dichloroquinone-4-chloroimide (Gibbs reagent) in aqueous methanolic medium. The reddish-brown colored condensation product is measured at 405 nm. The optimum experimental conditions for the

  4. Torsionally Responsive C[subscript 3]-Symmetric Azo Dyes: Azo−Hydrazone Tautomerism, Conformational Switching, and Application for Chemical Sensing

    SciTech Connect

    Lee, Ho Yong; Song, Xinli; Park, Hyunsoo; Baik, Mu-Hyun; Lee, Dongwhan

    2010-12-07

    An efficient triple azo coupling reaction between anilines and phloroglucinol furnished a series of C{sub 3}-symmetric molecules 7-9 supporting multiple conjugation pathways that converge at the molecular core. A combination of {sup 1}H/{sup 13}C NMR spectroscopy, X-ray crystallography, and density functional theory computational studies provided a coherent picture of the [n,{pi}]-conjugated molecular core, which is best described as the tris(hydrazone) [rather than tris(azo)] tautomer stabilized by resonance-assisted hydrogen bonding. For a homologous series of compounds, an increase in the torsional angles between the planar molecular core and the peripheral aryl groups results in a systematic blue shift in the low-energy electronic transitions (7, 523 nm; 8, 505 nm; 9, 445 nm in CHCl{sub 3}) that qualitatively correlates with the shrinkage of effective conjugation through structural distortion. Similar spectral shifts could also be induced by amine substrates that interact with the intramolecular hydrogen-bonding network to trigger bond-twisting motions. Specifically, a brief exposure of a thin film of 7 to vapor samples of butyl-, hexyl-, diethyl-, and diisopropylamine resulted in a rapid and reversible color change from pink to dark-orange. Under similar conditions, however, triethylamine did not elicit any detectable color change, despite the fact that it has a significantly higher vapor pressure than n-hexylamine. These findings implicate that the hydrogen-bonding donor ability is a key requirement for the binding-induced conformational switching, which allows for direct naked-eye detection of volatile amines under ambient conditions.

  5. High-performance liquid chromatographic determination of memantine hydrochloride in rat plasma using sensitive fluorometric derivatization.

    PubMed

    Xie, Mei-Fen; Zhou, Wei; Tong, Xin-Yi; Chen, Yi-Le; Cai, Yi; Li, Yan; Duan, Geng-Li

    2011-02-01

    In this study, we investigated a simple, sensitive and reliable liquid chromatography-fluorescence detection method for the determination of memantine hydrochloride in rat plasma which was based on derivatization with 9-fluorenylmethyl chloroformate (FMOC-Cl). For the first time, FMOC-Cl was introduced into derivatization of memantine hydrochloride in rat plasma. The amino groups of memantine hydrochloride and amantadine hydrochloride (internal standard) were trapped with FMOC-Cl to form memantine hydrochloride-FMOC-Cl and amantadine hydrochloride-FMOC-Cl compositions, which can be very compatible for LC-FLD. Precipitation of plasma proteins by acetonitrile was followed by vortex mixing and centrifugation. Chromatographic separation was performed on a C(18) column (DIAMONSIL 150 × 4.6 mm, id 5 μm) with a mobile phase consisting of acetonitrile and water at a flow rate of 1.0 mL/min. The retention times of memantine hydrochloride-FMOC-Cl and amantadine hydrochloride-FMOC-Cl compositions were 23.69 and 40.27 min, respectively. Optimal conditions for the derivatization of memantine hydrochloride were also described. The limit of quantification (LOQ) was 25 ng/mL for memantine hydrochloride in plasma, the linear range was 0.025-5.0 μg/mL in plasma with a correlation coefficient (r) of 0.9999. The relative standard deviations (RSDs) of intra-day and inter-day assays were 4.46-12.19 and 5.23-11.50%, respectively. The validated method was successfully applied to the determination of memantine hydrochloride in rat plasma samples. PMID:21268245

  6. Interaction between lidocaine hydrochloride (with and without adrenaline) and various irrigants: A nuclear magnetic resonance analysis

    PubMed Central

    Vidhya, Nirmal; Karthikeyan, Balasubramanian Saravana; Velmurugan, Natanasabapathy; Abarajithan, Mohan; Nithyanandan, Sivasankaran

    2014-01-01

    Background: Interaction between local anesthetic solution, lidocaine hydrochloride (with and without adrenaline), and root canal irrigants such as sodium hypochlorite (NaOCl), ethylene diamine tetra-acetic acid (EDTA), and chlorhexidine (CHX) has not been studied earlier. Hence, the purpose of this in vitro study was to evaluate the chemical interaction between 2% lidocaine hydrochloride (with and without adrenaline) and commonly used root canal irrigants, NaOCl, EDTA, and CHX. Materials and Methods: Samples were divided into eight experimental groups: Group I-Lidocaine hydrochloride (with adrenaline)/3% NaOCl, Group II-Lidocaine hydrochloride (with adrenaline)/17% EDTA, Group III- Lidocaine hydrochloride (with adrenaline)/2% CHX, Group IV-Lidocaine hydrochloride (without adrenaline)/3% NaOCl, Group V-Lidocaine hydrochloride (without adrenaline)/17% EDTA, Group VI-Lidocaine hydrochloride (without adrenaline)/2% CHX, and two control groups: Group VII-Lidocaine hydrochloride (with adrenaline)/deionized water and Group VIII-Lidocaine hydrochloride (without adrenaline)/deionized water. The respective solutions of various groups were mixed in equal proportions (1 ml each) and observed for precipitate formation. Chemical composition of the formed precipitate was then analysed by nuclear magnetic resonance spectroscopy (NMR) and confirmed with diazotation test. Results: In groups I and IV, a white precipitate was observed in all the samples on mixing the respective solutions, which showed a color change to reddish brown after 15 minutes. This precipitate was then analysed by NMR spectroscopy and was observed to be 2,6-xylidine, a reported toxic compound. The experimental groups II, III, V, and VI and control groups VII and VIII showed no precipitate formation in any of the respective samples, until 2 hours. Conclusion: Interaction between lidocaine hydrochloride (with and without adrenaline) and NaOCl showed precipitate formation containing 2,6-xylidine, a toxic compound

  7. 21 CFR 524.1484d - Neomycin sulfate, hydrocortisone acetate, tetracaine hydrochloride ear ointment.

    Code of Federal Regulations, 2011 CFR

    2011-04-01

    ..., tetracaine hydrochloride ear ointment. 524.1484d Section 524.1484d Food and Drugs FOOD AND DRUG..., tetracaine hydrochloride ear ointment. (a) Specifications. The product contains 5 milligrams of neomycin... a lesser degree, chronic otitis externa in dogs and cats. In treatment of ear canker and...

  8. 21 CFR 524.1484d - Neomycin sulfate, hydrocortisone acetate, tetracaine hydrochloride ear ointment.

    Code of Federal Regulations, 2012 CFR

    2012-04-01

    ..., tetracaine hydrochloride ear ointment. 524.1484d Section 524.1484d Food and Drugs FOOD AND DRUG..., tetracaine hydrochloride ear ointment. (a) Specifications. The product contains 5 milligrams of neomycin... a lesser degree, chronic otitis externa in dogs and cats. In treatment of ear canker and...

  9. 21 CFR 524.1484d - Neomycin sulfate, hydrocortisone acetate, tetracaine hydrochloride ear ointment.

    Code of Federal Regulations, 2010 CFR

    2010-04-01

    ..., tetracaine hydrochloride ear ointment. 524.1484d Section 524.1484d Food and Drugs FOOD AND DRUG..., tetracaine hydrochloride ear ointment. (a) Specifications. The product contains 5 milligrams of neomycin... a lesser degree, chronic otitis externa in dogs and cats. In treatment of ear canker and...

  10. 21 CFR 524.1484d - Neomycin sulfate, hydrocortisone acetate, tetracaine hydrochloride ear ointment.

    Code of Federal Regulations, 2013 CFR

    2013-04-01

    ..., tetracaine hydrochloride ear ointment. 524.1484d Section 524.1484d Food and Drugs FOOD AND DRUG..., tetracaine hydrochloride ear ointment. (a) Specifications. The product contains 5 milligrams of neomycin... a lesser degree, chronic otitis externa in dogs and cats. In treatment of ear canker and...

  11. 40 CFR Appendix B to Subpart Nnn... - Free Formaldehyde Analysis of Insulation Resins by Hydroxylamine Hydrochloride

    Code of Federal Regulations, 2014 CFR

    2014-07-01

    ... Insulation Resins by Hydroxylamine Hydrochloride B Appendix B to Subpart NNN of Part 63 Protection of... NNN of Part 63—Free Formaldehyde Analysis of Insulation Resins by Hydroxylamine Hydrochloride 1. Scope... free-formaldehyde (FF) content such as insulation resins. It may also be suitable for other...

  12. Effects of metomindate hydrochloride and tricaine methanesulfonate on the short term cortisol response in channel catfish

    Technology Transfer Automated Retrieval System (TEKTRAN)

    The effects of metomidate hydrochloride and tricaine methanesulfonate (MS-222) on cortisol stress response of channel catfish, Ictalurus punctatus, were examined during 10 minutes of sedation. Channel catfish were assigned to three treatments: 1. Metomidate hydrochloride (12.5 mg/L), 2. MS-222 (100...

  13. 21 CFR 520.1263a - Lincomycin hydrochloride monohydrate tablets and sirup.

    Code of Federal Regulations, 2010 CFR

    2010-04-01

    ... 21 Food and Drugs 6 2010-04-01 2010-04-01 false Lincomycin hydrochloride monohydrate tablets and sirup. 520.1263a Section 520.1263a Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND... § 520.1263a Lincomycin hydrochloride monohydrate tablets and sirup. (a) Specifications. The...

  14. Adverse drug reaction to metoclopramide hydrochloride in a macaw with proventricular dilatation syndrome.

    PubMed

    Massey, J G

    1993-08-15

    A 4-year-old female blue and gold macaw (Ara ararauna) with a history of chronic vomiting was treated with metoclopramide hydrochloride. After the second treatment, ataxia, torticollis, and opisthotonos became evident. These signs resolved with the administration of diphenhydramine hydrochloride. Despite supportive care, the bird died several days later. Histologic lesions were suggestive of proventricular dilatation syndrome. PMID:8407511

  15. 77 FR 41411 - Determination That TOPOTECAN INJECTION (Topotecan Hydrochloride) 1 Milligram (Base)/1 Milliliter...

    Federal Register 2010, 2011, 2012, 2013, 2014

    2012-07-13

    ....g., 72 FR 9763, March 5, 2007; 61 FR 25497, May 21, 1996), the Agency has determined that, for... Hydrochloride) 1 Milligram (Base)/1 Milliliter, 3 Milligram (Base)/3 Milliliter, 4 Milligram (Base)/4 Milliliter... TOPOTECAN INJECTION (topotecan hydrochloride) 1 milligram (mg) (base)/1 milliliter (mL), 3 mg (base)/3 mL,...

  16. 21 CFR 520.1263a - Lincomycin hydrochloride monohydrate tablets and sirup.

    Code of Federal Regulations, 2013 CFR

    2013-04-01

    ... 21 Food and Drugs 6 2013-04-01 2013-04-01 false Lincomycin hydrochloride monohydrate tablets and sirup. 520.1263a Section 520.1263a Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND... § 520.1263a Lincomycin hydrochloride monohydrate tablets and sirup. (a) Specifications. The...

  17. 21 CFR 520.1263a - Lincomycin hydrochloride monohydrate tablets and sirup.

    Code of Federal Regulations, 2012 CFR

    2012-04-01

    ... 21 Food and Drugs 6 2012-04-01 2012-04-01 false Lincomycin hydrochloride monohydrate tablets and sirup. 520.1263a Section 520.1263a Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND... § 520.1263a Lincomycin hydrochloride monohydrate tablets and sirup. (a) Specifications. The...

  18. 21 CFR 520.1263a - Lincomycin hydrochloride monohydrate tablets and sirup.

    Code of Federal Regulations, 2011 CFR

    2011-04-01

    ... 21 Food and Drugs 6 2011-04-01 2011-04-01 false Lincomycin hydrochloride monohydrate tablets and sirup. 520.1263a Section 520.1263a Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND... § 520.1263a Lincomycin hydrochloride monohydrate tablets and sirup. (a) Specifications. The...

  19. 21 CFR 520.1263a - Lincomycin hydrochloride monohydrate tablets and sirup.

    Code of Federal Regulations, 2014 CFR

    2014-04-01

    ... 21 Food and Drugs 6 2014-04-01 2014-04-01 false Lincomycin hydrochloride monohydrate tablets and sirup. 520.1263a Section 520.1263a Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND... § 520.1263a Lincomycin hydrochloride monohydrate tablets and sirup. (a) Specifications. The...

  20. 21 CFR 524.1662 - Oxytetracycline hydrochloride ophthalmic and topical dosage forms.

    Code of Federal Regulations, 2010 CFR

    2010-04-01

    ... 21 Food and Drugs 6 2010-04-01 2010-04-01 false Oxytetracycline hydrochloride ophthalmic and topical dosage forms. 524.1662 Section 524.1662 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF... DOSAGE FORM NEW ANIMAL DRUGS § 524.1662 Oxytetracycline hydrochloride ophthalmic and topical dosage forms....

  1. 21 CFR 522.1662 - Oxytetracycline hydrochloride implantation or injectable dosage forms.

    Code of Federal Regulations, 2010 CFR

    2010-04-01

    ... 21 Food and Drugs 6 2010-04-01 2010-04-01 false Oxytetracycline hydrochloride implantation or injectable dosage forms. 522.1662 Section 522.1662 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF... INJECTABLE DOSAGE FORM NEW ANIMAL DRUGS § 522.1662 Oxytetracycline hydrochloride implantation or...

  2. 78 FR 2416 - Notice of Issuance of Final Determination Concerning Rybix® (Tramadol Hydrochloride) Tablets

    Federal Register 2010, 2011, 2012, 2013, 2014

    2013-01-11

    ... Border Protection (``CBP'') has issued a final determination concerning the country of origin of Rybix... determination that India is the country of origin of the Rybix (tramadol hydrochloride) tablets for purposes of... the country of origin of Rybix (tramadol hydrochloride) tablets, which may be offered to the...

  3. Polydopamine-based immobilization of a hydrazone covalent organic framework for headspace solid-phase microextraction of pyrethroids in vegetables and fruits.

    PubMed

    Wu, Mingxue; Chen, Gang; Liu, Ping; Zhou, Weihong; Jia, Qiong

    2016-07-22

    We designed a novel hydrazone covalent organic framework (COF) and developed a polydopamine (PDA) method to immobilize COF on a stainless steel fiber for headspace solid-phase microextraction (HS-SPME). A series of characterization studies was performed to validate the structure and property of the prepared fiber. The COF-PDA fiber was applied for the extraction of pyrethroids coupled with gas chromatography equipped with an electron capture detector (GC-ECD). Under the optimum experimental conditions, high enhancement factors of 307-2327 were achieved, indicating that the hydrazone COF possessed good extraction efficiency for pyrethroids. The detection limits ranged from 0.11 to 0.23μgkg(-1) with relative standard deviations varying in the range of 3.6-9.2% (intra-batch) and 6.9-12.1% (inter-batch), respectively. The developed method was applied to the determination of pyrethroids in fruit and vegetable samples and the accuracy was assessed through recovery experiments. PMID:27317006

  4. The Cu/ligand stoichiometry effect on the coordination behavior of aroyl hydrazone with copper(II): Structure, anticancer activity and anticancer mechanism.

    PubMed

    Deng, JunGang; Gou, Yi; Chen, Wei; Fu, Xiang; Deng, Hang

    2016-05-15

    In an effort to better understand the biological efficacy of the tridentate aroyl hydrazone Cu(II) complexes, three Cu(II) complexes of acetylpyridine benzoyl hydrazone (HL), [Cu(L)(NO3) (H2O)]·H2O (C1), [Cu(L)2] (C2) and [Cu(L)(HL)]·(NO3)(Sas) (C3) (Sas=salicylic acid) were synthesized and characterized. X-ray crystal structures and infrared (IR) spectra of the complexes reveal that the L(-) ligand of C1 and C2 are predominantly in the enolate resonance form, while one L(-) ligand in C3 is represented enolate resonance form and the other HL ligand exhibits keto resonance form. All Cu(II) complexes showed significantly more anticancer activity than the ligand alone. Interestingly, the Cu complexes where the ligand/metal ratio was 1:1 (C1) rather than 2:1 (C2 and C3) had higher antitumor efficacy. Moreover, the 1:1 Cu/ligand complex, C1, promotes A549 cell apoptosis possibly through the intrinsic reactive oxygen species (ROS) mediated mitochondrial pathway, accompanied by the regulation of Bcl-2 family proteins. PMID:27056799

  5. Investigation of the azo-hydrazone tautomeric equilibrium in an azo dye involving the naphthalene moiety by UV-vis spectroscopy and quantum chemistry

    NASA Astrophysics Data System (ADS)

    Ünal, Arslan; Eren, Bilge; Eren, Erdal

    2013-10-01

    Photophysical properties of the azo-hydrazone tautomerism of Eriochrome Blue Black B (1-(1-hydroxy-2-naphthylazo)-2-naphthol-4-sulphonic acid) in DMF, MeCN and water were investigated using UV-visible spectroscopy and quantum chemical calculations. The optimized molecular structure parameters, relative energies, mole fractions, electronic absorption spectra and HOMO-LUMO energies for possible stable tautomeric forms of EBB were theoretically calculated by using hybrid density functional theory, (B3LYP) methods with 6-31G(d) basis set level and polarizable continuum model (PCM) for solvation effect. The effects of varying pH-, dye concentration-, solvent-, temperature-, and time-dependences on the UV-vis spectra of Eriochrome Blue Black B were also investigated experimentally. The calculations showed that the dye exhibited acid-base, azo-hydrazone and aggregate equilibria in DMF solution, while the most probably preferred form in MeCN solution was azo form. Thermodynamic parameters of dimerization reaction in DMF solution proved that entropy was the driving force of this reaction.

  6. Probing the Interaction between Acotiamide Hydrochloride and Pepsin by Multispectral Methods, Electrochemical Measurements, and Docking Studies.

    PubMed

    He, Jiawei; Ma, Xianglin; Wang, Qing; Huang, Yanmei; Li, Hui

    2016-07-01

    The interaction between acotiamide hydrochloride and pepsin was systematically characterized by fluorescence and electrochemical approaches. Fluorescence lifetime measurements showed that acotiamide hydrochloride quenched the intrinsic fluorescence of pepsin with a new complex formation via static mode, which was reconfirmed by cyclic voltammetry results. Both of the binding number and binding constants were calculated from differential pulse voltammetry analysis and fluorescence spectroscopy. The values obtained from the above two methods displayed a relatively high degree of consistency. Thermodynamic parameters suggested that acotiamide hydrochloride interacted with pepsin spontaneously by hydrogen bonding and van der Waals interactions. These results were consistent with the results obtained from molecular docking analysis. As revealed by synchronous fluorescence, three-dimensional fluorescence, Fourier transform infrared spectrometry, and circular dichroism spectra, acotiamide hydrochloride could affect the microenvironment and slightly change the secondary structure of pepsin. Furthermore, acotiamide hydrochloride can inhibit pepsin activity in vitro, as explained by the molecular docking. PMID:27018070

  7. Neuroprotection against vascular dementia after acupuncture combined with donepezil hydrochloride: P300 event related potential

    PubMed Central

    Liu, Qiang; Wang, Xiu-juan; Zhang, Zhe-cheng; Xue, Rong; Li, Ping; Li, Bo

    2016-01-01

    Acupuncture can be used to treat various nervous system diseases. Here, 168 vascular dementia patients were orally administered donepezil hydrochloride alone (5 mg/day, once a day for 56 days), or combined with acupuncture at Shenting (DU24), Tianzhu (BL10), Sishencong (Extra), Yintang (Extra), Renzhong (DU26), Neiguan (PC6), Shenmen (HT7), Fengchi (GB20), Wangu (GB12) and Baihui (DU20) (once a day for 56 days). Compared with donepezil hydrochloride alone, P300 event related potential latency was shorter with an increased amplitude in patients treated with donepezil hydrochloride and acupuncture. Mini-Mental State Examination score was also higher. Moreover, these differences in P300 latency were identified within different infarcted regions in patients treated with donepezil hydrochloride and acupuncture. These findings indicate that acupuncture combined with donepezil hydrochloride noticeably improves cognitive function in patients with vascular dementia, and exerts neuroprotective effects against vascular dementia. PMID:27127486

  8. Chitosan coated vancomycin hydrochloride liposomes: Characterizations and evaluation.

    PubMed

    Yang, Zhenlei; Liu, Junli; Gao, Jinhua; Chen, Shilei; Huang, Guihua

    2015-11-10

    The present work evaluated the feasibility of chitosan coated liposomes (c-Lips) for the intravenous delivery of vancomycin hydrochloride (VANH), a water-soluble antibiotic for the treatment of gram-positive bacterial infections like osteomyelitis, arthritis, endocarditis, pneumonia, etc. The objective of this research was to develop a suitable drug delivery system in vivo which could improve therapeutic efficacy and decrease side effects especially nephrotoxicity. Firstly, the vancomycin hydrochloride liposomes (VANH-Lips) were prepared by modified reverse phase evaporation method, then the chitosan wrapped vancomycin hydrochloride liposomes (c-VANH-Lips) nanosuspension was formulated by the method of electrostatic deposition. Based on the optimized results of single-factor screening experiment, the c-VANH-Lips were found to be relatively uniform in size (220.40 ± 3.56 nm) with a narrow polydispersity index (PI) (0.21 ± 0.03) and a positive zeta potential (25.7 ± 1.12 mV). The average drug entrapment efficiency (EE) and drug loading (DL) were 32.65 ± 0.59% and 2.18 ± 0.04%, respectively. The in vitro release profile of c-VANH-Lips possessed a sustained release Characterization and the release behavior was in accordance with the Weibull equation. Hemolysis experiments showed that its intravenous injection had preliminary safety. In vivo, after intravenous injection to mice, c-VANH-Lips showed a longer retention time and higher AUC values compared with the VANH injection (VANH-Inj) and VANH-Lips. In addition, biodistribution results clearly demonstrated that c-VANH-Lips preferentially decreased the drug distribution in kidney of mice after intravenous injection. These results revealed that injectable c-VANH-Lips may serve as a promising carrier for VANH to increase therapeutic efficacy on gram-positive bacterial infections and reduce nephrotoxicity, which provides significantly clinical value for long-term use of VANH. PMID:26325316

  9. Analgesic oral efficacy of tramadol hydrochloride in postoperative pain.

    PubMed

    Sunshine, A; Olson, N Z; Zighelboim, I; DeCastro, A; Minn, F L

    1992-06-01

    Tramadol hydrochloride is a synthetic opiate agonist with a plasma elimination half-life of 5 to 6 hours and peak plasma levels at about 1 1/2 hours. It derives its activity from attachment to the mu-receptor and blockage of norepinephrine reuptake. The purpose of this single-dose, double-blind, placebo-controlled study was to determine the analgesic effectiveness of an oral administration of two dose levels of tramadol hydrochloride (75 or 150 mg) compared with the combination of 650 mg acetaminophen plus 100 mg propoxyphene napsylate in 161 patients with severe postoperative pain after cesarean section. Analgesia was assessed over a 6-hour period. Treatments were compared on the basis of standard scales for pain intensity and relief and a number of derived variables based on these data. A global rating of the study medication was also used to compare treatments. The three active treatments were effective analgesics, statistically superior to placebo for many hourly and summary measures. A dose response was seen between the two tramadol doses, with the 150 mg dose providing significantly greater analgesia over the lower dose. The 75 mg dose of tramadol was generally more effective than the acetaminophen-propoxyphene combination after hour 2, and significantly so for some hourly time points, as well as for the global rating of the medication. The 150 mg dose of tramadol was significantly more effective than the acetaminophen-propoxyphene combination from hour 2 through hour 6 for the sum of pain intensity differences and total pain relief scores, as well as for the global rating of the medication. Tramadol hydrochloride at both dose levels is an effective analgesic agent and at 150 mg is statistically superior to the acetaminophen-propoxyphene combination. No serious adverse effects were observed; however, dizziness was more frequently reported with 150 mg tramadol. PMID:1351804

  10. The effects of Dalmane /flurazepam hydrochloride/ on human EEG characteristics.

    NASA Technical Reports Server (NTRS)

    Frost, J. D., Jr.; Carrie, J. R. G.; Borda, R. P.; Kellaway, P.

    1973-01-01

    Evaluation of the changes in the waking EEGs of six healthy male subjects who received 30 mg daily oral doses of flurazepam hydrochloride for two weeks. A placebo was then substituted for flurazepam for another two weeks. An increase in beta activity with a maximum in fronto-central leads was observed during the test period. A small increase in the mean wavelength of the alpha and theta activities in the central-occipital derivations was also apparent in the subjects during the period.

  11. Kinetics membrane disruption due to drug interactions of chlorpromazine hydrochloride.

    PubMed

    Nussio, Matthew R; Sykes, Matthew J; Miners, John O; Shapter, Joseph G

    2009-01-20

    Drug-membrane interactions assume considerable importance in pharmacokinetics and drug metabolism. Here, we present the interaction of chlorpromazine hydrochloride (CPZ) with supported phospholipid bilayers. It was demonstrated that CPZ binds rapidly to phospholipid bilayers, disturbing the molecular ordering of the phospholipids. These interactions were observed to follow first order kinetics, with an activation energy of approximately 420 kJ mol(-1). Time-dependent membrane disruption was also observed for the interaction with CPZ, such that holes appeared in the phospholipid bilayer after the interaction of CPZ. For this process of membrane disruption, "lag-burst" kinetics was demonstrated. PMID:19093750

  12. Application of direct crystallization for racemic compound propranolol hydrochloride.

    PubMed

    Wang, Xiujuan; Lu, Jie; Ching, Chi Bun

    2007-10-01

    The application of direct crystallization integrating with chromatography to the resolution of a racemic compound propranolol hydrochloride was studied and the crystallization progression was clearly illustrated in terms of the diagram of solubility and metastable zone widths with different enantiomeric compositions. The solubility and metastable zone widths of propranolol hydrochloride in the mixture of methanol and isopropanol were determined using an in situ Lasentec Focused Beam Reflectance Measurement (FBRM) probe. The direct crystallizations were carried out in an automatic lab reactor (Mettler Toledo LabMax) system. The optical purity of final product crystals was examined using differential scanning calorimetry (DSC), HPLC and PXRD. The crystal size distribution and morphology were analyzed using Malvern Mastersizer and Jeol SEM. It was found that optically pure crystal product could be obtained within certain safe supersaturation limit and there was no evidence of polymorph or solvate/hydrate transformation during the crystallization process. There was no selectivity of crystal growth or nucleation between the pure enantiomer and its racemate when the solution reaches the temperature lower than saturation temperature of the racemate. Hence, the critical supersaturation control of a solution was essential to obtain pure enantiomers from a partially resolved racemate. PMID:17549769

  13. The antipyretic effect of tilorone hydrochloride in the cat.

    PubMed Central

    Clark, W G; Robins, J A

    1978-01-01

    1 The antipyretic activity of tilorone hydrochloride was studied in conscious, unrestrained cats provided with implanted jugular venous catheters, third cerebral ventricular (i.c.v.) cannulae and retroperitoneal thermocouples. 2 In afebrile animals, 10 mg/kg i.v. or 1 mg i.c.v. tilorone hydrochloride did not alter body temperature, but 20 mg/kg i.v. or 2 to 5 mg i.c.v. caused hypothermia and various behavioural responses. 3 Non-hypothermogenic doses of tilorone (i.v. or i.c.v.) antagonized hyperthermic responses to leucocytic pyrogen (i.v. or i.c.v.), bacterial pyrogen (i.c.v.) and sodium arachidonate (i.c.v.) but did not antagonize prostaglandin E1 (i.c.v.). 4 These results indicate that tilorone has an antipyretic action within the central nervous system that is distinct from its hypothermogenic action. Although there is no published evidence to indicate that tilorone can inhibit prostaglandin synthesis peripherally, its ability to reduce hyperthermic responses to arachidonate suggests that it can inhibit prostaglandin synthesis within the brain. PMID:304749

  14. Intestinal Anisakiasis Treated Successfully with Prednisolone and Olopatadine Hydrochloride

    PubMed Central

    Toyoda, Hideki; Tanaka, Kyosuke

    2016-01-01

    The clinical characteristic of gastrointestinal anisakiasis is severe abdominal pain after eating raw fish. Intestinal anisakiasis is more uncommon than gastric anisakiasis. Most patients with intestinal anisakiasis need hospitalization because anisakiasis can cause intestinal obstruction, ileus, peritonitis or intestinal perforation. We report a case of intestinal anisakiasis. A 43-year-old woman presented with symptoms of intermittent abdominal pain 2 days after eating raw fish. Her brother had eaten the same food and had been suffering from gastric anisakiasis. Abdominal ultrasonography in this patient showed localized jejunal wall thickening with dilated lumen of proximal jejunum and ascites. According to the clinical course and examinations, she was diagnosed with intestinal anisakiasis. Administration of prednisolone 5 mg/day and olopatadine hydrochloride 10 mg/day improved her symptoms quickly without hospitalization. Prednisolone was administered for 10 days, and olopatadine hydrochloride was administered for a total of 6 weeks according to ultrasonographic findings. Six months after the treatment, the abdominal ultrasonography demonstrated normal findings. This case demonstrates that ultrasonography was quite useful for the diagnosis and surveillance of intestinal anisakiasis. Furthermore, treatment with corticosteroid and an antiallergic agent could be an option for patients with intestinal anisakiasis. PMID:27403099

  15. Modulation of Venlafaxine Hydrochloride Release from Press Coated Matrix Tablet

    PubMed Central

    Gohel, M. C.; Soni, C. D.; Nagori, S. A.; Sarvaiya, K. G.

    2008-01-01

    The aim of present study was to prepare novel modified release press coated tablets of venlafaxine hydrochloride. Hydroxypropylmethylcellulose K4M and hydroxypropylmethylcellulose K100M were used as release modifier in core and coat, respectively. A 32 full factorial design was adopted in the optimization study. The drug to polymer ratio in core and coat were chosen as independent variables. The drug release in the first hour and drug release rate between 1 and 12 h were chosen as dependent variables. The tablets were characterized for dimension analysis, crushing strength, friability and in vitro drug release. A check point batch, containing 1:2.6 and 1:5.4 drug to polymer in core and coat respectively, was prepared. The tablets of check point batch were subjected to in vitro drug release in dissolution media with pH 5, 7.2 and distilled water. The kinetics of drug release was best explained by Korsmeyer and Peppas model (anomalous non-Fickian diffusion). The systematic formulation approach enabled us to develop modified release venlafaxine hydrochloride tablets. PMID:20046735

  16. [Examination of effectiveness of olopatadine hydrochloride in atopic dermatitis].

    PubMed

    Shimizu, Tadamichi; Mashiko, Maki; Shimizu, Hiroshi

    2005-02-01

    Subjective/objective symptoms (itching, papula, erythema, lichenification, desquamation, scratching, erosion) and the levels of IgE, LDH, interleukin (IL) -6, thymus and activation-regulated chemokine (TARC) were compared before and after administering olopatadine hydrochloride (ALLELOCK tablets) to 17 atopic dermatitis (AD) patients. Subject/objective symptoms improved significantly after administering the agent, and the total dosage of the combined topical steroids was also significantly decreased after administration (p<0.05), although IgE, IL-6 and LDH levels did not change, TARC was significantly decreased (p<0.05). The correlation between the levels of IgE, IL-6, LDH and TARC before and after the administration was examined. There was a positive correlation between IgE and TARC (r=0.62, p<0.01) and between IL-6 and TARC (r=0.78, p<0.01). Olopatadine hydrochloride is therefore useful in improving the symptoms in AD, and TARC may be used as an indicator of the symptom improvement. PMID:15864020

  17. Butenafine hydrochloride: for the treatment of interdigital tinea pedis.

    PubMed

    Syed, T A; Maibach, H I

    2000-03-01

    Butenafine, a derivative of benzylamine with potent fungicidal activity is a new generation of antimycotic compound that has shown to be extremely effective against experimentally-induced tinea pedis in the guinea-pig, a situation that resembles synergetic pathology similar to that of tinea pedis in humans. Butenafine, (N-4-tert-butylbenzyl-N-methyl-1-naphthalenemethyl-amine hydrochloride) with a chemical structure and mode of action similar to those of the allylamines, demonstrates superior fungicidal activity in vitro against dermatophytes and superior fungistatic activity toward Candida albicans that of naftifine and terbinafine. In vitro, pharmacodynamic data has shown that the geometric mean of minimum inhibitory concentration values for butenafine were comparatively lower than those of naftifine and clotrimazole against clinical isolates for many dermatophytes. It inhibits sterol synthesis by blocking the squalene epoxidation stage in fungi. In phramacokinetic assessments butenafine achieves and maintains high concentrations and long retention time in skin, with associated anti-inflammatory activity in vivo. In controlled clinical trials when applied topically, butenafine appears to be well tolerated with a subjective mild burning sensation at the application site. There were no withdrawals from the study. Butenafine is sparingly soluble in water but readily soluble in methanol, ethanol, dichloromethane and chloroform. If incorporated properly in semisolid topical preparations, with a balanced vehicle, butenafine hydrochloride potentially exhibits as a promising alternative antimycotic agent for the treatment of tinea pedis. PMID:11249531

  18. Intestinal Anisakiasis Treated Successfully with Prednisolone and Olopatadine Hydrochloride.

    PubMed

    Toyoda, Hideki; Tanaka, Kyosuke

    2016-01-01

    The clinical characteristic of gastrointestinal anisakiasis is severe abdominal pain after eating raw fish. Intestinal anisakiasis is more uncommon than gastric anisakiasis. Most patients with intestinal anisakiasis need hospitalization because anisakiasis can cause intestinal obstruction, ileus, peritonitis or intestinal perforation. We report a case of intestinal anisakiasis. A 43-year-old woman presented with symptoms of intermittent abdominal pain 2 days after eating raw fish. Her brother had eaten the same food and had been suffering from gastric anisakiasis. Abdominal ultrasonography in this patient showed localized jejunal wall thickening with dilated lumen of proximal jejunum and ascites. According to the clinical course and examinations, she was diagnosed with intestinal anisakiasis. Administration of prednisolone 5 mg/day and olopatadine hydrochloride 10 mg/day improved her symptoms quickly without hospitalization. Prednisolone was administered for 10 days, and olopatadine hydrochloride was administered for a total of 6 weeks according to ultrasonographic findings. Six months after the treatment, the abdominal ultrasonography demonstrated normal findings. This case demonstrates that ultrasonography was quite useful for the diagnosis and surveillance of intestinal anisakiasis. Furthermore, treatment with corticosteroid and an antiallergic agent could be an option for patients with intestinal anisakiasis. PMID:27403099

  19. [Spectroscopic studies on the binding of phenazopyridine hydrochloride and bovine serum albumin].

    PubMed

    Zhou, Hong; Chen, Chang-Yun; Xie, An-Jian

    2007-09-01

    The binding of phenazopyridine hydrochloride and bovine serum albumin under physiological conditions was studied by spectroscopic method. The quenching mechanism of the fluorescence of bovine serum albumin by phenazopyridine hydrochloride was studied with fluorescence and absorption spectroscopy. The binding constant Kb and the number of binding sites n were determined at different temperatures according to Scatchard equation, and the main binding force was discussed by thermodynamic equations. The effect of the drug on bovine serum albumin conformation was also studied by using synchronous fluorescence spectroscopy. The quenching mechanism of phenazopyridine hydrochloride to bovine serum albumin is static quenching and non-radiation energy transfer. The binding constants Kb at 15, 25 and 37 degrees C are 2.47 x 10(7), 9.15 x 10(6) and 4.36 x 10(6) mol(-1) with one binding site, respectively. The thermodynamic parameters of the reaction are DeltaH = -71.2 kJ x mol(-1), and DeltaS = 124.8 J x mol(-1) x K(-1). Binding phenazopyridine hydrochloride to bovine serum albumin is a spontaneous inter-molecular interaction in which entropy increases and Gibbs free energy decreases. The binding distance r between phenazopyridine hydrochloride and bovine serum albumin is 1.61 nm according to Forster theory of non-radiation energy transfer. The binding force is electrostatic interaction. Phenazopyridine hydrochloride can be deposited and transported by serum protein in vivo. Phenazopyridine hydrochloride does affect the serum protein conformation. PMID:18051539

  20. Extractive determination of ephedrine hydrochloride and bromhexine hydrochloride in pure solutions, pharmaceutical dosage form and urine samples.

    PubMed

    Abdel-Ghani, N T; Rizk, M S; Mostafa, M

    2013-07-01

    Simple, rapid, sensitive, precise and accurate spectrophotometeric methods for the determination of ephedrine hydrochloride (E-HCl) and bromhexine hydrochloride (Br-HCl) in bulk samples, dosage form and in spiked urine samples were investigated. The methods are based on the formation of a yellow colored ion-associates due to the interaction between the examined drugs with picric acid (PA), chlorophyllin coppered trisodium salt (CLPH), alizarin red (AR) and ammonium reineckate (Rk) reagents. A buffer solution had been used and the extraction was carried out using organic solvent, the ion associates exhibit absorption maxima at 410, 410, 430 and 530 nm of (Br-HCl)with PA, CLPH, AR and Rk respectively; 410, 410, 435 and 530 of (E-HCl) with PA, CLPH, AR and Rk respectively. (E-HCl) and (Br-HCl) could be determined up to 13, 121, 120 and 160; 25, 200, 92 and 206 μg mL(-1), using PA, CLPH, AR and Rk respectively. The optimum reaction conditions for quantitative analysis were investigated. In addition, the molar absorptivity, Sandell sensitivity were determined for the investigated drug. The correlation coefficient was ≥0.995 (n=6) with a relative standard deviation (RSD) ≤1.15 for five selected concentrations of the reagents. Therefore the concentration of Br-HCl and E-HCl drugs in their pharmaceutical formulations and spiked urine samples had been determined successfully. PMID:23624039

  1. Reagents for astatination of biomolecules. 5. Evaluation of hydrazone linkers in (211)At- and (125)I-labeled closo-decaborate(2-) conjugates of Fab' as a means of decreasing kidney retention.

    PubMed

    Wilbur, D Scott; Chyan, Ming-Kuan; Hamlin, Donald K; Nguyen, Holly; Vessella, Robert L

    2011-06-15

    Evaluation of monoclonal antibody (mAb) fragments (e.g., Fab', Fab, or engineered fragments) as cancer-targeting reagents for therapy with the α-particle emitting radionuclide astatine-211 ((211)At) has been hampered by low in vivo stability of the label and a propensity of these proteins localize to kidneys. Fortunately, our group has shown that the low stability of the (211)At label, generally a meta- or para-[(211)At]astatobenzoyl conjugate, on mAb Fab' fragments can be dramatically improved by the use of closo-decaborate(2-) conjugates. However, the higher stability of radiolabeled mAb Fab' conjugates appears to result in retention of radioactivity in the kidneys. This investigation was conducted to evaluate whether the retention of radioactivity in kidney might be decreased by the use of an acid-cleavable hydrazone between the Fab' and the radiolabeled closo-decaborate(2-) moiety. Five conjugation reagents containing sulfhydryl-reactive maleimide groups, a hydrazone functionality, and a closo-decaborate(2-) moiety were prepared. In four of the five conjugation reagents, a discrete poly(ethylene glycol) (PEG) linker was used, and one substituent adjacent to the hydrazone was varied (phenyl, benzoate, anisole, or methyl) to provide varying acid sensitivity. In the initial studies, the five maleimido-closo-decaborate(2-) conjugation reagents were radioiodinated ((125)I or (131)I), then conjugated with an anti-PSMA Fab' (107-1A4 Fab'). Biodistributions of the five radioiodinated Fab' conjugates were obtained in nude mice at 1, 4, and 24 h post injection (pi). In contrast to closo-decaborate(2-) conjugated to 107-1A4 Fab' through a noncleavable linker, two conjugates containing either a benzoate or a methyl substituent on the hydrazone functionality displayed clearance rates from kidney, liver, and spleen that were similar to those obtained with directly radioiodinated Fab' (i.e., no conjugate). The maleimido-closo-decaborate(2-) conjugation reagent containing a

  2. A highly selective turn-on fluorescent probe for hypochlorous acid based on hypochlorous acid-induced oxidative intramolecular cyclization of boron dipyrromethene-hydrazone.

    PubMed

    Chen, Wei-Chieh; Venkatesan, Parthiban; Wu, Shu-Pao

    2015-07-01

    A BODIPY-based fluorescent probe, HBP, was developed for the detection of hypochlorous acid based on the specific hypochlorous acid-promoted oxidative intramolecular cyclization of heterocyclic hydrazone in response to the amount of HOCl. The reaction is accompanied by a 41-fold increase in the fluorescent quantum yield (from 0.004 to 0.164). The fluorescence intensity of the reaction between HOCl and HBP is linear in the HOCl concentration range of 1-8 μM with a detection limit of 2.4 nM (S/N=3). Confocal fluorescence microscopy imaging using RAW264.7 cells showed that the new probe HBP could be used as an effective fluorescent probe for detecting HOCl in living cells. PMID:26043093

  3. An efficient PEGylated liposomal nanocarrier containing cell-penetrating peptide and pH-sensitive hydrazone bond for enhancing tumor-targeted drug delivery.

    PubMed

    Ding, Yuan; Sun, Dan; Wang, Gui-Ling; Yang, Hong-Ge; Xu, Hai-Feng; Chen, Jian-Hua; Xie, Ying; Wang, Zhi-Qiang

    2015-01-01

    Cell-penetrating peptides (CPPs) as small molecular transporters with abilities of cell penetrating, internalization, and endosomal escape have potential prospect in drug delivery systems. However, a bottleneck hampering their application is the poor specificity for cells. By utilizing the function of hydration shell of polyethylene glycol (PEG) and acid sensitivity of hydrazone bond, we constructed a kind of CPP-modified pH-sensitive PEGylated liposomes (CPPL) to improve the selectivity of these peptides for tumor targeting. In CPPL, CPP was directly attached to liposome surfaces via coupling with stearate (STR) to avoid the hindrance of PEG as a linker on the penetrating efficiency of CPP. A PEG derivative by conjugating PEG with STR via acid-degradable hydrazone bond (PEG2000-Hz-STR, PHS) was synthesized. High-performance liquid chromatography and flow cytometry demonstrated that PHS was stable at normal neutral conditions and PEG could be completely cleaved from liposome surface to expose CPP under acidic environments in tumor. An optimal CPP density on liposomes was screened to guaranty a maximum targeting efficiency on tumor cells as well as not being captured by normal cells that consequently lead to a long circulation in blood. In vitro and in vivo studies indicated, in 4 mol% CPP of lipid modified system, that CPP exerted higher efficiency on internalizing the liposomes into targeted subcellular compartments while remaining inactive and free from opsonins at a maximum extent in systemic circulation. The 4% CPPL as a drug delivery system will have great potential in the clinical application of anticancer drugs in future. PMID:26491292

  4. Synthesis, biological evaluation, drug-likeness, and in silico screening of novel benzylidene-hydrazone analogues as small molecule anticancer agents.

    PubMed

    Alam, Mohammad Sayed; Lee, Dong-Ung

    2016-02-01

    A series of fifteen benzylidene-hydrazone analogues (3a-o), including eight new compounds, were synthesized and evaluated for their cytotoxic activities in four human cancer cell lines and for their antioxidant activities using DPPH. Of the tested compounds 3e, which possesses two methoxy substituents in its benzylidene phenyl ring, was found to be potently cytotoxic to all cancer cell lines tested with IC50 values of 0.12 (lung), 0.024 (ovarian), 0.097 (melanoma), and 0.05 μM (colon), and these IC50 values were comparable to those of the doxorubicin standard (IC50 = 0.021, 0.074, 0.001, and 0.872 μM, respectively). DPPH assay showed compounds 3f, 3i, and 3g had IC50 values of 0.60, 0.99, and 1.30 μM, respectively, which were comparable to that of ascorbic acid (IC50 = 0.87 μM). Computational parameters such as, drug-likeness, ADME properties, toxicity effects, and drug scores were evaluated, and none of the fifteen compounds violated Lipinski's rule of five or Veber's rule, and thus they demonstrated good drug-likeness properties. In addition, all fifteen compounds had a higher drug score than the doxorubicin and BIBR1532. In silico screening was also conducted by docking of the active compounds on the active site of telomerase reverse transcriptase catalytic subunit, an important therapeutic target of anticancer agents, to determine the probable binding properties. The total binding energies of docked compounds are correlated well with cytotoxic potencies (pIC50) against lung, ovarian, melanoma, and colon cancer cell lines indicating that the benzylidene-hydrazones could use for the development of new anticancer agents as a telomerase inhibitor. PMID:26694484

  5. An efficient PEGylated liposomal nanocarrier containing cell-penetrating peptide and pH-sensitive hydrazone bond for enhancing tumor-targeted drug delivery

    PubMed Central

    Ding, Yuan; Sun, Dan; Wang, Gui-Ling; Yang, Hong-Ge; Xu, Hai-Feng; Chen, Jian-Hua; Xie, Ying; Wang, Zhi-Qiang

    2015-01-01

    Cell-penetrating peptides (CPPs) as small molecular transporters with abilities of cell penetrating, internalization, and endosomal escape have potential prospect in drug delivery systems. However, a bottleneck hampering their application is the poor specificity for cells. By utilizing the function of hydration shell of polyethylene glycol (PEG) and acid sensitivity of hydrazone bond, we constructed a kind of CPP-modified pH-sensitive PEGylated liposomes (CPPL) to improve the selectivity of these peptides for tumor targeting. In CPPL, CPP was directly attached to liposome surfaces via coupling with stearate (STR) to avoid the hindrance of PEG as a linker on the penetrating efficiency of CPP. A PEG derivative by conjugating PEG with STR via acid-degradable hydrazone bond (PEG2000-Hz-STR, PHS) was synthesized. High-performance liquid chromatography and flow cytometry demonstrated that PHS was stable at normal neutral conditions and PEG could be completely cleaved from liposome surface to expose CPP under acidic environments in tumor. An optimal CPP density on liposomes was screened to guaranty a maximum targeting efficiency on tumor cells as well as not being captured by normal cells that consequently lead to a long circulation in blood. In vitro and in vivo studies indicated, in 4 mol% CPP of lipid modified system, that CPP exerted higher efficiency on internalizing the liposomes into targeted subcellular compartments while remaining inactive and free from opsonins at a maximum extent in systemic circulation. The 4% CPPL as a drug delivery system will have great potential in the clinical application of anticancer drugs in future. PMID:26491292

  6. An Eco-Friendly Ultrasound-Assisted Synthesis of Novel Fluorinated Pyridinium Salts-Based Hydrazones and Antimicrobial and Antitumor Screening

    PubMed Central

    Rezki, Nadjet; Al-Sodies, Salsabeel A.; Aouad, Mohamed R.; Bardaweel, Sanaa; Messali, Mouslim; El Ashry, El Sayed H.

    2016-01-01

    The present work reports an efficient synthesis of fluorinated pyridinium salts-based hydrazones under both conventional and eco-friendly ultrasound procedures. The synthetic approach first involves the preparation of halogenated pyridinium salts through the condensation of isonicotinic acid hydrazide (1) with p-fluorobenzaldehyde (2) followed by the nucleophilic alkylation of the resulting N-(4-fluorobenzylidene)isonicotinohydrazide (3) with a different alkyl iodide. The iodide counteranion of 5–10 was subjected to an anion exchange metathesis reaction in the presence of an excess of the appropriate metal salts to afford a new series of fluorinated pyridinium salts tethering a hydrazone linkage 11–40. Ultrasound irradiation led to higher yields in considerably less time than the conventional methods. The newly synthesized ILs were well-characterized with FT-IR, 1H NMR, 13C NMR, 11B, 19F, 31P and mass spectral analyses. The ILs were also screened for their antimicrobial and antitumor activities. Within the series, the salts tethering fluorinated counter anions 11–13, 21–23, 31–33 and 36–38 were found to be more potent against all bacterial and fungal strains at MIC 4–8 µg/mL. The in vitro antiproliferative activity was also investigated against four tumor cell lines (human ductal breast epithelial tumor T47D, human breast adenocarcinoma MCF-7, human epithelial carcinoma HeLa and human epithelial colorectal adenocarcinoma Caco-2) using the MTT assay, which revealed that promising antitumor activity was exhibited by compounds 5, 12 and 14. PMID:27213367

  7. An Eco-Friendly Ultrasound-Assisted Synthesis of Novel Fluorinated Pyridinium Salts-Based Hydrazones and Antimicrobial and Antitumor Screening.

    PubMed

    Rezki, Nadjet; Al-Sodies, Salsabeel A; Aouad, Mohamed R; Bardaweel, Sanaa; Messali, Mouslim; El Ashry, El Sayed H

    2016-01-01

    The present work reports an efficient synthesis of fluorinated pyridinium salts-based hydrazones under both conventional and eco-friendly ultrasound procedures. The synthetic approach first involves the preparation of halogenated pyridinium salts through the condensation of isonicotinic acid hydrazide (1) with p-fluorobenzaldehyde (2) followed by the nucleophilic alkylation of the resulting N-(4-fluorobenzylidene)isonicotinohydrazide (3) with a different alkyl iodide. The iodide counteranion of 5-10 was subjected to an anion exchange metathesis reaction in the presence of an excess of the appropriate metal salts to afford a new series of fluorinated pyridinium salts tethering a hydrazone linkage 11-40. Ultrasound irradiation led to higher yields in considerably less time than the conventional methods. The newly synthesized ILs were well-characterized with FT-IR, ¹H NMR, (13)C NMR, (11)B, (19)F, (31)P and mass spectral analyses. The ILs were also screened for their antimicrobial and antitumor activities. Within the series, the salts tethering fluorinated counter anions 11-13, 21-23, 31-33 and 36-38 were found to be more potent against all bacterial and fungal strains at MIC 4-8 µg/mL. The in vitro antiproliferative activity was also investigated against four tumor cell lines (human ductal breast epithelial tumor T47D, human breast adenocarcinoma MCF-7, human epithelial carcinoma HeLa and human epithelial colorectal adenocarcinoma Caco-2) using the MTT assay, which revealed that promising antitumor activity was exhibited by compounds 5, 12 and 14. PMID:27213367

  8. Identification and Characterization of Potential Impurities in Raloxifene Hydrochloride

    PubMed Central

    Reddy, Reguri Buchi; Goud, Thirumani Venkateshwar; Nagamani, Nagabushanam; Kumar, Nutakki Pavan; Alagudurai, Anandan; Murugan, Raman; Parthasarathy, Kannabiran; Karthikeyan, Vinayagam; Balaji, Perumal

    2012-01-01

    During the synthesis of the bulk drug Raloxifene hydrochloride, eight impurities were observed, four of which were found to be new. All of the impurities were detected using the gradient high performance liquid chromatographic (HPLC) method, whose area percentages ranged from 0.05 to 0.1%. LCMS was performed to identify the mass number of these impurities, and a systematic study was carried out to characterize them. These impurities were synthesized and characterized by spectral data, subjected to co-injection in HPLC, and were found to be matching with the impurities present in the sample. Based on their spectral data (IR, NMR, and Mass), these impurities were characterized as Raloxifene-N-Oxide [Impurity: 1]; EP impurity A [Impurity: 2]; EP impurity B [Impurity: 3]; Raloxifene Dimer [Impurity: 4]; HABT (6-Acetoxy-2-[4-hydroxyphenyl]-1-benzothiophene or 6-Hydroxy-2-[4-acetoxyphenyl]-1-benzothiophene) [Impurity: 5]; PEBE (Methyl[4-[2-(piperidin-1-yl)ethoxy

  9. Simultaneous Estimation of Nebivolol Hydrochloride and Valsartan using RP HPLC

    PubMed Central

    Kokil, S. U.; Bhatia, M. S.

    2009-01-01

    In this study, a rapid, precise, accurate, specific and sensitive ion-paired reverse phase liquid chromatographic method has been developed for the simultaneous estimation of nebivolol hydrochloride and valsartan in their capsule formulation. The chromatographic method was standardized using a HIQ sil C18 column (250×4.6 mm i.d., 5 μm particle size) with UV detection at 289 nm and flow rate of 1 ml/min. The mobile phase consisting of methanol:water (80:20 v/v) with addition of 0.1 percent 1-hexanesulfonic acid monohydrate sodium salt as an ion-pairing reagent was selected. The method was validated and produced accurate and precise results for estimation of the two drugs. PMID:20336202

  10. Peganine hydrochloride dihydrate an orally active antileishmanial agent.

    PubMed

    Khaliq, Tanvir; Misra, Pragya; Gupta, Swati; Reddy, K Papi; Kant, Ruchir; Maulik, P R; Dube, Anuradha; Narender, T

    2009-05-01

    Protozoic infections caused by genus Leishmania pose an enormous public health threat in developing countries, compounded by the toxicity and resistance to current therapies. Under the aegis of our ongoing program on drug discovery and development on antileishmanial agents from plants, we carried out bioassay guided fractionation on Peganum harmala seeds which resulted in the isolation of 1 as an antileishmanial agent. 2D-NMR spectral data and single crystal X-ray crystallography data indicated 1 as peganine hydrochloride in dihydrated form. The compound 1 exhibited in-vitro activity against both extracellular promastigotes as well as intracellular amastigotes residing within murine macrophages in Leishmania donovani. Furthermore, 1 also exhibited in-vivo activity, 79.6 (+/-8.07)% against established VL in hamsters at a dose of 100mg/kgb.wt. PMID:19339182

  11. Interaction between fasudil hydrochloride and bovine serum albumin: spectroscopic study.

    PubMed

    Yu, Xianyong; Jiang, Bingfei; Xun, Caifang; Yao, Qing

    2016-06-01

    The interaction between fasudil hydrochloride (FSD) and bovine serum albumin (BSA) was investigated using fluorescence and ultraviolet spectroscopy under imitated physiological conditions. The Stern-Volmer quenching model has been successfully applied and the results revealed that FSD could quench the intrinsic fluorescence of BSA effectively via static quenching. The binding constants and binding sites for the BSA-FSD system were evaluated. The corresponding thermodynamic parameters obtained at different temperatures indicated that hydrophobic force played a major role in the interaction of FSD and BSA. The distance between the donor (BSA) and the acceptor (FSD) was obtained according to fluorescence resonance energy transfer (FRET). Synchronous fluorescence spectroscopy and FT-IR spectra showed that the conformation of BSA was changed in the presence of FSD. Copyright © 2015 John Wiley & Sons, Ltd. PMID:26554343

  12. [Photodegradation of Ciprofloxacin Hydrochloride in the Aqueous Solution Under UV].

    PubMed

    Duan, Lun-chao; Wang, Feng-he; Zhao, Bin; Chen, Ya-jun

    2016-01-15

    Effects of ciprofloxacin hydrochloride (CIP) initial concentration, Pb (NO3) 2, Cd (NO3) 2, PbCl2 and CdCl2 on the photodegradation of CIP using UV irradiation were investigated. The experiments results showed that UV irradiation could lead to effective removal of CIP, but there was no CIP degradation in dark. The photodegradation rate of CIP reduced with increasing initial concentration under UV irradiation. Pb(NO3)2 and Cd(NO3)2 (except for the experiment group of 0.006 mmol x L(-1)) could enhance CIP photodegradation, and the half-life of CIP gradually increased with increasing molar ratio between heavy metal and CIP ( with the decreasing concentration of nitrate). With increasing molar ratio (with the decreasing concentration of chlorate), PbCl2 and CdCl2 first promoted and then inhibited the CIP photodegradation. PMID:27078959

  13. Multilayer Films and Capsules of Sodium Carboxymethylcellulose and Polyhexamethylenguanidine Hydrochloride

    NASA Astrophysics Data System (ADS)

    Guzenko, Nataliia; Gabchak, Oleksandra; Pakhlov, Evgenij

    The complexation of polyhexamethylenguanidine hydrochloride (PHMG) and sodium carboxymethylcellulose (CMC) was investigated for different conditions. Mixing of equiconcentrated aqueous solutions of the polyelectrolytes was found to result in the formation of an insoluble interpolyelectrolyte complex with an overweight of carboxymethylcellulose. A step-by-step formation of stable, irreversibly adsorbed multilayer film of the polymers was demonstrated using the quartz crystal microbalance method. Unusually thick polymer shells with a large number of loops and tails of the polyanion were formed by the method of layer-by-layer self-assembly of PHMG and CMC on spherical CaCO3 particles. Hollow multilayer capsules stable in neutral media were obtained by dissolution of the inorganic matrix in EDTA solution.

  14. Stability of morphine sulphate and diamorphine hydrochloride in intrasite gel.

    PubMed

    Zeppetella, Giovambattista; Joel, Simon P; Ribeiro, Maria D C

    2005-03-01

    Several studies have reported that opioids applied topically to painful ulcers produce an analgesic effect. It is unknown whether these opioids (usually mixed with hydrogels) are stable and, if so, for how long. We investigated the stability of morphine sulphate and diamorphine hydrochloride, each mixed with intrasite gel at a concentration of 1.25 mg/mL. Samples were prepared in the laboratory and then stored in plastic containers in the dark, at room temperature, in conditions of normal day/night at room temperature, and at 4 degrees C. Aliquots were collected from each container over a 28-day period and analysed using HPLC. No known degradation products were measured in the morphine-intrasite gel mixture stored for up to 28 days, irrespective of the temperature and whether or not samples were exposed to light, suggesting that morphine remains stable. Diamorphine, breaks down to morphine and no other degradation products are measurable. PMID:15810752

  15. Determination of tetracycline hydrochloride by terahertz spectroscopy with PLSR model.

    PubMed

    Qin, Jianyuan; Xie, Lijuan; Ying, Yibin

    2015-03-01

    Antibiotic residues in agricultural and food products are of great concern to legislatures and consumers. Reliable techniques for rapid and sensitive detection of these residues are necessary to ensure food safety. In this study, tetracycline hydrochloride (TC-HCl) in powder and solution form was detected and quantified using terahertz (THz) spectroscopy. Partial least-squares regression (PLSR) was used to build calibration models. The results obtained in this study indicated that the PLSR model for powder samples was excellent and could be used for quality control. However, the PLSR model for solution samples was not robust and needed to be improved. Overall, THz spectroscopy combined with PLSR model had its potential for the rapid and non-destructive prediction of TC-HCl residue without sophisticated methods, although the accuracy was not high for solution samples which should be improved in future study. PMID:25306365

  16. Cryptolepine hydrochloride: a potent antimycobacterial alkaloid derived from Cryptolepis sanguinolenta.

    PubMed

    Gibbons, Simon; Fallah, Fatemeh; Wright, Colin W

    2003-04-01

    The activity of cryptolepine hydrochloride, a salt of the main indoloquinoline alkaloid from the West African medicinal plant Cryptolepis sanguinolenta, was assessed against the fast growing mycobacterial species Mycobacterium fortuitum, which has recently been shown to be of use in the evaluation of antitubercular drugs. The low minimum inhibitory concentration (MIC) of this compound (16 microg/mL) prompted further evaluation against other fast growing mycobacteria namely, M. phlei, M. aurum, M. smegmatis, M. bovis BCG and M. abcessus and the MICs ranged over 2-32 microg/mL for these species. The strong activity of this agent, the need for new antibiotics with activity against Mycobacterium tuberculosis, coupled with the ethnobotanical use of C. sanguinolenta extracts to treat infections, highlight the potential of the cryptolepine template for development of antimycobacterial agents. PMID:12722159

  17. Simple colorimetric method for determination of thiamine hydrochloride in pharmaceuticals.

    PubMed

    Sane, R T; Doshi, V J; Jukar, S; Joshi, S K; Sawant, S V; Pandit, U R

    1985-01-01

    A simple colorimetric method is described for the determination of thiamine hydrochloride (vitamin B1) in dosage forms. The method is based on measurement of a yellow complex formed when thiamine HCl is treated with p-methylaminophenol sulfate (Metol) under alkaline conditions. Compounds such as vitamins A, B2, B6, B12, C, D, and E, and niacinamide, citric acid, liquid glucose, calcium pantothenate, biotin, liver extract, and folic acid do not interfere in the reaction. Extracting the complex into chloroform before quantitation enhances the stability of the reaction product and removes interference of water-soluble colored constituents in syrup samples. Statistical validation shows that the method is precise and accurate. Results agree well with those obtained by other methods in the literature. PMID:3980419

  18. Stability of apomorphine hydrochloride in aqueous sodium bisulphite solutions.

    PubMed

    Ng Ying Kin, N M; Lal, S; Thavundayil, J X

    2001-10-01

    Apomorphine (Apo), a dopamine receptor agonist used extensively in clinical research, is known to be chemically unstable. The authors have used a high performance liquid chromatography (HPLC) method to study the long-term stability of pharmaceutical preparations of R(-) Apomorphine hydrochloride (ApoHCI) for parenteral use. In a concentration of 1 mg/ml, ApoHCI in aqueous solutions of sodium metabisulphite (0.125%), kept at 4 degrees and shielded from light, was found to be stable for up to six months. On the other hand, solutions of 0.1 mg/ml were found to decompose after only three weeks, showing extraneous peaks in the HPLC. However, the blue-green discoloration, characteristic of Apo degradation, was only apparent after six weeks storage. The rapidity of the HPLC method used, its reproducibility and sensitivity make it suitable for quality control studies of pharmaceutical preparations of ApoHCI intended for clinical research. PMID:11513359

  19. Development and Statistical Optimisation of Buspirone Hydrochloride Buccoadhesive Films

    PubMed Central

    Nagaich, Upendra; Chaudhary, Vandana; Nagaich, Jaya

    2014-01-01

    The aim of the present study was to prepare unidirectional buccal films of buspirone hydrochloride by solvent casting technique. Hydroxypropylmethylcellulose (HPMC K15M) and Eudragit RL-100 were used as polymers in different proportion. Polyethylene glycol 400 and sodium lauryl sulphate were used as plasticizer and permeation enhancer, respectively, in different concentration. In the formulation, total amount of polymer (X1) and percentage of HPMC K15M (X2) were kept as independent variables. Afterwards, statistically optimized process was carried out and two optimized formulations (OF1 and OF2) were developed. The observed results of optimized formulation were showed a greater degree of percentage of similarity with predicted values. The stability studies showed that there was no significant change found in physicochemical properties, in-vitro release, and ex-vivo diffusion studies. PMID:27351002

  20. Coated hydralazine hydrochloride beads for sustained release after oral administration.

    PubMed

    Mughal, M Akhlaq; Saripella, Kalyan K; Kouba, Chahinaz; Iqbal, Zafar; Neau, Steven H

    2013-09-01

    Hydralazine hydrochloride is an antihypertensive used alone or in combination with isosorbide nitrate for the treatment of congestive heart failure. Since control of blood pressure should be continuous, sustained release delivery of this drug is considered therapeutically beneficial. Core beads for oral administration of this drug were prepared by extrusion-spheronization. Using experimental design to define the coat that was applied, the core beads were coated using a fluid bed coater to different coat thickness with combinations of two commercially available products dissolved in a hydroalcoholic solvent. The coat is a film with a combination of ethylcellulose and hydroxypropylcellulose that can provide desirable release profiles. Visually spherical and rugged bead products were obtained. Two products were identified that exhibited essentially a zero order release profile following a 2-h lag time with release of greater than 70% of the drug over the next 10 h in simulated intestinal fluid. PMID:23057650

  1. Formulation and evaluation of verapamil hydrochloride loaded solid lipid microparticles.

    PubMed

    Pilaniya, U; Pilaniya, K; Chandrawanshi, H K; Gupta, N; Rajput, M S

    2011-01-01

    The present study aimed to produce verapamil hydrochloride-loaded solid lipid microparticles (SLM) by the w/o/w emulsion solvent evaporation technique, using diethyl ether as solvent phase, glyceryl monostearate as biodegradable polymer and Span 60 as surfactant. SLM of spherical shape were prepared by simple dilution of the emulsion with water. To increase the lipid load the process was conducted at 50 degrees C, and in order to reach sub-micron size, a high-shear homogenizer was used. The encapsulation efficiency of prepared SLM reached 74.29 +/- 0.76%. Particle size (98.55 +/- 1.42 microm), surface morphology (spherical) and drug loading efficiency (18.57 +/- 1.25% w/w) were investigated. And optimization of drug polymer ratio (3:1), nature and concentration of emulsion stabilizer in the external aqueous (0.1%), phase viscosity of external aqueous phase (0.5%), volume of external aqueous phase and stirring rate (1000 rpm) were detected. Analysis of microsphere content after processing showed that verapamil did not undergo any chemical modification within the micro-particles. The in-vitro release of verapamil from the microparticles was very low and an initial burst effect of 17% of the dose was observed. The slow release may help to avoid a high frequency of administration. The prepared solid lipid microparticles appear to have interesting perspectives as delivery systems for the oral administration of verapamil hydrochloride with improved half-life, improved bioavailability, and minimized local and systemic gastrointestinal disturbances of the drug. PMID:21391431

  2. 40 CFR Appendix B to Subpart Nnn... - Free Formaldehyde Analysis of Insulation Resins by Hydroxylamine Hydrochloride

    Code of Federal Regulations, 2013 CFR

    2013-07-01

    ... in the polymeric form. The hydrolysis of these polymers is catalyzed by hydrogen ions. 2.2The resin... hydroxylamine hydrochloride will produce sufficient hydrogen ions to catalyze the depolymerization of...

  3. The effect of tramadol hydrochloride on early life stages of fish.

    PubMed

    Sehonova, Pavla; Plhalova, Lucie; Blahova, Jana; Berankova, Petra; Doubkova, Veronika; Prokes, Miroslav; Tichy, Frantisek; Vecerek, Vladimir; Svobodova, Zdenka

    2016-06-01

    The aim of this study was to perform the fish embryo acute toxicity test (FET) on zebrafish (Danio rerio) and the early-life stage toxicity test on common carp (Cyprinus carpio) with tramadol hydrochloride. The FET was performed using the method inspired by the OECD guideline 236. Newly fertilized zebrafish eggs were exposed to tramadol hydrochloride at concentrations of 10; 50; 100 and 200μg/l for a period of 144h. An embryo-larval toxicity test on C. carpio was performed according to OECD guideline 210 also with tramadol hydrochloride at concentrations 10; 50; 100 and 200μg/l for a period of 32 days. Hatching was significantly influenced in both acute and subchronic toxicity assays. Subchronic exposure also influenced early ontogeny, both morphometric and condition characteristics and caused changes in antioxidant enzyme activity. The LOEC value was found to be 10μg/l tramadol hydrochloride. PMID:27208654

  4. 78 FR 40484 - Determination That METADATE ER (Methylphenidate Hydrochloride) Extended-Release Tablet, 10...

    Federal Register 2010, 2011, 2012, 2013, 2014

    2013-07-05

    ... HUMAN SERVICES Food and Drug Administration Determination That METADATE ER (Methylphenidate... Administration (FDA) has determined that METADATE ER (methylphenidate hydrochloride (HCl)) extended-release... determination will allow FDA to approve abbreviated new drug applications (ANDAs) for methylphenidate...

  5. Sustained transdermal release of diltiazem hydrochloride through electron beam irradiated different PVA hydrogel membranes

    NASA Astrophysics Data System (ADS)

    Bhunia, Tridib; Goswami, Luna; Chattopadhyay, Dipankar; Bandyopadhyay, Abhijit

    2011-08-01

    Extremely fast release of diltiazem hydrochloride (water soluble, anti anginal drug used to treat chest pain) together with its faster erosion has been the primary problem in conventional oral therapy. It has been addressed in this paper by encapsulating the drug in electron beam irradiated various poly (vinyl alcohol) hydrogel membranes and delivering it through transdermal route. Results show excellent control over the release of diltiazem hydrochloride through these membranes subject to their physico-mechanicals.

  6. 40 CFR Appendix B to Subpart Nnn... - Free Formaldehyde Analysis of Insulation Resins by Hydroxylamine Hydrochloride

    Code of Federal Regulations, 2010 CFR

    2010-07-01

    ... hydrochloric acid that is liberated when hydroxylamine hydrochloride reacts with formaldehyde to form..., using the prestandardized pH meter, 1.0 N hydrochloric acid, 0.1 N hydrochloric acid, and 0.1 N sodium... hydrochloride solution, 100 grams per liter, pH adjusted to 4.00. 4.3Hydrochloric acid solution, 1.0 N and 0.1...

  7. 40 CFR Appendix B to Subpart Nnn... - Free Formaldehyde Analysis of Insulation Resins by Hydroxylamine Hydrochloride

    Code of Federal Regulations, 2011 CFR

    2011-07-01

    ... hydrochloric acid that is liberated when hydroxylamine hydrochloride reacts with formaldehyde to form..., using the prestandardized pH meter, 1.0 N hydrochloric acid, 0.1 N hydrochloric acid, and 0.1 N sodium... hydrochloride solution, 100 grams per liter, pH adjusted to 4.00. 4.3Hydrochloric acid solution, 1.0 N and 0.1...

  8. Benzydamine hydrochloride in prevention and management of pain in oral mucositis associated with radiation therapy

    SciTech Connect

    Epstein, J.B.; Stevenson-Moore, P.

    1986-08-01

    Benzydamine hydrochloride rinse reduced pain associated with radiation mucositis when it was used during the course of radiation therapy. Fewer patients using benzydamine rinse required systemic analgesics. All patients using benzydamine tolerated the rinse well and continued with regular rinsing throughout the course of radiation therapy. Benzydamine hydrochloride is currently undergoing clinical trials in the United States for application for approval from the Food and Drug Administration.

  9. Effects of Olopatadine Hydrochloride, a Histamine H1 Receptor Antagonist, on Histamine-Induced Skin Responses

    PubMed Central

    Hashimoto, Takashi; Ishii, Norito; Hamada, Takahiro; Dainichi, Teruki; Karashima, Tadashi; Nakama, Takekuni; Yasumoto, Shinichiro

    2010-01-01

    Effects of olopatadine hydrochloride, a histamine H1 receptor antagonist, on histamine-induced skin responses were evaluated in 10 healthy subjects in comparison with placebo, fexofenadine hydrochloride, and bepotastine besilate. Olopatadine significantly suppressed histamine-induced wheal, flare, and itch, starting 30 minutes after oral administration. Olopatadine was more effective than fexofenadine and bepotastine. None of the drugs studied impaired performance of word processing tasks. These results suggest that olopatadine can suppress skin symptoms caused by histamine soon after administration. PMID:20886023

  10. Co-Amorphous Combination of Nateglinide-Metformin Hydrochloride for Dissolution Enhancement.

    PubMed

    Wairkar, Sarika; Gaud, Ram

    2016-06-01

    The aim of the present work was to prepare a co-amorphous mixture (COAM) of Nateglinide and Metformin hydrochloride to enhance the dissolution rate of poorly soluble Nateglinide. Nateglinide (120 mg) and Metformin hydrochloride (500 mg) COAM, as a dose ratio, were prepared by ball-milling technique. COAMs were characterized for saturation solubility, amorphism and physicochemical interactions (X-ray powder diffraction (XRPD), differential scanning calorimetry (DSC), Fourier transform infrared spectroscopy (FTIR)), SEM, in vitro dissolution, and stability studies. Solubility studies revealed a sevenfold rise in solubility of Nateglinide from 0.061 to 0.423 mg/ml in dose ratio of COAM. Solid-state characterization of COAM suggested amorphization of Nateglinide after 6 h of ball milling. XRPD and DSC studies confirmed amorphism in Nateglinide, whereas FTIR elucidated hydrogen interactions (proton exchange between Nateglinide and Metformin hydrochloride). Interestingly, due to low energy of fusion, Nateglinide was completely amorphized and stabilized by Metformin hydrochloride. Consequently, in vitro drug release showed significant increase in dissolution of Nateglinide in COAM, irrespective of dissolution medium. However, little change was observed in the solubility and dissolution profile of Metformin hydrochloride, revealing small change in its crystallinity. Stability data indicated no traces of devitrification in XRPD of stability sample of COAM, and % drug release remained unaffected at accelerated storage conditions. Amorphism of Nateglinide, proton exchange with Metformin hydrochloride, and stabilization of its amorphous form have been noted in ball-milled COAM of Nateglinide-Metformin hydrochloride, revealing enhanced dissolution of Nateglinide. Thus, COAM of Nateglinide-Metformin hydrochloride system is a promising approach for combination therapy in diabetic patients. PMID:26314243

  11. Safety and efficacy of tramadol hydrochloride on treatment of premature ejaculation.

    PubMed

    Eassa, Bayoumy I; El-Shazly, Mohamed A

    2013-01-01

    Premature ejaculation (PE) is the most common sexual disorder. It affects 20%-30% of adult men; the aetiology of this condition has not yet been elucidated. The aim of this study is to evaluate the efficacy, safety, tolerability, undesirable effects and improved satisfaction with sexual intercourse with tramadol hydrochloride at different dosages for the treatment of PE. A total of 300 patients who presented with lifelong (primary) PE were included in this study. The study was performed for 28 weeks, in which placebo (starch tablet) was given for 4 weeks, and active ingredient (tramadol hydrochloride) was administered at different therapeutic dosages for 24 weeks. Patients were divided into three equal groups, each consisting of 100 patients. The first group (A) was given tramadol hydrochloride capsule 25 mg. The second group (B) was given tramadol hydrochloride capsule 50 mg. The third group (C) was given tramadol hydrochloride capsule 100 mg. All of the 300 participants included completed the study voluntarily. The age of the patients varied from 25 to 50 years. After the treatment period, the recorded data were collected for each group and analysed. The results showed a highly significant increase in the mean intravaginal ejaculatory latency time (IELT) in all groups compared to baseline data (P<0.0001). We concluded that using tramadol hydrochloride at different doses on demand for the treatment of PE is effective, safe and tolerable, with minimal undesirable effects, and approval for this indication should be sought. PMID:23103596

  12. Stability-indicating HPLC Method for Simultaneous Determination of Montelukast and Fexofenadine Hydrochloride

    PubMed Central

    Pankhaniya, Mona; Patel, Parula; Shah, J. S.

    2013-01-01

    A simple, specific, accurate, and stability-indicating reversed-phase high-performance liquid chromatographic method was developed for the simultaneous determination of montelukast and fexofenadine hydrochloride, using a Lichrospher® 100, RP-18e column and a mobile phase composed of methanol:0.1% o-phosphoric acid (90:10 v/v), pH 6.8. The retention times of montelukast and fexofenadine hydrochloride were found to be 10.16 and 12.03 min, respectively. Linearity was established for montelukast and fexofenadine hydrochloride in the range of 2-10 μg/ml and 24-120 μg/ml, respectively. The percentage recoveries of montelukast and fexofenadine hydrochloride were found to be in the range of 99.09 and 99.81%, respectively. Both the drugs were subjected to acid and base hydrolysis, oxidation, photolytic, and thermal degradation conditions. The degradation products of montelukast and fexofenadine hydrochloride were well resolved from the pure drug with significant differences in their retention time values. This method can be successfully employed for simultaneous quantitative analysis of montelukast and fexofenadine hydrochloride in bulk drugs and formulations. PMID:24082344

  13. Using crystal structure prediction to rationalize the hydration propensities of substituted adamantane hydrochloride salts.

    PubMed

    Mohamed, Sharmarke; Karothu, Durga Prasad; Naumov, Panče

    2016-08-01

    The crystal energy landscapes of the salts of two rigid pharmaceutically active molecules reveal that the experimental structure of amantadine hydrochloride is the most stable structure with the majority of low-energy structures adopting a chain hydrogen-bond motif and packings that do not have solvent accessible voids. By contrast, memantine hydrochloride which differs in the substitution of two methyl groups on the adamantane ring has a crystal energy landscape where all structures within 10 kJ mol(-1) of the global minimum have solvent-accessible voids ranging from 3 to 14% of the unit-cell volume including the lattice energy minimum that was calculated after removing water from the hydrated memantine hydrochloride salt structure. The success in using crystal structure prediction (CSP) to rationalize the different hydration propensities of these substituted adamantane hydrochloride salts allowed us to extend the model to predict under blind test conditions the experimental crystal structures of the previously uncharacterized 1-(methylamino)adamantane base and its corresponding hydrochloride salt. Although the crystal structure of 1-(methylamino)adamantane was correctly predicted as the second ranked structure on the static lattice energy landscape, the crystallization of a Z' = 3 structure of 1-(methylamino)adamantane hydrochloride reveals the limits of applying CSP when the contents of the crystallographic asymmetric unit are unknown. PMID:27484376

  14. Safety and efficacy of tramadol hydrochloride on treatment of premature ejaculation

    PubMed Central

    Eassa, Bayoumy I; El-Shazly, Mohamed A

    2013-01-01

    Premature ejaculation (PE) is the most common sexual disorder. It affects 20%–30% of adult men; the aetiology of this condition has not yet been elucidated. The aim of this study is to evaluate the efficacy, safety, tolerability, undesirable effects and improved satisfaction with sexual intercourse with tramadol hydrochloride at different dosages for the treatment of PE. A total of 300 patients who presented with lifelong (primary) PE were included in this study. The study was performed for 28 weeks, in which placebo (starch tablet) was given for 4 weeks, and active ingredient (tramadol hydrochloride) was administered at different therapeutic dosages for 24 weeks. Patients were divided into three equal groups, each consisting of 100 patients. The first group (A) was given tramadol hydrochloride capsule 25 mg. The second group (B) was given tramadol hydrochloride capsule 50 mg. The third group (C) was given tramadol hydrochloride capsule 100 mg. All of the 300 participants included completed the study voluntarily. The age of the patients varied from 25 to 50 years. After the treatment period, the recorded data were collected for each group and analysed. The results showed a highly significant increase in the mean intravaginal ejaculatory latency time (IELT) in all groups compared to baseline data (P<0.0001). We concluded that using tramadol hydrochloride at different doses on demand for the treatment of PE is effective, safe and tolerable, with minimal undesirable effects, and approval for this indication should be sought. PMID:23103596

  15. Increased Mortality in Groups of Cattle Administered the β-Adrenergic Agonists Ractopamine Hydrochloride and Zilpaterol Hydrochloride

    PubMed Central

    Loneragan, Guy H.; Thomson, Daniel U.; Scott, H. Morgan

    2014-01-01

    The United States Food and Drug Administration (FDA) approved two β-adrenergic agonists (βAA) for in-feed administration to cattle fed in confinement for human consumption. Anecdotal reports have generated concern that administration of βAA might be associated with an increased incidence of cattle deaths. Our objectives, therefore, were to a) quantify the association between βAA administration and mortality in feedlot cattle, and b) explore those variables that may confound or modify this association. Three datasets were acquired for analysis: one included information from randomized and controlled clinical trials of the βAA ractopamine hydrochloride, while the other two were observational data on zilpaterol hydrochloride administration to large numbers of cattle housed, fed, and cared for using routine commercial production practices in the U.S. Various population and time at-risk models were developed to explore potential βAA relationships with mortality, as well as the extent of confounding and effect modification. Measures of effect were relatively consistent across datasets and models in that the cumulative risk and incidence rate of death was 75 to 90% greater in animals administered the βAA compared to contemporaneous controls. During the exposure period, 40 to 50% of deaths among groups administered the βAA were attributed to administration of the drug. None of the available covariates meaningfully confounded the relationship between βAA and increased mortality. Only month of slaughter, presumably a proxy for climate, consistently modified the effect in that the biological association was generally greatest during the warmer months of the year. While death is a rare event in feedlot cattle, the data reported herein provide compelling evidence that mortality is nevertheless increased in response to administration of FDA-approved βAA and represents a heretofore unquantified adverse drug event. PMID:24621596

  16. Electron paramagnetic resonance studies of gamma-irradiated DL-alanine ethyl ester hydrochloride, L-theanine and L-glutamic acid dimethyl ester hydrochloride.

    PubMed

    Başkan, M Halim; Aydın, Murat

    2013-08-01

    The electron paramagnetic resonance (EPR) of gamma irradiated powders of DL-alanine ethyl ester hydrochloride, L-theanine and L-glutamic acid dimethyl ester hydrochloride were investigated at room temperature. The observed paramagnetic species were attributed to the CH3ĊHCOOC2H5, -CH2ĊHCOOH and -CH2ĊHCOOCH3 radicals, respectively. Hyperfine structure constants and g-values were determined for these three radicals. Some spectroscopic properties and suggestions concerning the possible structure of the radicals were also discussed. PMID:23680512

  17. Electron paramagnetic resonance studies of gamma-irradiated DL-alanine ethyl ester hydrochloride, L-theanine and L-glutamic acid dimethyl ester hydrochloride

    NASA Astrophysics Data System (ADS)

    Başkan, M. Halim; Aydın, Murat

    2013-08-01

    The electron paramagnetic resonance (EPR) of gamma irradiated powders of DL-alanine ethyl ester hydrochloride, L-theanine and L-glutamic acid dimethyl ester hydrochloride were investigated at room temperature. The observed paramagnetic species were attributed to the CH3ĊHCOOC2H5, -CH2ĊHCOOH and -CH2ĊHCOOCH3 radicals, respectively. Hyperfine structure constants and g-values were determined for these three radicals. Some spectroscopic properties and suggestions concerning the possible structure of the radicals were also discussed.

  18. Microneedle-assisted delivery of verapamil hydrochloride and amlodipine besylate.

    PubMed

    Kaur, Monika; Ita, Kevin B; Popova, Inna E; Parikh, Sanjai J; Bair, Daniel A

    2014-02-01

    The aim of this project was to study the effect of stainless steel solid microneedles and microneedle rollers on percutaneous penetration of verapamil hydrochloride and amlodipine besylate. Verapamil, 2-(3,4-dimethooxyphenyl)-5-[2-(3,4 dimethoxyphenyl)ethyl-methyl-amino]-2-propan-2-yl-pentanenitrile is a calcium channel blocker agent that regulates high blood pressure by decreasing myocardial contractilty, heart rate and impulse conduction. Amlodipine, (R, S)-2-[(2-aminoethoxy) methyl]-4-(2-chlorophenyl)-3-ethoxycarbonyl-5-methoxycarbonyl-6-methyl-1, 4-dihydropyridine, is a calcium channel blocker that is used for the management of hypertension and ischemic heart disease. Passive penetration of verapamil and amlodipine across the skin is low. In vitro studies were performed with microneedle-treated porcine ear skin using vertical static Franz diffusion cells (PermeGear, Hellertown, PA, USA). The receiver chamber contained 5ml of PBS (pH7.4) and was constantly maintained at 37°C temperature with a water circulation jacket. The diffusion area of the skin was 1.77cm(2). The donor compartment was loaded with 1ml of the solution containing 2.5mg/ml of amlodipine besylate. The donor chamber was covered with parafilm to avoid evaporation. Passive diffusion across untreated porcine skin served as control. Aliquots were taken every 2h for 12h and analyzed by liquid chromatography-mass spectrometry. Transcutaneous flux of verapamil increased significantly from 8.75μg/cm(2)/h to 49.96μg/cm(2)/h across microneedle-roller treated porcine skin. Percutaneous flux of amlodipine besylate following the use of stainless steel microneedles was 22.39μg/cm(2)/h. Passive flux for the drug was 1.57μg/cm(2)/h. This enhancement of amlodipine flux was statistically significant. Transdermal flux of amlodipine with microneedle roller was 1.05μg/cm(2)/h in comparison with passive diffusion flux of 0.19μg/cm(2)/h. The difference in flux values was also statistically significant. Stainless

  19. Stability-indicating HPTLC determination of ambroxol hydrochloride in bulk drug and pharmaceutical dosage form.

    PubMed

    Jain, P S

    2010-01-01

    A simple, selective, precise, and stability-indicating high-performance thin-layer chromatographic (HPTLC) method for the analysis of ambroxol hydrochloride both as a bulk drug and in formulations was developed and validated. The method employed HPTLC aluminium plates precoated with silica gel 60F-254 as the stationary phase. The solvent system consisted of methanol-triethylamine (4:6 v/v). The system was found to give a compact spot for ambroxol hydrochloride (R(f) value of 0.53 +/- 0.02). Densitometric analysis of ambroxol hydrochloride was carried out in the absorbance mode at 254 nm. The linear regression analysis data for the calibration plots showed good linear relationship with r(2) = 0.9966 +/- 0.0013 with respect to peak area in the concentration range 100-1000 ng/spot. The mean value +/- standard deviation of slope and intercept were 164.85 +/- 0.72 and 1168.3 +/- 8.26 with respect to peak area. The method was validated for precision, recovery, and robustness. The limits of detection and quantitation were 10 and 30 ng/spot, respectively. Ambroxol hydrochloride was subjected to oxidation and thermal degradation. The drug undergoes degradation under oxidation and heat conditions. This indicates that the drug is susceptible to oxidation and heat. Statistical analysis proves that the method is repeatable, selective, and accurate for the estimation of said drug. Stability indicating of new chemical entities is an important part for the drug development of ambroxol hydrochloride and for its estimation in plasma and other biological fluids; the novel Statistical analysis proves that the method is repeatable and selective for the analysis of ambroxol hydrochloride as bulk drug and in pharmaceutical formulations. The proposed developed HPTLC method can be applied for identification and quantitative determination of ambroxol hydrochloride in bulk drug and dosage forms. This work is to determine the purity of the drug available from the various sources by detecting

  20. Efficacy of landiolol hydrochloride for atrial fibrillation after open heart surgery.

    PubMed

    Nishi, Hiroyuki; Sakaguchi, Taichi; Miyagawa, Shigeru; Yoshikawa, Yasushi; Fukushima, Satsuki; Saito, Shunsuke; Ueno, Takayoshi; Kuratani, Toru; Sawa, Yoshiki

    2013-07-01

    It is important to establish effective treatment for postoperative atrial fibrillation (AF), the most common complication after cardiac surgery. We evaluated the efficacy and safety of landiolol hydrochloride for rhythm conversion in patients with postoperative AF. Among 134 patients who developed new-onset AF after open heart surgery between 2007 and 2009, 69 patients who received landiolol hydrochloride for treatment of postoperative AF were enrolled. The AF conversion rate, the percentage of patients with 20 % reduction of the ventricular rate, and the factors related to successful treatment were evaluated. Then, the landiolol group was compared with 65 patients who had postoperative AF and did not receive landiolol hydrochloride. Landiolol hydrochloride was the first-line treatment in 46 patients and the only therapy in 26 patients. Reversion to sinus rhythm was achieved in 51 patients, while the conversion rate in patients without landiolol hydrochloride was only 56.8 % (p < 0.05). A 20 % reduction of the ventricular rate was achieved more frequently in the landiolol group. Although landiolol hydrochloride was highly effective in patients who had undergone off-pump coronary artery bypass grafting, patients with cardiopulmonary bypass did not respond as well. The heart rate was reduced from 130 ± 26 to 81 ± 12 (p < 0.05) after landiolol administration, while blood pressure did not decrease significantly. Landiolol hydrochloride was effective for conversion of postoperative AF. This ultra-short-acting β-blocker is a safe first-line treatment for postoperative AF after open heart surgery, and is most effective in patients who have undergone off-pump coronary artery bypass grafting. PMID:22661097

  1. A Double-Blind, Placebo-Controlled Trial of Dexmethylphenidate Hydrochloride and D,l-Threo-Methylphenidate Hydrochloride in Children with Attention-Deficit-Hyperactivity Disorder

    ERIC Educational Resources Information Center

    Wigal, Sharon; Swanson, James M.; Feifel, David; Sangal, R. Bart; Elia, Josephine; Casat, Charles D.; Zeldis, Jerome B.; Conners, C. Keith

    2004-01-01

    Objective: To evaluate the efficacy and safety of dexmethylphenidate hydrochloride (d-MPH, Focalin[TM]) for the treatment of attention-deficit/hyperactivity disorder (ADHD) and to test an a priori hypothesis that d-MPH would have a longer duration of action than d,l-threo-methylphenidate (d,l-MPH). Method: This was a randomized, double-blind study…

  2. Development and validation of a HPLC method for the determination of buprenorphine hydrochloride, naloxone hydrochloride and noroxymorphone in a tablet formulation.

    PubMed

    Mostafavi, Ali; Abedi, Ghazaleh; Jamshidi, Ahmad; Afzali, Daryoush; Talebi, Mohammad

    2009-02-15

    A simple isocratic reversed-phase high-performance liquid chromatographic method (RP-HPLC) was developed for the simultaneous determination of buprenorphine hydrochloride, naloxone hydrochloride dihydrate and its major impurity, noroxymorphone, in pharmaceutical tablets. The chromatographic separation was achieved with 10 mmol L(-1) potassium phosphate buffer adjusted to pH 6.0 with orthophosphoric acid and acetonitrile (17:83, v/v) as mobile phase, a C-18 column, Perfectsil Target ODS3 (150 mm x 4.6mm i.d., 5 microm) kept at 35 degrees C and UV detection at 210 nm. The compounds were eluted isocratically at a flow rate of 1.0 mL min(-1). The average retention times for naloxone, noroxymorphone and buprenorphine were 2.4, 3.8 and 8.1 min, respectively. The method was validated according to the ICH guidelines. The validation characteristics included accuracy, precision, linearity, range, specificity, limit of quantitation and robustness. The calibration curves were linear (r>0.996) over the concentration range 0.22-220 microg mL(-1) for buprenorphine hydrochloride and 0.1-100 microg mL(-1) for naloxone hydrochloride dihydrate and noroxymorphone. The recoveries for all three compounds were above 96%. No spectral or chromatographic interferences from the tablet excipients were found. This method is rapid and simple, does not require any sample preparation and is suitable for routine quality control analyses. PMID:19084658

  3. Trans-ungual delivery of itraconazole hydrochloride by iontophoresis.

    PubMed

    Kushwaha, Avadhesh; Jacob, Melissa; Shiva Kumar, H N; Hiremath, Shobharani; Aradhya, Sacchidanand; Repka, Michael A; Murthy, S Narasimha

    2015-01-01

    Itraconazole (ITR) is a potent antifungal drug. However, poor aqueous solubility limits its permeation ability across the human nail plate. Therefore, in this project, ITR was converted to hydrochloride salt (ITR-HCl) to improve its solubility and to render it amenable to iontophoresis. ITR-HCl was characterized by spectroscopic methods and antifungal efficacy was evaluated in comparison to the base. In vitro and ex vivo transport studies (passive and iontophoresis) were carried out across the porcine hoof membrane and excised human cadaver toe using two different protocols; continuous delivery of drug for 24 h and pulsed delivery of drug for 3 days (8 h/day). The antifungal efficacy of ITR-HCL was comparable to ITR. Iontophoresis was found to be more effective than passive mode of delivery of ITR-HCL. In both iontophoresis as well as passive mode of delivery, the pulsed protocol resulted in more ungual and trans-ungual delivery of drug than continuous protocol. ITR-HCL could be delivered into and across the nail plate by iontophoresis. Human cadaver toe appears to be a good model to investigate the ungual delivery of drugs. PMID:25482587

  4. Stability of revex, nalmefene hydrochloride injection, in injectable solutions.

    PubMed

    Murthy, S S; Brittain, H G

    1996-11-01

    The short-term stability of Revex, nalmefene hydrochloride injection, was determined in a number of diluents commonly employed for intravenous use. An HPLC method was used to follow the potency of the diluted solutions, and was fully validated for its intended concentration range prior to its use. Dilutions of Revex were prepared separately in 0.9% sodium chloride injection, 0.45% sodium chloride injection, 5% dextrose injection, 5% dextrose and 0.45% sodium chloride injection, lactated Ringer's injection, 5% dextrose and lactated Ringer's injection and 5% sodium hydrogencarbonate injection. Each admixture was stored at 4 degrees C, room temperature (21 degrees C) and 40 degrees C, with samples being tested after storage at each temperature for 0, 24, 48 and 72 h. Defining stability as the retention of at least 95% of the initial drug concentration at the end of the storage period, it was concluded that the diluted solutions of Revex were uniformly stable for up to 72 h in all of the injectable solutions maintained at either 4, 21 or 40 degrees C. PMID:8933423

  5. [Pharmacokinetics of naltrexone hydrochloride and naltrexone glucuronide in the dog].

    PubMed

    Li, H; Zhao, S F; Wang, N; Ge, Z H

    1996-01-01

    Pharmacokinetics of naltrexone hydrochloride (NTX) and naltrexone glucuronide was studied in the dog using HPLC-electrochemical detection with naloxone as internal standard. After iv 5 mg or po 10 mg NTX, the plasma concentration-time curves of NTX were found to fit to a two-compartment model and a single compartment with first-order absorption. The elimination half-lives of NTX were 78 +/- 6 min and 74 +/- 6 min, respectively. Although NTX could be absorbed rapidly in the dog after po administration, the plasma concentration of the parent drug was very low and its absolute bioavailability was 15.8%. The experiments showed that the major metabolite of NTX in dog plasma was beta-glucuronidase-hydrolyzable conjugate. Dosing NTX intravenously and orally, the plasma levels of the conjugate were 1.3 and 23 times as high as that of the parent drug, the elimination half-lives of the glucuronide from plasma were 3.4 h and 12.6 h, respectively. The results indicate that NTX is subjected to a marked first-pass effect in the dog after oral administration. PMID:9208648

  6. Preliminary Toxicological Report of Metformin Hydrochloride Loaded Polymeric Nanoparticles

    PubMed Central

    Lekshmi, Unnikrishnan Meenakshi Dhana; Reddy, Pully Neelakanta

    2012-01-01

    Nanosized materials have tremendous application in every field of human activity, with a lot of economic benefit increasing nanoparticle research and use. There are number of nanosized products already available commercially and many others are in queue. Therefore, there is a pressing need for careful consideration of benefits and side effects of the use of nanoparticles in medicine. This research work aims at providing a balanced update of this exciting potentially toxicological effect of manufactured Metformin hydrochloride loaded polymeric nanoparticles. To assess the toxicities systematically on the functions of various tissues and organs in rats, the rats were fed with the manufactured polymeric nanoparticles for a period of 30 days repeated oral administration. Variation in the protein, carbohydrate and fat metabolic profile of the rat exposed to nanoparticles were studied by hematobiochemical and pathology profiles. The haemolytic potential of these nanoparticles were determined by means of an in vitro haemolysis assay. All formulations showed haemolytic effect less than 5%. The study revealed that Metformin loaded PMMA and PLGA polymeric nanoparticle did not produce any toxicity. PMID:23293465

  7. Release kinetics of papaverine hydrochloride from tablets with different excipients.

    PubMed

    Kasperek, Regina; Polski, Andrzej; Zimmer, Łukasz; Poleszak, Ewa

    2014-09-01

    The influence of excipients on the disintegration times of tablets and the release of papaverine hydrochloride (PAP) from tablets were studied. Ten different formulations of tablets with PAP were prepared by direct powder compression. Different binders, disintegrants, fillers, and lubricants were used as excipients. The release of PAP was carried out in the paddle apparatus using 0.1 N HCl as a dissolution medium. The results of the disintegration times of tablets showed that six formulations can be classified as fast dissolving tablets (FDT). FDT formulations contained Avicel PH 101, Avicel PH 102, mannitol, (3-lactose, PVP K 10, gelatinized starch (CPharmGel), Prosolv Easy Tab, Prosolv SMCC 90, magnesium stearate, and the addition of disintegrants such as AcDiSol and Kollidon CL. Drug release kinetics were estimated by the zero- and first-order, Higuchi release rate, and Korsmeyer-Peppas models. Two formulations of the tablets containing PVP (K10) (10%), CPharmGel (10% and 25%), and Prosolv Easy Tab (44% and 60%) without the addition of a disintegrant were well-fitted to the kinetics models such as the Higuchi and zero-order, which are suitable for controlled- or sustained-release. PMID:25853076

  8. Kinetics of degradation of imidapril hydrochloride in finished dosage formulations.

    PubMed

    Stanisz, Beata; Regulska, Katarzyna

    2013-01-01

    This study investigates the impact of relative air humidity and temperature on the stability of imidapril hydrochloride (IMD) tablets. For this purpose the forced degradation test was used and the following environmental conditions were employed: RH = 76.4% and the temperature range of 313 - 333 K. For the determination of IMD content in the analyzed samples a reversed-phase high performance liquid chromatography (RP-HPLC) technique was used. Three series of tablets were prepared: whole-blistered tablets, whole-bare tablets and halved-bare tablets, in order to analyze the influence of different in-home storage habits on IMD tablets' quality. In the course of the study, the degradation of IMD was observed in each series of tablets. The kinetic mechanisms and the thermodynamic parameters of these reactions were established. It was evidenced that halved IMD tablets stored without immediate packaging retain their quality only for 12 days while tablets stored according to label recommendations are stable for 513 days. PMID:23923397

  9. Cinchocaine hydrochloride determination by atomic absorption spectrometry and spectrophotometry.

    PubMed

    Abdel-Ghani, Nour T; Youssef, Ahmed F A; Awady, Mohamed A

    2005-05-01

    Two sensitive spectrophotometric and atomic absorption spectrometric procedures have been developed for determination of cinchocaine hydrochloride (Cin.Cl) in pure form and in pharmaceutical formulation. The spectrophotometric method was based on formation of an insoluble colored ion-associate between the cited drug and tetrathiocyanatocobaltate (CoTC) or hexathiocyanatochromate (CrTC) which dissolved and extracted in an organic solvent. The optimal experimental conditions for quantitative extraction such as pH, concentration of the reagents and solvent were studied. Toluene and iso-butyl alcohol proved to be the most suitable solvents for quantitative extraction of Cin-CoTC and Cin-CrTC ion-associates with maximum absorbance at 620 and 555 nm, respectively. The optimum concentration ranges, molar absorptivities, Ringbom ranges and Sandell sensitivities were also evaluated. The atomic absorption spectrometric method is based on measuring of the excess cobalt or chromium in the aqueous solution, after precipitation of the drug, at 240.7 and 357.9 nm, respectively. Linear application ranges, characteristic masses and detection limits were 57.99-361.9, 50.40 and 4.22 microg ml(-1) of Cin.Cl, in case of CoTC, while 37.99-379.9, 18.94 and 0.81 microg ml(-1) in case of CrTC. PMID:15910814

  10. Conformation and interactions of dopamine hydrochloride in solution

    SciTech Connect

    Callear, Samantha K.; Imberti, Silvia; Johnston, Andrew; McLain, Sylvia E.

    2015-01-07

    The aqueous solution of dopamine hydrochloride has been investigated using neutron and X-ray total scattering data together with Monte-Carlo based modelling using Empirical Potential Structure Refinement. The conformation of the protonated dopamine molecule is presented and the results compared to the conformations found in crystal structures, dopamine-complexed protein crystal structures and predicted from theoretical calculations and pharmacophoric models. It is found that protonated dopamine adopts a range of conformations in solution, highlighting the low rotational energy barrier between different conformations, with the preferred conformation being trans-perpendicular. The interactions between each of the species present (protonated dopamine molecules, water molecules, and chloride anions) have been determined and are discussed with reference to interactions observed in similar systems both in the liquid and crystalline state, and predicted from theoretical calculations. The expected strong hydrogen bonds between the strong hydrogen bond donors and acceptors are observed, together with evidence of weaker CH hydrogen bonds and π interactions also playing a significant role in determining the arrangement of adjacent molecules.

  11. Echocardiographic reference values in healthy cats sedated with ketamine hydrochloride.

    PubMed

    Fox, P R; Bond, B R; Peterson, M E

    1985-07-01

    An M-mode echocardiographic examination was performed in a consistent manner in 30 clinically healthy cats under light ketamine hydrochloride sedation. There was a significant linear relationship between increasing body size and increasing cardiac dimensions for several echocardiographic values. Positive correlation existed between body weight and body surface area with aortic root, left ventricular caudal wall thickness (LVCW), interventricular septal thickness (IVS), IVS/LVCW, and mean velocity of circumferential fiber shortening (Vcf); there was a negative correlation between body weight and body surface area with left ventricular ejection time (LVET). Body surface area also correlated positively with percentage of ventricular minor axis dimensional change (% delta D). Positive correlations were recorded between left ventricular end-diastolic dimension (LVEDD) and left ventricular endsystolic dimension (LVESD), LVESD and LVET, LVCW and IVS, LVET (calculated by LVCW motion) and LVET (calculated by aortic valve motion), % delta D and Vcf, heart rate and Vcf, and Vcf (calculated using aortic valve motion to compute LVET) and Vcf (using LVCW motion to compute LVET). There were negative correlations between LVEDD and % delta D, LVEDD and Vcf, LVESD and Vcf, LVET and Vcf, LVET and heart rate, LVET and % delta D. Significant differences were recorded between means of echocardiographic reference values generated in this and other studies, except for LVESD. PMID:4026030

  12. Preliminary toxicological report of metformin hydrochloride loaded polymeric nanoparticles.

    PubMed

    Lekshmi, Unnikrishnan Meenakshi Dhana; Reddy, Pully Neelakanta

    2012-09-01

    Nanosized materials have tremendous application in every field of human activity, with a lot of economic benefit increasing nanoparticle research and use. There are number of nanosized products already available commercially and many others are in queue. Therefore, there is a pressing need for careful consideration of benefits and side effects of the use of nanoparticles in medicine. This research work aims at providing a balanced update of this exciting potentially toxicological effect of manufactured Metformin hydrochloride loaded polymeric nanoparticles. To assess the toxicities systematically on the functions of various tissues and organs in rats, the rats were fed with the manufactured polymeric nanoparticles for a period of 30 days repeated oral administration. Variation in the protein, carbohydrate and fat metabolic profile of the rat exposed to nanoparticles were studied by hematobiochemical and pathology profiles. The haemolytic potential of these nanoparticles were determined by means of an in vitro haemolysis assay. All formulations showed haemolytic effect less than 5%. The study revealed that Metformin loaded PMMA and PLGA polymeric nanoparticle did not produce any toxicity. PMID:23293465

  13. [Effect of flunarizine hydrochloride on striatal D-2 dopamine receptors].

    PubMed

    Ogawa, N; Asanuma, M; Takayama, H; Sato, H; Nukina, I

    1990-11-01

    Flunarizine hydrochloride (FZ) is used to improve cerebral circulation and possesses Ca antagonistic effects. In recent years, this drug has been reported to induce parkinsonism and depressive symptoms as side effects, particularly in the elderly. Effects of FZ on dopamine receptors of the rat striatum were studied by radiolabeled receptor assay to clarify the mechanism of onset of parkinsonism in response to FZ. FZ was found to directly and competitively affect D-2 receptors without affecting D-1 receptors. Furthermore, the effect of FZ on D-2 receptors was found to be antagonistic based on the finding that the displacement curve for FZ in the binding of [3H]spiperone to D-2 receptors remained unchanged even after the addition of GppNHp. The effect of FZ on the D-2 receptors in aged rats was more marked than that in young-adult rats. In addition, the tertiary structures of FZ and the anti-schizophrenic agents, pimozide and haloperidol, were examined using computer graphics. FZ was found to have a tertiary structure highly analogous to pimozide and haloperidol, and FZ also had an alkyl structure linking a fluorophenyl group and a nitrogen atom, believed to be particularly necessary for the binding of anti-schizophrenic agents to D-2 receptors. These results may contribute to clarifying the mechanism of onset of parkinsonism in response to FZ, especially in the elderly. PMID:2150791

  14. Adsorption behavior of epirubicin hydrochloride on carboxylated carbon nanotubes.

    PubMed

    Chen, Zhe; Pierre, Dramou; He, Hua; Tan, Shuhua; Pham-Huy, Chuong; Hong, Hao; Huang, Jilong

    2011-02-28

    The aim of this study was to understand the interaction between carboxylated carbon nanotubes (c-CNTs) and anticancer agents and evaluate the drug-loading ability of c-CNTs. We prepared carboxylated multi-walled carbon nanotubes (c-MWNTs) with nitric acid treatment, then evaluated the adsorption ability of c-MWNTs as adsorbents for loading of the anticancer drug, epirubicin hydrochloride (EPI), and investigated the adsorption behavior of EPI on c-MWNTs. Unmodified multi-walled carbon nanotubes (MWNTs) and single-walled carbon nanotubes (SWNTs) were included as comparative adsorbents. The results showed that carbon nanotubes were able to form supramolecular complexes with EPI via π-π stacking and possessed favorable loading properties as drug carriers. The Freundilich adsorption model was successfully employed to describe the adsorption process. Because of the high surface area and hydrogen bonding, c-MWNTs' adsorption efficiency was the highest and the most stable and their drug-loading capacity was superior to that of MWNTs. With the increase of pH, the adsorption capacity of EPI on the c-MWNTs increased. Low-temperature facilitated the adsorption. More rapid EPI adsorption rate and higher drug-loading ability were observed from c-MWNTs with smaller diameter. Moreover, the adsorption kinetics of EPI on c-MWNTs could be well depicted by using the pseudo-second-order kinetic model. PMID:21145959

  15. Release Kinetics of Papaverine Hydrochloride from Tablets with Different Excipients

    PubMed Central

    Kasperek, Regina; Polski, Andrzej; Zimmer, Łukasz; Poleszak, Ewa

    2014-01-01

    Abstract The influence of excipients on the disintegration times of tablets and the release of papaverine hydrochloride (PAP) from tablets were studied. Ten different formulations of tablets with PAP were prepared by direct powder compression. Different binders, disintegrants, fillers, and lubricants were used as excipients. The release of PAP was carried out in the paddle apparatus using 0.1 N HCl as a dissolution medium. The results of the disintegration times of tablets showed that six formulations can be classified as fast dissolving tablets (FDT). FDT formulations contained Avicel PH 101, Avicel PH 102, mannitol, (3-lactose, PVP K 10, gelatinized starch (CPharmGel), Prosolv Easy Tab, Prosolv SMCC 90, magnesium stearate, and the addition of disintegrants such as AcDiSol and Kollidon CL. Drug release kinetics were estimated by the zero- and first-order, Higuchi release rate, and Korsmeyer-Peppas models. Two formulations of the tablets containing PVP (K10) (10%), CPharmGel (10% and 25%), and Prosolv Easy Tab (44% and 60%) without the addition of a disintegrant were well-fitted to the kinetics models such as the Higuchi and zero-order, which are suitable for controlled- or sustained-release. PMID:25853076

  16. Control of self-assembly through the influence of terminal hydroxymethyl groups on the metal coordination of pyrimidine-hydrazone Cu(II) complexes.

    PubMed

    Hutchinson, Daniel J; Hanton, Lyall R; Moratti, Stephen C

    2010-07-01

    The synthesis and characterization of 6-hydroxymethylpyridine-2-carboxaldehyde (2-methyl-pyrimidine-4,6-diyl)bis(1-methylhydrazone) (1) is reported. Ligand 1 was designed as a ditopic pyrimidine-hydrazone molecular strand with hydroxymethyl groups attached to the terminal pyridine rings. Coordination of 1 with Cu(ClO(4))(2) x 6 H(2)O or Cu(SO(3)CF(3))(2) x 4 H(2)O in a 1:2 molar ratio resulted in the dinuclear Cu(II) complexes [Cu(2)1(CH(3)CN)(4)](ClO(4))(4) x CH(3)CN (4) and [Cu(2)1(SO(3)CF(3))(2)(CH(3)CN)(2)](SO(3)CF(3))(2) x CH(3)CN (5). X-ray crystallography and (1)H NMR NOESY experiments showed that 1 adopted a horseshoe shape with both pyrimidine-hydrazone (pym-hyz) bonds in a transoid conformation, while 4 and 5 were linear in shape, with both pym-hyz bonds in a cisoid conformation. Coordination of 1 with Cu(ClO(4))(2) x 6 H(2)O or Cu(SO(3)CF(3))(2) x 4 H(2)O in a 1:1 molar ratio resulted in three different bent complexes, [Cu(1H)(ClO(4))(2)](ClO(4)) (6), [Cu(1H)(CH(3)CN)](ClO(4))(3) x 0.5 H(2)O (7), and [Cu1(SO(3)CF(3))](2)(SO(3)CF(3))(2) x CH(3)CN (8), where the pym-hyz bond of the occupied coordination site adopted a cisoid conformation, while the pym-hyz bond of the unoccupied site retained a transoid conformation. Both 6 and 7 showed protonation of the pyridine nitrogen donor in the empty coordination site; complex 8, however, was not protonated. A variety of Cu(II) coordination geometries were seen in structures 4 to 8, including distorted octahedral, trigonal bipyramidal, and square pyramidal geometries. Coordination of the hydroxymethyl arm in the mononuclear Cu(II) complexes 6, 7, and 8 appeared to inhibit the formation of a [2 x 2] grid by blocking further access to the Cu(II) coordination sphere. In addition, the terminal hydroxymethyl groups contributed to the supramolecular structures of the complexes through coordination to the Cu(II) ions and hydrogen bonding. PMID:20509604

  17. In vitro effects of Pilocarpus microphyllus extracts and pilocarpine hydrochloride on Rhipicephalus (Boophilus) microplus.

    PubMed

    Castro, Karina Neoob de Carvalho; Lima, David Fernandes; Wolschick, Dolores; Andrade, Ivanilza Moreira de; Santos, Raimunda Cardoso Dos; Santos, Francisco José de Seixas Dos; Veras, Leiz Maria Costa; Costa-Júnior, Lívio Martins

    2016-06-01

    The aim of this study was to assess the activity of aqueous (AE) and ethanolic extracts (EE) and pilocarpine hydrochloride, which were extracted and isolated from Pilocarpus microphyllus (Jaborandi), respectively, on Rhipicephalus (Boophilus) microplus. High performance liquid chromatography (HPLC) was performed to quantify these compounds. Larval packet and adult immersion tests were conducted with different concentrations. Five AE and EE concentrations, ranging from 6.2 to 100.0 mg mL-1, and six concentrations of pilocarpine hydrochloride, ranging from 0.7 to 24.0 mg mL-1, were tested. The lethal concentration (LC50) of each extract for larvae and engorged females was calculated through Probit analysis. The concentration of pilocarpine hydrochloride obtained from the EE and the AE was 1.3 and 0.3% (m/m), respectively. Pilocarpine hydrochloride presented the highest acaricidal activity on larvae (LC50 2.6 mg mL-1) and engorged females (LC50 11.8 mg mL-1) of R.(B.) microplus, followed by the EE which presented LC50 of 56.4 and 15.9 mg mL-1, for larvae and engorged females, respectively. Such results indicate that pilocarpine hydrochloride has acaricidal activity, and may be the primary compound responsible for this activity by P. microphyllus EE. PMID:27276670

  18. In vitro effects of Pilocarpus microphyllus extracts and pilocarpine hydrochloride on Rhipicephalus (Boophilus) microplus.

    PubMed

    Castro, Karina Neoob de Carvalho; Lima, David Fernandes; Wolschick, Dolores; Andrade, Ivanilza Moreira de; Santos, Raimunda Cardoso Dos; Santos, Francisco José de Seixas Dos; Veras, Leiz Maria Costa; Costa-Júnior, Lívio Martins

    2016-06-01

    The aim of this study was to assess the activity of aqueous (AE) and ethanolic extracts (EE) and pilocarpine hydrochloride, which were extracted and isolated from Pilocarpus microphyllus (Jaborandi), respectively, on Rhipicephalus (Boophilus) microplus. High performance liquid chromatography (HPLC) was performed to quantify these compounds. Larval packet and adult immersion tests were conducted with different concentrations. Five AE and EE concentrations, ranging from 6.2 to 100.0 mg mL-1, and six concentrations of pilocarpine hydrochloride, ranging from 0.7 to 24.0 mg mL-1, were tested. The lethal concentration (LC50) of each extract for larvae and engorged females was calculated through Probit analysis. The concentration of pilocarpine hydrochloride obtained from the EE and the AE was 1.3 and 0.3% (m/m), respectively. Pilocarpine hydrochloride presented the highest acaricidal activity on larvae (LC50 2.6 mg mL-1) and engorged females (LC50 11.8 mg mL-1) of R.(B.) microplus, followed by the EE which presented LC50 of 56.4 and 15.9 mg mL-1, for larvae and engorged females, respectively. Such results indicate that pilocarpine hydrochloride has acaricidal activity, and may be the primary compound responsible for this activity by P. microphyllus EE. PMID:27334829

  19. Design and development of polyethylene oxide based matrix tablets for verapamil hydrochloride.

    PubMed

    Vidyadhara, S; Sasidhar, R L C; Nagaraju, R

    2013-03-01

    In the present investigation an attempt has been made to increase therapeutic efficacy, reduced frequency of administration and improved patient compliance by developing controlled release matrix tablets of verapamil hydrochloride. Verapamil hydrochloride was formulated as oral controlled release matrix tablets by using the polyethylene oxides (Polyox WSR 303). The aim of this study was to investigate the influence of polymer level and type of fillers namely lactose (soluble filler), swellable filler (starch 1500), microcrystalline cellulose and dibasic calcium phosphate (insoluble fillers) on the release rate and mechanism of release for verapamil hydrochloride from matrix tablets prepared by direct compression process. Higher polymeric content in the matrix decreased the release rate of drug. On the other hand, replacement of lactose with anhydrous dibasic calcium phosphate and microcrystalline cellulose has significantly retarded the release rate of verapamil hydrochloride. Biopharmaceutical evaluation of satisfactory formulations were also carried out on New Zealand rabbits and parameters such as maximum plasma concentration, time to reach peak plasma concentration, area under the plasma concentration time curve(0-t) and area under first moment curve(0-t) were determined. In vivo pharmacokinetic study proves that the verapamil hydrochloride from matrix tablets showed prolonged release and were be able to sustain the therapeutic effect up to 24 h. PMID:24019567

  20. HPLC study on the stability of bendamustine hydrochloride immobilized onto polyphosphoesters.

    PubMed

    Pencheva, Ivanka; Bogomilova, Anita; Koseva, Neli; Obreshkova, Danka; Troev, Kolio

    2008-12-01

    Novel water soluble polymer complexes of bendamustine hydrochloride, a bifunctional alkylating agent with antimetabolic and cytotoxic activity, were developed using biodegradable polymer carriers-poly(oxyethylene H-phosphonate), poly(methyloxyethylene phosphate) and poly(hydroxyoxyethylene phosphate). Bendamustine hydrochloride was immobilized onto polyphosphoesters via covalent, ionic and hydrogen bonding. The structure of the complexes formed was elucidated by (1)H, (13)C, (31)P NMR and FT-IR spectroscopy. The chemical stability of bendamustine hydrochloride in the novel complexes was studied by HPLC analysis based on a validated method with appointed analytical parameters such as specificity, repeatability, limit of quantitation, limit of detection and linearity. The results from the HPLC indicate that in neutral (pH 7) and alkaline (pH 9) media bendamustine hydrochloride in the polymer complexes is more stable than the pure bendamustine hydrochloride. The enhanced stability of the immobilized drug is explained with the drug interaction with the polymer carriers or their degradation products. PMID:18926656

  1. 40 CFR 721.1025 - Benzenamine, 4-chloro-2-methyl-; benzenamine, 4-chloro-2-methyl-, hydrochloride; and ben-zenamine...

    Code of Federal Regulations, 2010 CFR

    2010-07-01

    ... 40 Protection of Environment 30 2010-07-01 2010-07-01 false Benzenamine, 4-chloro-2-methyl-; benzenamine, 4-chloro-2-methyl-, hydrochloride; and ben-zenamine, 2-chloro-6-methyl-. 721.1025 Section 721... Benzenamine, 4-chloro-2-methyl-; benzenamine, 4-chloro-2-methyl-, hydrochloride; and ben-zenamine,...

  2. 40 CFR 721.1025 - Benzenamine, 4-chloro-2-methyl-; benzenamine, 4-chloro-2-methyl-, hydrochloride; and ben-zenamine...

    Code of Federal Regulations, 2011 CFR

    2011-07-01

    ... 40 Protection of Environment 31 2011-07-01 2011-07-01 false Benzenamine, 4-chloro-2-methyl-; benzenamine, 4-chloro-2-methyl-, hydrochloride; and ben-zenamine, 2-chloro-6-methyl-. 721.1025 Section 721... Benzenamine, 4-chloro-2-methyl-; benzenamine, 4-chloro-2-methyl-, hydrochloride; and ben-zenamine,...

  3. Pharmacokinetics of hydromorphone hydrochloride after intravenous and intramuscular administration of a single dose to American kestrels (Falco sparverius)

    USGS Publications Warehouse

    Guzman, David Sanchez-Migallon; KuKanich, Butch; Drazenovich, Tracy L.; Olsen, Glenn H.; Paul-Murphy, Joanne R.

    2014-01-01

    Results indicated hydromorphone hydrochloride had high bioavailability and rapid elimination after IM administration, with a short terminal half-life, rapid plasma clearance, and large volume of distribution in American kestrels. Further studies regarding the effects of other doses, other administration routes, constantrate infusions, and slow release formulations on the pharmacokinetics of hydromorphone hydrochloride and its metabolites in American kestrels may be indicated.

  4. Synthesis, antitumor activity and mechanism of action of novel 1,3-thiazole derivatives containing hydrazide-hydrazone and carboxamide moiety.

    PubMed

    He, Haifeng; Wang, Xiaoyan; Shi, Liqiao; Yin, Wenyan; Yang, Ziwen; He, Hongwu; Liang, Ying

    2016-07-15

    A series of novel 2,4,5-trisubstituted 1,3-thiazole derivatives containing hydrazide-hydrazine, and carboxamide moiety including 46 compounds T were synthesized, and evaluated for their antitumor activity in vitro against a panel of five human cancer cell lines. Eighteen title compounds T displayed higher inhibitory activity than that of 5-Fu against MCF-7, HepG2, BGC-823, Hela, and A549 cell lines. Especially, T1, T26 and T38 exhibit best cytotoxic activity with IC50 values of 2.21μg/mL, 1.67μg/mL and 1.11μg/mL, against MCF-7, BCG-823, and HepG2 cell lines, respectively. These results suggested that the combination of 1,3-thiazole, hydrazide-hydrazone, and carboxamide moiety was much favorable to cytotoxicity activity. Furthermore, the flow cytometry analysis revealed that compounds T1 and T38 could induce apoptosis in HepG2 cells, and it was confirmed T38 led the induction of cell apoptosis by S cell-cycle arrest. PMID:27262600

  5. Interaction of Di-2-pyridylketone 2-pyridine Carboxylic Acid Hydrazone and Its Copper Complex with BSA: Effect on Antitumor Activity as Revealed by Spectroscopic Studies.

    PubMed

    Li, Cuiping; Huang, Tengfei; Fu, Yun; Liu, Youxun; Zhou, Sufeng; Qi, Zhangyang; Li, Changzheng

    2016-01-01

    The drug, di-2-pyridylketone-2-pyridine carboxylic acid hydrazone (DPPCAH) and its copper complex (DPPCAH-Cu) exhibit significant antitumor activity. However, the mechanism of their pharmacological interaction with the biological molecule bovine serum albumin (BSA) remains poorly understood. The present study elucidates the interactions between the drug and BSA through MTT assays, spectroscopic methods and molecular docking analysis. Our results indicate that BSA could attenuate effect on the cytotoxicity of DPPCAH, but not DPPCAH-Cu. Data from fluorescence quenching measurements demonstrated that both DPPCAH and DPPCAH-Cu could bind to BSA, with a reversed effect on the environment of tryptophan residues in polarity. CD spectra revealed that the DPPCAH-Cu exerted a slightly stronger effect on the secondary structure of BSA than DPPCAH. The association constant of DPPCAH with BSA was greater than that of DPPCAH-Cu. Docking studies indicated that the binding of DPPCAH to BSA involved a greater number of hydrogen bonds compared to DPPCAH-Cu. The calculated distances between bound ligands and tryptophans in BSA were in agreement with fluorescence resonance energy transfer results. Thus, the binding affinity of the drug (DPPCAH or DPPCAH-Cu) with BSA partially contributes to its antitumor activity; the greater the drug affinity is to BSA, the less is its antitumor activity. PMID:27136517

  6. Mono- and binuclear copper(II) complexes of new hydrazone ligands derived from 4,6-diacetylresorcinol: Synthesis, spectral studies and antimicrobial activity

    NASA Astrophysics Data System (ADS)

    Shebl, Magdy; El-ghamry, Mosad A.; Khalil, Saied M. E.; Kishk, Mona A. A.

    Two new hydrazone ligands, H2L1 and H2L2, were synthesized by the condensation of 4,6-diacetylresorcinol with 3-hydrazino-5,6-diphenyl-1,2,4-triazine and isatin monohydrazone, respectively. The structures of the ligands were elucidated by elemental analyses, IR, 1H NMR, electronic and mass spectra. Reactions of the ligands with several copper(II) salts, including AcO-, NO3-, SO42-, Cl- and Br- afforded mono- and binuclear metal complexes. Also, the ligands were allowed to react with Cu(II) ion in the presence of a secondary ligand (L‧) [N,O-donor; 8-hydroxyquinoline, N,N-donor; 1,10-phenanthroline or O,O-donor; benzoylacetone]. Characterization and structure elucidation of the prepared complexes were achieved by elemental and thermal analyses, IR, electronic, mass and ESR spectra as well as conductivity and magnetic susceptibility measurements. The ESR spin Hamiltonian parameters of some complexes were calculated. The spectroscopic data showed that the H2L1 ligand acts as a neutral or monobasic tridentate ligand while the H2L2 ligand acts as a bis(monobasic tridentate) ligand. The coordination sites with the copper(II) ion are phenolic oxygen, azomethine nitrogen and triazinic nitrogen (H2L1 ligand) or isatinic oxygen (H2L2 ligand). The metal complexes exhibited octahedral and square planar geometrical arrangements depending on the nature of the anion. The ligands and some metal complexes showed antimicrobial activity.

  7. [Synthesis and antituberculosis activity of the derivatives of glycoside steviolbioside from the plant Stevia rebaudiana and diterpenoid isosteviol containing hydrazone, hydrazide and pyridinoyl moieties].

    PubMed

    Kataev, V E; Strobykina, I Iu; Andreeva, O V; Garifullin, B F; Sharipova, R R; Mironov, V F; Chestnova, R V

    2011-01-01

    Conjugates of antitubercular drug Isoniazid (hydrazide of isonicotinic acid), nicotinic and alpha-picolinic acid hydrazides and glycoside steviolbioside from the plant Stevia rebaudiana as well as the product of its acid hydrolysis, diterpenoid isosteviol, were synthesized. Besides, isosteviol hydrazide and hydrazone derivatives as well as conjugates containing two isosteviol moieties connected by dihydrazide linker were also obtained. Both initial compounds and their synthetic derivatives inhibit the growth of Mycobacterium tuberculosis (H37Rv in vitro). The minimum concentration at which the growth of M. tuberculosis was inhibited by 100% (MIC) for stevioside and steviolbioside equals 7.5 and 3.8 microg/mL, respectively. MIC values for conjugates of the hydrazides of pyridine carbonic acids and steviolbioside as well as isosteviol are in the ranges 5-10 and 10-20 microg/mL, respectively. Maximum inhibitory effect against M. tuberculosis showed the conjugates of isosteviol and adipic acid dihydrazide (MIC values ranged from 1.7 to 3.1 microg/mL). Antitubercular activity of the compounds studied is higher than the activity of antitubercular drug Pyrizanamide (MIC = 12.5-20 microg/mL) but lower than the activity of antitubercular drug Isoniazid (MIC = 0.02-0.04 microg/mL). PMID:22096997

  8. Tautomeric effect of hydrazone Schiff bases in tetranuclear Cu(II) complexes: magnetism and catalytic activity towards mild hydrocarboxylation of alkanes.

    PubMed

    Sutradhar, Manas; Kirillova, Marina V; Guedes da Silva, M Fátima C; Liu, Cai-Ming; Pombeiro, Armando J L

    2013-12-21

    Three new tetranuclear copper(II) complexes [Cu(HL(1))]4·4EtOH (1·4EtOH), [Cu(HL(2))]4 (2) and [Cu(H2L(3))]4(NO3)4·2H2O (3·2H2O) have been synthesized using three different hydrazone Schiff base ligands derived from the condensation of the aromatic acid hydrazides 2-hydroxybenzo-, 2-aminobenzo- or benzo-hydrazide, with 2,3-dihydroxybenzaldehyde. Complexes 1 and 3 have been characterized by single crystal X-ray diffraction analysis. The coordinating behaviour of the ligand depends on the nature of the ortho substituent present in the hydrazide moiety. The ligands bearing a strong electron donating group (by resonance) in the ortho position undergo complexation via enolization and deprotonation, whereas the absence of such an effect leads to complexation via the keto form, and two different types of tetranuclear Cu(II) clusters, viz. open-cubane and cubane, are obtained. Variable temperature magnetic susceptibility measurements of complexes 1 and 3 have been carried out to examine the nature of magnetic interaction between the Cu(II) centres. All the three complexes (1-3) act as good catalyst precursors towards mild hydrocarboxylation of linear and cyclic alkanes into carboxylic acids in water-acetonitrile medium. PMID:24068161

  9. Spectroscopic and biological studies of new mononuclear metal complexes of a bidentate NN and NO hydrazone-oxime ligand derived from egonol.

    PubMed

    Babahan, Ilknur; Emirdağ-Öztürk, Safiye; Poyrazoğlu-Çoban, Esin

    2015-04-15

    A novel ligand, vicinal dioxime ligand (egonol-hydrazone glyoxime) (LH2) was synthesized and characterized using (1)H NMR, (13)C NMR, MS, AAS, infrared spectroscopy, and magnetic susceptibility measurements. Mononuclear nickel (II), copper (II) and cobalt (II) complexes with a metal:ligand ratio of 1:2 for LH2 were also synthesized. Zn(II) forms complex [Zn(LH)Cl2] with a metal to ligand ratio of 1:1. IR spectrum shows that the ligand act in a bidentate manner and coordinates N4 donor groups of the ligands to Ni(II), Cu(II), Co(II) and Zn(II) ions. The detection of H-bonding (OH⋯O) in the [M(LH)2] metal complexes by IR spectra supported the square-planar MN4 coordination of Ni(II), Cu(II) and Co(II) complexes. The antimicrobial activities of compounds LH2 and their Ni(II), Cu(II), Co(II) and Zn(II) complexes were evaluated using the disc diffusion method against 16 bacteria and 5 yeasts. The minimal inhibitory concentrations (MICs) against all the bacteria and yeasts were also determined. Among the attempted test compounds, it is showed that all the compounds (L, LH2, [Ni(LH)2], [Cu(LH)2], [Co(LH)2(H2O)2], [Zn(LH)Cl2]) were effective against used test microorganisms. PMID:25686861

  10. Spectroscopic and biological studies of new mononuclear metal complexes of a bidentate NN and NO hydrazone-oxime ligand derived from egonol

    NASA Astrophysics Data System (ADS)

    Babahan, Ilknur; Emirdağ-Öztürk, Safiye; Poyrazoğlu-Çoban, Esin

    2015-04-01

    A novel ligand, vicinal dioxime ligand (egonol-hydrazone glyoxime) (LH2) was synthesized and characterized using 1H NMR, 13C NMR, MS, AAS, infrared spectroscopy, and magnetic susceptibility measurements. Mononuclear nickel (II), copper (II) and cobalt (II) complexes with a metal:ligand ratio of 1:2 for LH2 were also synthesized. Zn(II) forms complex [Zn(LH)Cl2] with a metal to ligand ratio of 1:1. IR spectrum shows that the ligand act in a bidentate manner and coordinates N4 donor groups of the ligands to NiII, CuII, CoII and ZnII ions. The detection of H-bonding (Osbnd H⋯O) in the [M(LH)2] metal complexes by IR spectra supported the square-planar MN4 coordination of Ni(II), Cu(II) and Co(II) complexes. The antimicrobial activities of compounds LH2 and their Ni(II), Cu(II), Co(II) and Zn(II) complexes were evaluated using the disc diffusion method against 16 bacteria and 5 yeasts. The minimal inhibitory concentrations (MICs) against all the bacteria and yeasts were also determined. Among the attempted test compounds, it is showed that all the compounds (L, LH2, [Ni(LH)2], [Cu(LH)2], [Co(LH)2(H2O)2], [Zn(LH)Cl2]) were effective against used test microorganisms.

  11. Synthesis, crystal structure and DNA-binding studies of the Ln(III) complex with 6-hydroxychromone-3-carbaldehyde benzoyl hydrazone.

    PubMed

    Wang, Bao-dui; Yang, Zheng-Yin; Crewdson, Patrick; Wang, Da-qi

    2007-10-01

    A novel 6-hydroxy chromone-3-carbaldehyde benzoyl hydrazone ligand (L) and its Ln(III) complexes, [Ln=La(1) and Sm(2)], have been prepared and characterized. The crystal and molecular structures of complexes 1 and 2 were determined by single-crystal X-ray diffraction. Antioxidative activity tests in vitro showed that L and its complexes have significant antioxidative activity against hydroxyl free radicals from the Fenton reaction and also oxygen free radicals, and that the effect of the La(III) complex 1 is stronger than that of mannitol and the other compounds. The compounds were tested against tumor cell lines including HL-60 and A-549. The data shows that the suppression rate of complexes 1 and 2 against the tested tumor cells are superior to the free ligand (L). The interactions of complexes 1 and 2, and L, with calf thymus DNA were investigated by UV-visible (UV-vis), fluorescence, denaturation experiments and viscosity measurements. Experimental results indicated that complexes 1 and 2, and L can bind to DNA via the intercalation mode, and that the binding affinity of complex 1 is higher than that of complex 2 and of free ligand (L). The intrinsic binding constants of complexes 1 and 2, and L were (7.62+/-0.56)x10(6), (3.70+/-0.47)x10(6) and (2.41+/-0.46)x10(6)M(-1), respectively. PMID:17692381

  12. Reactivity Differences between [alpha, beta]-Unsaturated Carbonyls and Hydrazones Investigated by Experimental and Theoretical Electron Density and Electron Localizability Analyses

    SciTech Connect

    Grabowsky, Simon; Weber, Manuela; Jayatilaka, Dylan; Chen, Yu-Sheng; Grabowski, Matthias T.; Brehme, Rainer; Hesse, Malte; Schirmeister, Tanja; Luger, Peter

    2012-10-11

    It is still a challenge to predict a compound's reactivity from its ground-state electronic nature although Bader-type topological analyses of the electron density (ED) and electron localizability indicator (ELI) give detailed and useful information on electron concentration and electron-pair localization, respectively. Both ED and ELI can be obtained from theoretical calculations as well as high-resolution X-ray diffraction experiments. Besides ED and ELI descriptors, the delocalization index is used here; it is likewise derived from theoretical calculations as well as from experimental X-ray results, but in the latter case, demonstrated here for the first time. We investigate {alpha},{beta}-unsaturated carbonyl and hydrazone compounds because resonance exhibited by these compounds in the electronic ground-state determines their reactive behavior. The degree of resonance as well as the reactivity contrast are quantified with the electronic descriptors. Moreover, competitive mesomeric substituent effects are studied using the two biologically important compounds acrolein and acrylamide. The reactivity differences predicted from the analyses are in line with the known reactivity of these compounds in organic synthesis. Hence, the capability of the ED and ELI for rationalizing and predicting different and competing substituent effects with respect to reactivity is demonstrated.

  13. Effect of the protonophore carbonyl cyanide-p-trifluoromethoxyphenyl-hydrazon on the glutamate release from rat brain nerve terminals under altered gravity conditions.

    NASA Astrophysics Data System (ADS)

    Borisova, T.; Krisanova, N.

    L-glutamate acts within the mammalian central nervous system as the predominant excitatory neurotransmitter and as a potent neurotoxin The balance between these physiological and pathological actions of glutamate is thought to be kept in check by the rapid removal of the neurotransmitter from the synaptic cleft The majority of uptake is mediated by the high-affinity Na -dependent glutamate transporters Depolarization leads to stimulation of glutamate efflux mediated by reversal of the high-affinity glutamate transporters The effects of the protonophore carbonyl cyanide-p-trifluoromethoxyphenyl-hydrazon FCCP on the glutamate release from isolated nerve terminals rat brain synaptosomes were investigated in control and after centrifuge-induced hypergravity rats were rotated in a long-arm centrifuge at ten-G during one-hour period The treatment of synaptosomes with 1 mu M FCCP during 11 min resulted in the increase in L- 14 C glutamate release by 23 0 pm 2 3 of total accumulated synaptosomal label in control animals and 24 0 pm 2 3 animals subjected to hypergravity FCCP evoked release of L- 14 C glutamate from synaptosomes was not altered in animals exposed to hypergravity as compared to control Glutamate transport is of electrogenic nature and thus depends on the membrane potential The high-KCl stimulated L- 14 C glutamate release in Ca 2 -free media occurred due to reversal of the glutamate transporters Carrier --mediated release of L- 14 C glutamate 6 min slightly increased as a result of

  14. Identification of impurities and statistical classification of methamphetamine hydrochloride drugs seized in the China

    PubMed Central

    Zhang, Jian Xin; Zhang, Da Ming; Han, Xu Guang

    2008-01-01

    A total of 48 methamphetamine hydrochloride samples from eight seizures were analyzed using gas chromatography–mass spectrometry (GC–MS) and a flame ionization detector (GC–FID). Major impurities detected include 1,2-dimethyl-3-phenylaziridine, Ephedrine/pseudoephedrine, 1,3-dimethyl-2-phenylnaphthalene, 1-benzyl-3-methylnaphthalene. These data are suggestive of ephedrine/pseudoephedrine as the main precursor of the methamphetamine hydrochloride samples seized during 2006–2007. Additionally the presence of 1,3-dimethyl-2-phenylnaphthalene, 1-benzyl-3-methylnaphthalene is indicative that six seizures were synthesized via the more specific ephedrine/hydriodic acid/red phosphorus method. In addition, five impurities were found for the first time in methamphetamine hydrochloride samples. Seventeen impurity peaks were selected from the GC–FID chromatograms. The peak areas of the selected peaks were then grouped for cluster analysis. PMID:19008060

  15. Photoacoustic imaging to detect rat brain activation after cocaine hydrochloride injection

    NASA Astrophysics Data System (ADS)

    Jo, Janggun; Yang, Xinmai

    2011-03-01

    Photoacoustic imaging (PAI) was employed to detect small animal brain activation after the administration of cocaine hydrochloride. Sprague Dawley rats were injected with different concentrations (2.5, 3.0, and 5.0 mg per kg body) of cocaine hydrochloride in saline solution through tail veins. The brain functional response to the injection was monitored by photoacoustic tomography (PAT) system with horizontal scanning of cerebral cortex of rat brain. Photoacoustic microscopy (PAM) was also used for coronal view images. The modified PAT system used multiple ultrasonic detectors to reduce the scanning time and maintain a good signal-to-noise ratio (SNR). The measured photoacoustic signal changes confirmed that cocaine hydrochloride injection excited high blood volume in brain. This result shows PAI can be used to monitor drug abuse-induced brain activation.

  16. Thermal Analysis Investigation of Dapoxetine and Vardenafil Hydrochlorides using Molecular Orbital Calculations

    PubMed Central

    Attia, Ali Kamal; Souaya, Eglal R.; Soliman, Ethar A.

    2015-01-01

    Purpose: Thermal analysis techniques have been used to study the thermal behavior of dapoxetine and vardenafil hydrochlorides and confirmed using semi-empirical molecular orbital calculations. Methods: Thermogravimetric analysis, derivative thermogravimetry, differential thermal analysis and differential scanning calorimetry were used to determine the thermal behavior and purity of the drugs under investigation. Thermodynamic parameters such as activation energy, enthalpy, entropy and Gibbs free energy were calculated. Results: Thermal behavior of DAP and VAR were confirmed using by semi-empirical molecular orbital calculations. The purity values were found to be 99.97% and 99.95% for dapoxetine and vardenafil hydrochlorides, respectively. The purity of dapoxetine and vardenafil hydrochlorides is similar to that found by reported methods according to DSC data. Conclusion: Thermal analysis justifies its application in quality control of pharmaceutical compounds due to its simplicity, sensitivity and low operational costs. PMID:26819925

  17. Impurity profiling of methamphetamine hydrochloride drugs seized in the Philippines.

    PubMed

    Dayrit, Fabian M; Dumlao, Morphy C

    2004-08-11

    Methamphetamine hydrochloride is one of the most widely used illicit drugs in the Philippines. In this study, we describe the application of cluster analysis of trace impurities in the profiling of the seized methamphetamine drug samples. Thirty milligrams of a homogenized drug sample were dissolved in 1 mL of pH 10.5 buffer solution and extracted with ethyl acetate containing three internal standards. The trace impurities were identified using gas chromatography-mass spectrometry (GC-MS) and quantified by gas chromatography with a flame ionization detector (GC-FID). Following previously reported methodologies, 30 impurity peaks were selected from the GC-FID chromatograms. The peak areas and retention times were referenced to the internal standards. The peak areas of the selected peaks were then grouped for cluster analysis. In order to check for consistency of clustering, two further cluster analyses were performed using 40 and 50 impurity peaks. Changes in clustering were observed in going from 30 to 40 impurity peaks, while analyses using 40 and 50 impurity peaks gave similar results. Thus, for the seized drug samples used in this study, cluster analysis using at least 40 impurity peaks showed better consistency of clustering as compared to analysis using 30 peaks only. Ten of the impurity peaks were identified, of which four were identified for the first time in methamphetamine drug samples. These are p-bromotoluene, N-benzyl amphetamine, N-ethyl amphetamine, and N-ethyl methamphetamine. The presence of phenyl-2-propanone (P2P), N,N-dimethyl amphetamine, and N-formyl amphetamine is indicative that these casework samples were synthesized using the Leuckart method. PMID:15240018

  18. Effect of penehyclidine hydrochloride on heart rate variability in hysteroscopy

    PubMed Central

    LIU, XIAO-BO; PAN, SHU; YANG, XI-GE; LI, ZHI-WEN; SUN, QING-SHAN; ZHAO, ZHUANG; MA, HAI-CHUN; CUI, CHENG-RI

    2015-01-01

    In order to evaluate the effect of different doses of penehyclidine hydrochloride (penehyclidine) on heart rate (HR) and HR variability (HRV) in hysteroscopy, 180 patients (American Society of Anesthesiologists grade I–II) were randomized equally to three groups: 0.5 mg penehyclidine and intravenous anesthesia (group I), 1.0 mg penehyclidine and intravenous anesthesia (group II) and saddle anesthesia combined with intravenous anesthesia (control group). HR and HRV, including total power (TP), low-frequency power (LF), high-frequency power (HF) and the LF to HF ratio (LF/HF), were recorded prior and subsequent to the induction of anesthesia (T0 and T1, respectively), following the start of surgery (T2) and following completion of surgery (T3). HR was lower at T2 than at T0 in the control patients, but no differences were observed in groups I and II. The HR at T2 was increased in group II compared with that in group I. TP in group II was significantly higher compared with that in group I at T2. At T1 and at T2, the LF and HF values were lower in group I than those in the controls. Patients in group II also had higher LF and HF at T2 than patients in group I. The HF was higher at T2 than that at T0 in the controls; however, the HF and LF did not change significantly within groups I and II. No significant differences were observed in the LF/HF ratio among the three groups. At a dose of 0.5 mg, penehyclidine stabilized HRV and did not alter the autonomic nervous modulation of HR. A penehyclidine dose of 1.0 mg may be superior to a dose of 0.5 mg in maintaining HR, but is less effective at balancing sympathetic and parasympathetic activity. PMID:26170932

  19. Retinal toxicity of chloroquine hydrochloride administered by intraperitoneal injection.

    PubMed

    Gaynes, Bruce Ira; Torczynski, Elise; Varro, Zoltan; Grostern, Richard; Perlman, Jay

    2008-10-01

    Chloroquine is quinolone derivative known to exert dose-related retinal toxicity, albeit in a variable manner. It is thought that variability in the presentation of chloroquine retinopathy may be the result of perturbations in drug bioavailability subsequent to oral ingestion. In order to better understand the ramifications of bioavailability on the development of retinal injury subsequent to chloroquine use, this study investigated the relationship between retinal injury and chloroquine administration via intraperitoneal rather than oral administration. Four-week-old C57/6J mice underwent daily intraperitoneal injection of 10 mg kg(-1) chloroquine hydrochloride for a total of 62 days. Following treatment, tissue was fixed in preparation for analysis by light and transmission electron microscopy. Treated animals demonstrated marked abnormality of the outer retinal layers described as complete loss of the outer plexiform layer as well as photoreceptors and photoreceptor nuclei. The retinal pigmented epithelium demonstrated focal atrophy, loss of nuclei and pigment irregularity. Findings in the inner retina were notable for the loss of Müller cells and the presence of membranous cytoplasmic bodies. Retinae of control animals were entirely normal. In contrast to previous studies in the murine model examining chloroquine retinopathy subsequent to oral administration, this study suggests that intraperitoneal chloroquine administration facilitates retinal toxicity, presumably due to heightened drug absorption and bioavailability. It is posited that an increased rate of drug accumulation within the retina leads to an enhanced lysosomotrophic drug effect due to inability of the lysosome to compensate for chloroquine-induced elevation in pH through re-acidification of the intra-lysosomal content. PMID:18484088

  20. Determination of phenformin hydrochloride employing a sensitive fluorescent probe.

    PubMed

    Shi, Lin; Xie, Jian-Hong; Du, Li-Ming; Chang, Yin-Xia; Wu, Hao

    2016-06-01

    A complexation of non-fluorescent phenformin hydrochloride (PFH) with cucurbit [7]uril (CB [7]) in aqueous solution was investigated using the fluorescent probe of palmatine (PAL) coupled with CB [7]. The fluorescent probe of CB [7]-PAL exhibited strong fluorescence in aqueous solution, which was quenched gradually with the increase of PFH. This effect is observed because when PFH was added to the host-guest system of CB [7]-PAL, PFH and PAL competed to occupy the CB [7] cavity. Portions of the PAL molecule were expelled from the CB [7] cavity owing to the introduction of PFH. Based on the significant quenching of the supramolecular complex fluorescence intensity, a fluorescence method of high sensitivity and selectivity was developed to determine PFH with good precision and accuracy for the first time. The linear range of the method was 0.005-1.9μgmL(-1) with a detection limit of 0.003μgmL(-1). In this work, association constants (K) of PFH with CB [7] were also determined. KCB [7]-PFH=(2.52±0.05)×10(5)Lmol(-1). The ability of PFH to bind with CB [7] is stronger than that of PAL. The results of a density functional theory calculation authenticated that the moiety of PFH was embedded in the hydrophobic cavity of CB [7] tightly, and the nitrogen atom is located in the vicinity of a carbonyl-laced portal in the energy-minimized structure. The molecular modelling of the interaction between PFH and CB [7] was also confirmed by (1)H NMR spectra (Bruker 600MHz). PMID:26994318

  1. Potentiometric sensor for the high throughput determination of tetramisole hydrochloride.

    PubMed

    Gupta, Vinod Kumar; Singh, Ashok Kumar; Gupta, Barkha

    2007-08-01

    The electrochemical response characteristics of poly(vinyl)chloride (PVC) based membrane sensors for determination of tetramisole hydrochloride (TmCl) is described. The membranes of these electrodes consist of tetramisole-tetraphenyl borate (Tm-TPB), chlorophenyl borate (Tm-ClPB), and phosphotungstate (Tm(3)-PT) ion associations dispersed in a PVC matrix with dibutylpthalate as a plasticizer. The electrodes were fully characterized in terms of composition, life span, usable pH range, and working concentration range and ionic strength. The electrodes showed Nernstian response over the concentration ranges of 7.4 x 10(-7) to 1.0 x 10(-2) M, 1.7 x 10(-6) to 1.0 x 10(-2) M, and 5.6 x 10(-6) to 1.0 x 10(-2) M TmCl, respectively, and were applied to the potentiometric determination of tetramisole ion in pure solutions and pharmaceutical preparations. The potentiometric determination was also used in the determination of tetramisole in pharmaceutical preparations in four batches of different expiration dates. The electrodes exhibited good selectivity for TmCl with respect to a large number of excipients such as inorganic cations, organic cations, amino acids, and sugars. The solubility product of the ion-pair and the formation constant of the precipitation reaction leading to the ion-pair formation were determined conductometrically. The new potentiometric method offers the advantages of high-throughput determination, simplicity, accuracy, automation feasibility, and applicability to turbid and colored sample solutions. PMID:17979641

  2. Determination of phenformin hydrochloride employing a sensitive fluorescent probe

    NASA Astrophysics Data System (ADS)

    Shi, Lin; Xie, Jian-Hong; Du, Li-Ming; Chang, Yin-xia; Wu, Hao

    2016-06-01

    A complexation of non-fluorescent phenformin hydrochloride (PFH) with cucurbit [7]uril (CB [7]) in aqueous solution was investigated using the fluorescent probe of palmatine (PAL) coupled with CB [7]. The fluorescent probe of CB [7]-PAL exhibited strong fluorescence in aqueous solution, which was quenched gradually with the increase of PFH. This effect is observed because when PFH was added to the host-guest system of CB [7]-PAL, PFH and PAL competed to occupy the CB [7] cavity. Portions of the PAL molecule were expelled from the CB [7] cavity owing to the introduction of PFH. Based on the significant quenching of the supramolecular complex fluorescence intensity, a fluorescence method of high sensitivity and selectivity was developed to determine PFH with good precision and accuracy for the first time. The linear range of the method was 0.005-1.9 μg mL- 1 with a detection limit of 0.003 μg mL- 1. In this work, association constants (K) of PFH with CB [7] were also determined. KCB [7]-PFH = (2.52 ± 0.05) × 105 L mol- 1. The ability of PFH to bind with CB [7] is stronger than that of PAL. The results of a density functional theory calculation authenticated that the moiety of PFH was embedded in the hydrophobic cavity of CB [7] tightly, and the nitrogen atom is located in the vicinity of a carbonyl-laced portal in the energy-minimized structure. The molecular modelling of the interaction between PFH and CB [7] was also confirmed by 1H NMR spectra (Bruker 600 MHz).

  3. Vibrational spectra of ketamine hydrochloride and 3, 4-methylenedioxymethamphetamine in terahertz range

    NASA Astrophysics Data System (ADS)

    Wang, Guangqin; Shen, Jingling; Jia, Yan

    2007-07-01

    The terahertz spectrum of ketamine hydrochloride at room temperature, in the range of 0.2-2.6THz, has been measured by terahertz time-domain spectroscopy (TDS). Full-geometry optimizations and frequency calculations using the density functional theory (DFT) are also applied to predict the absorption spectra of ketamine hydrochloride and 3, 4-methylenedioxymethamphetamine (MDMA). The results of the simulation show qualitative agreement with the experimental data especially for MDMA, and the observed spectra features are assigned based on the DFT calculation. The results suggest that use of the terahertz TDS technique can be an effective method for the detection and inspection of illicit drugs.

  4. [Effect of crystallinity on the rate of solution of oxytetracycline hydrochloride].

    PubMed

    Grakovskaia, L K; Nesterova, L Ia

    1982-11-01

    The crystal structure of 2 forms of oxytetracycline hydrochloride prepared with the method of crystallization from various solvents was studied. It was shown that these forms were 2 polymorphic modifications of the antibiotic with different crystal structures. The modification prepared with the method of crystallization from methanol was characterized by better dissolution in water. Its dissolution rate constant was 3 times as higher which makes this crystalline modification of oxytetracycline hydrochloride preferable for preparation of the antibiotic pharmaceutical forms with high bioavailability levels. PMID:7181463

  5. A validated HPTLC method for estimation of moxifloxacin hydrochloride in tablets.

    PubMed

    Dhillon, Vandana; Chaudhary, Alok Kumar

    2010-10-01

    A simple HPTLC method having high accuracy, precision and reproducibility was developed for the routine estimation of moxifloxacin hydrochloride in the tablets available in market and was validated for various parameters according to ICH guidelines. moxifloxacin hydrochloride was estimated at 292 nm by densitometry using Silica gel 60 F254 as stationary phase and a premix of methylene chloride: methanol: strong ammonia solution and acetonitrile (10:10:5:10) as mobile phase. Method was found linear in a range of 9-54 nanograms with a correlation coefficient >0.99. The regression equation was: AUC = 65.57 × (Amount in nanograms) + 163 (r(2) = 0.9908). PMID:23781417

  6. Comparative effects of zilpaterol hydrochloride and ractopamine hydrochloride on live performance and carcass characteristics of calf-fed Holstein steers.

    PubMed

    Brown, T R; Sexten, A K; Lawrence, T E; Miller, M F; Thomas, C L; Yates, D A; Hutcheson, J P; Hodgen, J M; Brooks, J C

    2014-09-01

    Holstein steers (n = 2,275) were assigned to 1 of 3 treatments: 1) a control diet containing no β-agonists, 2) a diet that contained zilpaterol hydrochloride (ZH; 8.3 mg/kg [100% DM basis]) for 20 d with a 3-d withdrawal period before harvest, and 3) a diet that contained ractopamine hydrochloride (RH; 30.1 mg/kg [100% DM basis]) for 28 d before harvest. No differences (P ≥ 0.18) were detected between treatments for initial BW, BW at d 28, or DMI. Final BW, BW gain for the last 28 d, total BW gain, ADG for the last 28 d, and overall ADG were greater (P < 0.05) for steers fed ZH or RH than for steers fed the control diet. Additionally, G:F for the last 28 d and G:F for the entire trial was increased (P < 0.02) for steers fed ZH (0.147, 0.147) or RH (0.153, 0.151) compared to steers fed the control diet (0.134, 0.143), respectively. Steers fed ZH or RH had HCW that were 15.5 and 8.2 kg heavier (P ≤ 0.01) and LM areas that were 7.1 and 2.3 cm(2) larger (P < 0.01) than control cattle. Steers fed ZH also had dressed carcass yields that were 1.3% to 1.5% greater and USDA calculated yield grades that were decreased 0.16 to 0.23 units compared to RH and control steers. No differences (P ≥ 0.39) were found between treatments for marbling score, fat thickness, and percentage KPH. Steers fed ZH had an increased (P ≤ 0.04) percentage of yield grade 1 and 2 carcasses (15.1, 55.0) and a reduced (P ≤ 0.02) percentage of yield grade 3 carcasses (27.1) compared with those fed RH (10.5, 49.1, 36.1) or the control diet (9.0, 47.4, 36.4), respectively. Additionally, ZH-fed steers had a decreased (P ≤ 0.04) percentage of yield grade 4 and 5 carcasses (2.8) compared with steers fed the control diet (6.9). Steers fed ZH had an increased (P ≤ 0.01) percentage of USDA Select grading carcass (31.0%) and a decreased (P ≤ 0.01) percentage of USDA Choice grading carcasses (65.0%) compared with steers fed RH (25.8%, 70.2%) and no β-agonist (24.8%, 72.0%), respectively. Feeding

  7. Dexmethylphenidate--Novartis/Celgene. Focalin, D-MPH, D-methylphenidate hydrochloride, D-methylphenidate, dexmethylphenidate, dexmethylphenidate hydrochloride.

    PubMed

    2002-01-01

    Celgene has developed a chirally pure form of methylphenidate (Ritalin), called dexmethylphenidate [d-methylphenidate, d-methylphenidate hydrochloride, d-MPH; Focalin]. The drug has been launched in the USA and is undergoing registration in Canada for the treatment of children with attention-deficit hyperactivity disorder (ADHD). Dexmethylphenidate is the single isomer version of racemic methylphenidate (Ritalin), which contains the active d isomer of Ritalin. Dexmethylphenidate acts via the inhibition of reuptake of norepinephrine and dopamine. Research is ongoing to further clarify the mode of therapeutic action in ADHD. Dexmethylphenidate was developed with the aim of reducing drug load, adverse events and drug interactions. Dexmethylphenidate provides effective management of attention-deficit hyperactivity disorder at half the dose of Ritalin. In April 2000, worldwide rights (excluding Canada) to dexmethylphenidate were granted to Novartis. Celgene has also granted Novartis rights to all related intellectual properties and patents. Novartis will fund all remaining development and marketing expenses required for regulatory approval and commercialisation of dexmethylphenidate. Crystaal Corporation, the marketing division of Biovail Corporation International, has exclusive Canadian marketing rights for all formulations of dexmethylphenidate. Novartis launched dexmethylphenidate (Focalin) in the USA during Q1 2002. It is available as a D-shaped tablet (2.5, 5 and 10 mg doses). Novartis had planned to use the tradename Ritadex, however the FDA recommended an alternative name due to potential prescribing errors with Ritalin. The finalized tradename to be used is Focalin. In July 2001, a new drug submission was filed with Canada's Therapeutic Products Programme for dexmethylphenidate in the treatment of attention-deficit disorder and attention-deficit hyperactivity disorder. Novartis is also developing an extended-release version of chirally pure dexmethylphenidate

  8. An evaluation of the influence of medetomidine hydrochloride and atipamezole hydrochloride on the arrhythmogenic dose of epinephrine in dogs during halothane anesthesia.

    PubMed Central

    Pettifer, G R; Dyson, D H; McDonell, W N

    1996-01-01

    Alterations in the arrhythmogenic dose of epinephrine (ADE) were determined following administration of medetomidine hydrochloride (750 micrograms/M2) and a saline placebo, or medetomidine hydrochloride (750 micrograms/M2), followed by specific medetomidine reversal agent, atipamezole hydrochloride (50 micrograms/kg) 20 min later, in halothane-anesthetized dogs (n = 6). ADE determinations were made prior to the administration of either treatment, 20 min and 4 h following medetomidine/saline or medetomidine/atipamezole administration. Epinephrine was infused for 3 min at increasing dose rates (2.5 and 5.0 micrograms/kg/min) until the arrhythmia criterion (4 or more intermittent or continuous premature ventricular contractions) was reached. The interinfusion interval was 20 min. There were no significant differences in the amount of epinephrine required to reach the arrhythmia criterion following the administration of either treatment. In addition, the ADE at each determination was not different between treatment groups. In this study, the administration of medetomidine to halothane-anesthetized dogs did not alter their arrhythmogenic response to infused epinephrine. PMID:8825986

  9. Unfolding and inactivation of cutinases by AOT and guanidine hydrochloride.

    PubMed

    Ternström, Tomas; Svendsen, Allan; Akke, Mikael; Adlercreutz, Patrick

    2005-04-15

    We present a comparative analysis of the unfolding and inactivation of three cutinases in the presence of guanidine hydrochloride (GdnHCl) and bis(2-ethylhexyl) sodium sulfosuccinate (AOT). Previous investigations have focused on the cutinase from Fusarium solani pisi (FsC). In addition to FsC, the present study includes the cutinase from Humicola insolens (HiC) and a mutant variant of HiC (muHiC) with increased activity and decreased surfactant sensitivity. Equilibrium and time-resolved denaturation by AOT were studied in aqueous solution and reverse micelles, and were compared with GdnHCl denaturation. The far-UV CD and fluorescence denaturation profiles obtained in the aqueous solutions of the two denaturants coincide for all three cutinases, indicating that unfolding is a co-operative two-state process under these conditions. In reverse micelles, the cutinases unfold with mono-exponential rates, again indicating a two-state process. The free energy of denaturation in water was calculated by linear extrapolation of equilibrium data, yielding very similar values for the three cutinases with averages of -11.6 kcal mol(-1) and -2.6 kcal mol(-1) for GdnHCl and AOT, respectively. Hence, the AOT denatured state (D(AOT)) is less destabilised than the GdnHCl denatured state (D(GdnHCl)), relative to the native state in water. Far-UV CD spectroscopy revealed that D(AOT) retains some secondary structure, while D(GdnHCl) is essentially unstructured. Similarly, fluorescence data suggest that D(AOT) is more compact than D(GdnHCl). Activity measurements reveal that both D(AOT) and D(GdnHCl) are practically inactive (catalytic activity <1% of that of the native enzyme). The fluorescence spectrum of D(AOT) in reverse micelles did not differ significantly from that observed in aqueous AOT. NMR studies of D(AOT) in reverse micelles indicated that the structure is characteristic of a molten globule, consistent with the CD and fluorescence data. PMID:15752695

  10. Performance of finishing beef steers in response to anabolic implant dose and zilpaterol hydrochloride

    Technology Transfer Automated Retrieval System (TEKTRAN)

    British × Continental steers (n = 168; 7 pens/treatment; initial BW = 362 kg) were used to evaluate the dose of trenbolone acetate (TBA) and estradiol-17ß (E2) and feeding of zilpaterol hydrochloride (ZH) on performance and carcass characteristics. A randomized complete block design was used with a ...

  11. Performance of finishing beef steers in response to anabolic implant and zilpaterol hydrochloride supplementation

    Technology Transfer Automated Retrieval System (TEKTRAN)

    Our objectives were to evaluate the dose/payout pattern of trenbolone acetate (TBA) and estradiol-17b (E2) implants and feeding of zilpaterol hydrochloride (ZH) on performance and carcass characteristics of finishing beef steers. A randomized complete block design was used with a 3 × 2 factorial arr...

  12. 78 FR 38053 - Determination That OPANA ER (Oxymorphone Hydrochloride) Drug Products Covered by New Drug...

    Federal Register 2010, 2011, 2012, 2013, 2014

    2013-06-25

    ...The Food and Drug Administration (FDA) has determined that OPANA ER (oxymorphone hydrochloride (HCl)) Extended-Release Tablet products approved under new drug application (NDA) 21-610 were not withdrawn from sale for reasons of safety or effectiveness. This determination means that FDA will not begin procedures to withdraw approval of abbreviated new drug applications (ANDAs) that refer to......

  13. Interaction of heparin sodium and dopamine hydrochloride in admixtures studied by microcalorimetry.

    PubMed

    Pereira-Rosario, R; Utamura, T; Perrin, J H

    1988-06-01

    Microcalorimetry was used to investigate the interaction between dopamine hydrochloride and heparin sodium in 5% dextrose injection and in 0.9% sodium chloride injection. Heat of reaction (in microjoules) was measured by flow calorimetry for the following combinations of solutions: dopamine hydrochloride solution and heparin sodium solution prepared from powdered forms of the drugs in water; solutions of the powdered drugs in 5% dextrose injection; solutions of the powdered drugs in 0.9% sodium chloride injection; solutions prepared in 5% dextrose injection from commercial dopamine hydrochloride injection and commercial heparin sodium injection; and solutions prepared in 0.9% sodium chloride injection from the commercial drug injections. Mixing the solutions of the powdered drugs in water caused heat to be evolved, as did mixing the solutions of the powdered drugs diluted with 5% dextrose injection and the commercial injections diluted with 5% dextrose injection. The interactions of the two drugs were believed to be ionic, based on the exothermic nature of the reaction. No heat of reaction was measurable when sodium chloride was used as the diluent. Based on this preliminary investigation, admixtures containing heparin sodium and dopamine hydrochloride should be mixed in 0.9% sodium chloride injection to minimize the risk of interaction between the two drugs. PMID:3414704

  14. Quantitative HPLC Analysis of a Psychotherapeutic Medication: Simultaneous Determination of Amitriptyline Hydrochloride and Perphenazine

    NASA Astrophysics Data System (ADS)

    Ferguson, Glenda K.

    1998-12-01

    A quantitative high-performance liquid chromatography (HPLC) laboratory experiment which entails the isocratic separation and simultaneous determination of the two active components of a commercial antipsychotic tablet has been developed. The prescription formulation used in this experiment contains amitriptyline hydrochloride (a tricyclic antidepressant) and perphenazine (a tranquilizer). Our experiment makes use of a straightforward HPLC separation on a cyanopropyl-packed column with an acetonitrile:methanol:aqueous monopotassium phosphate mobile phase pumped at a flow rate of 2.0 mL/min. Analytes are detected by UV absorbance at 215 nm. These conditions yield highly symmetrical and well-resolved peaks in less than 5 min after the injection of a mixture. In the experiment, students are given amitriptyline hydrochloride-perphenazine tablets without the manufacturer's labeled composition claim and a stock solution mixture with known concentrations of amitriptyline hydrochloride and perphenazine. They prepare four standards and a pharmaceutical sample of unknown concentration, assay each solution in quadruplicate, and plot average peak areas of the concentrations of the known solutions in the construction of a standard curve. From the mathematical relationships that result, the average masses of amitriptyline hydrochloride and perphenazine in the prescription tablet are determined. Finally, the standard deviations of the mean masses are calculated. The entire laboratory procedure and statistical data analysis can be completed in a single 3-hour period.

  15. 40 CFR Appendix B to Subpart Nnn... - Free Formaldehyde Analysis of Insulation Resins by Hydroxylamine Hydrochloride

    Code of Federal Regulations, 2012 CFR

    2012-07-01

    ... 40 Protection of Environment 12 2012-07-01 2011-07-01 true Free Formaldehyde Analysis of Insulation Resins by Hydroxylamine Hydrochloride B Appendix B to Subpart NNN of Part 63 Protection of Environment ENVIRONMENTAL PROTECTION AGENCY (CONTINUED) AIR PROGRAMS (CONTINUED) NATIONAL EMISSION STANDARDS FOR HAZARDOUS AIR POLLUTANTS FOR...

  16. 40 CFR 721.5775 - Phenol, 5-amino-2,4-dicholoro-, hydrochloride.

    Code of Federal Regulations, 2010 CFR

    2010-07-01

    ... 40 Protection of Environment 30 2010-07-01 2010-07-01 false Phenol, 5-amino-2,4-dicholoro... Specific Chemical Substances § 721.5775 Phenol, 5-amino-2,4-dicholoro-, hydrochloride. (a) Chemical substance and significant new uses subject to reporting. (1) The chemical substance identified as phenol,...

  17. Enhancing the Effectiveness of Relaxation--Thermal Biofeedback Training with Propranolol Hydrochloride.

    ERIC Educational Resources Information Center

    Holroyd, Kenneth A.; And Others

    1995-01-01

    Evaluated the ability of propranolol hydrochloride to enhance results achieved with relaxation-biofeedback training. Results suggest that concomitant propranolol therapy (CPT) significantly enhanced the effectiveness of relaxation-biofeedback training. CPT also yielded larger reductions in analgesic use and greater improvements in quality-of-life…

  18. 21 CFR 520.2345h - Tetracycline hydrochloride, sodium novobiocin, and prednisolone tablets.

    Code of Federal Regulations, 2010 CFR

    2010-04-01

    ... 21 Food and Drugs 6 2010-04-01 2010-04-01 false Tetracycline hydrochloride, sodium novobiocin, and prednisolone tablets. 520.2345h Section 520.2345h Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL DRUGS, FEEDS, AND RELATED PRODUCTS ORAL DOSAGE FORM NEW ANIMAL DRUGS § 520.2345h...

  19. 21 CFR 520.2345g - Tetracycline hydrochloride and sodium novobiocin tablets.

    Code of Federal Regulations, 2010 CFR

    2010-04-01

    ... 21 Food and Drugs 6 2010-04-01 2010-04-01 false Tetracycline hydrochloride and sodium novobiocin tablets. 520.2345g Section 520.2345g Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL DRUGS, FEEDS, AND RELATED PRODUCTS ORAL DOSAGE FORM NEW ANIMAL DRUGS § 520.2345g Tetracycline...

  20. 75 FR 14444 - Determination That DIDREX (Benzphetamine Hydrochloride) Tablets, 25 Milligrams, Were Not...

    Federal Register 2010, 2011, 2012, 2013, 2014

    2010-03-25

    ...The Food and Drug Administration (FDA) has determined that DIDREX (benzphetamine hydrochloride (HCl)) Tablets, 25 milligrams (mg), were not withdrawn from sale for reasons of safety or effectiveness. This determination will allow FDA to approve abbreviated new drug applications (ANDAs) for benzphetamine HCl 25 mg tablets, if all other legal and regulatory requirements are...

  1. 40 CFR 721.5775 - Phenol, 5-amino-2,4-dicholoro-, hydrochloride.

    Code of Federal Regulations, 2011 CFR

    2011-07-01

    ... 40 Protection of Environment 31 2011-07-01 2011-07-01 false Phenol, 5-amino-2,4-dicholoro... Specific Chemical Substances § 721.5775 Phenol, 5-amino-2,4-dicholoro-, hydrochloride. (a) Chemical substance and significant new uses subject to reporting. (1) The chemical substance identified as phenol,...

  2. HEALTH AND ENVIRONMENTAL EFFECTS PROFILE FOR 2,4-DIMETHYLANILINE AND 2,4-DIMETHYLANILINE HYDROCHLORIDE

    EPA Science Inventory

    The Health and Environmental Effects Profile for 2-4-Dimethylaniline and 2,4-Dimethylaniline Hydrochloride was prepared to support listings of hazardous constituents of a wide range of waste streams under Section 3001 of the Resource Conservation and Recovery Act (RCRA) and to pr...

  3. The effects of zilpaterol hydrochloride and shade on blood metabolites of finishing beef steers

    Technology Transfer Automated Retrieval System (TEKTRAN)

    The effects of feeding zilpaterol hydrochloride (ZH) and shade were evaluated on blood metabolites and lung score in finishing beef steers. Cattle were fed 0 or 8.33 mg/kg ZH for 21 d with a 3- or 4-d withdrawal before harvest and were housed in open or shaded pens. Blood samples and lung scores w...

  4. 21 CFR 524.1662b - Oxytetracycline hydrochloride, polymyxin B sulfate ophthalmic ointment.

    Code of Federal Regulations, 2012 CFR

    2012-04-01

    ... 21 Food and Drugs 6 2012-04-01 2012-04-01 false Oxytetracycline hydrochloride, polymyxin B sulfate ophthalmic ointment. 524.1662b Section 524.1662b Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL DRUGS, FEEDS, AND RELATED PRODUCTS OPHTHALMIC AND TOPICAL DOSAGE FORM NEW ANIMAL DRUGS...

  5. 77 FR 7583 - Determination That WILPO (phentermine hydrochloride) Tablets, 8 Milligrams, Was Not Withdrawn...

    Federal Register 2010, 2011, 2012, 2013, 2014

    2012-02-13

    ... amendments include what is now section 505(j)(7) of the Federal Food, Drug, and Cosmetic Act (21 U.S.C. 355(j... suspends approval of the drug's NDA or ANDA for reasons of safety or effectiveness or if FDA determines... HUMAN SERVICES Food and Drug Administration Determination That WILPO (phentermine hydrochloride)...

  6. A Parent Guide To Understanding the Effects of Ritalin (Methylphenidate Hydrochloride).

    ERIC Educational Resources Information Center

    Villegas, Orlando; And Others

    This guide provides information to help parents decide whether their child with attention deficit hyperactivity disorder (ADHD) should take methylphenidate hydrochloride (Ritalin). Information is provided in a question-and-answer format on various concerns, including: the meaning of ADHD, whether Ritalin is overprescribed, when this medication is…

  7. Effects of zilpaterol hydrochloride on blood gas, electrolyte balance, and pH in feedlot cattle

    Technology Transfer Automated Retrieval System (TEKTRAN)

    The objective of this study was to examine the effects of zilpaterol hydrochloride (ZH) on blood gas, electrolyte balance and pH in feedlot cattle. Black-hided steers and heifers (n=96) were sourced from a commercial feedlot and transported to the Texas Tech University Beef Center in New Deal, TX. C...

  8. Evaluation of objective and subjective mobility variables in feedlot cattle supplemented with zilpaterol hydrochloride

    Technology Transfer Automated Retrieval System (TEKTRAN)

    The objective of this study was to examine the effects of zilpaterol hydrochloride (ZH) on mobility in feedlot cattle. Black-hided steers and heifers (n=96) were sourced from a commercial feedlot and transported to the Texas Tech University Beef Center in New Deal, TX. Cattle were weighed and scan...

  9. Improved compressibility, flowability, dissolution and bioavailability of pioglitazone hydrochloride by emulsion solvent diffusion with additives.

    PubMed

    Patil, S V; Pawar, A P; Sahoo, S K

    2012-03-01

    Spherical agglomerates of pioglitazone hydrochloride were prepared by the emulsion solvent diffusion method with additives (polyethylene glycol 6000, polyvinyl pyrrolidone, beta cyclodextrin, eudragit RS100, low acyl gellan gum and xanthan gum) using methanol, chloroform and water as a good solvent, bridging liquid and poor solvent respectively. Prepared agglomerates were evaluated for compressibility, solubility, dissolution rate and bioavailability, and characterized by SEM, XRPD, DSC and FTIR spectroscopy. Particle size, flowability, compactibility, packability, solubility, dissolution rate and bioavailability of plain agglomerates and agglomerates with additives (except with polyvinyl pyrrolidone) were advantageously improved compared with raw crystalline pioglitazone hydrochloride. These improved properties for direct compression were due to their large-spherical shape and enhanced fragmentation during compaction, together with increased tensile strength and reduced elastic recovery of the compacts. XRPD and DSC studies indicated polymorphic transition of pioglitazone hydrochloride from form II to I during recrystallization but this was not associated with any chemical transition, as indicated by FTIR spectra, well supported by stability studies. Thus spherical crystallization by the emulsion solvent diffusion method with selected additives is a satisfactory method for direct tableting of pioglitazone hydrochloride giving improved bioavailability. PMID:22530302

  10. 21 CFR 524.1484f - Neomycin sulfate, prednisolone acetate, tetracaine hydrochloride eardrops.

    Code of Federal Regulations, 2011 CFR

    2011-04-01

    ... 21 Food and Drugs 6 2011-04-01 2011-04-01 false Neomycin sulfate, prednisolone acetate, tetracaine hydrochloride eardrops. 524.1484f Section 524.1484f Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF...-susceptible organisms and/or allergy. In otitis externa, 2 to 6 drops may be placed in the external ear...

  11. 21 CFR 524.1484f - Neomycin sulfate, prednisolone acetate, tetracaine hydrochloride eardrops.

    Code of Federal Regulations, 2013 CFR

    2013-04-01

    ... 21 Food and Drugs 6 2013-04-01 2013-04-01 false Neomycin sulfate, prednisolone acetate, tetracaine hydrochloride eardrops. 524.1484f Section 524.1484f Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF...-susceptible organisms and/or allergy. In otitis externa, 2 to 6 drops may be placed in the external ear...

  12. 21 CFR 524.1484c - Neomycin sulfate, isoflupredone acetate, tetracaine hydrochloride ointment.

    Code of Federal Regulations, 2010 CFR

    2010-04-01

    ... 21 Food and Drugs 6 2010-04-01 2010-04-01 false Neomycin sulfate, isoflupredone acetate, tetracaine hydrochloride ointment. 524.1484c Section 524.1484c Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL DRUGS, FEEDS, AND RELATED PRODUCTS OPHTHALMIC AND TOPICAL DOSAGE FORM NEW ANIMAL DRUGS §...

  13. 21 CFR 524.1484f - Neomycin sulfate, prednisolone acetate, tetracaine hydrochloride eardrops.

    Code of Federal Regulations, 2012 CFR

    2012-04-01

    ... 21 Food and Drugs 6 2012-04-01 2012-04-01 false Neomycin sulfate, prednisolone acetate, tetracaine hydrochloride eardrops. 524.1484f Section 524.1484f Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF...-susceptible organisms and/or allergy. In otitis externa, 2 to 6 drops may be placed in the external ear...

  14. 21 CFR 524.1484c - Neomycin sulfate, isoflupredone acetate, tetracaine hydrochloride ointment.

    Code of Federal Regulations, 2013 CFR

    2013-04-01

    ... 21 Food and Drugs 6 2013-04-01 2013-04-01 false Neomycin sulfate, isoflupredone acetate, tetracaine hydrochloride ointment. 524.1484c Section 524.1484c Food and Drugs FOOD AND DRUG ADMINISTRATION... observe animals being treated for evidence of hypersensitivity or allergy to the drug. If such signs...

  15. 21 CFR 524.1484c - Neomycin sulfate, isoflupredone acetate, tetracaine hydrochloride ointment.

    Code of Federal Regulations, 2011 CFR

    2011-04-01

    ... 21 Food and Drugs 6 2011-04-01 2011-04-01 false Neomycin sulfate, isoflupredone acetate, tetracaine hydrochloride ointment. 524.1484c Section 524.1484c Food and Drugs FOOD AND DRUG ADMINISTRATION... observe animals being treated for evidence of hypersensitivity or allergy to the drug. If such signs...

  16. 21 CFR 524.1484c - Neomycin sulfate, isoflupredone acetate, tetracaine hydrochloride ointment.

    Code of Federal Regulations, 2012 CFR

    2012-04-01

    ... 21 Food and Drugs 6 2012-04-01 2012-04-01 false Neomycin sulfate, isoflupredone acetate, tetracaine hydrochloride ointment. 524.1484c Section 524.1484c Food and Drugs FOOD AND DRUG ADMINISTRATION... observe animals being treated for evidence of hypersensitivity or allergy to the drug. If such signs...

  17. 21 CFR 524.1484f - Neomycin sulfate, prednisolone acetate, tetracaine hydrochloride eardrops.

    Code of Federal Regulations, 2010 CFR

    2010-04-01

    ... 21 Food and Drugs 6 2010-04-01 2010-04-01 false Neomycin sulfate, prednisolone acetate, tetracaine hydrochloride eardrops. 524.1484f Section 524.1484f Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL DRUGS, FEEDS, AND RELATED PRODUCTS OPHTHALMIC AND TOPICAL DOSAGE FORM NEW ANIMAL DRUGS...

  18. 76 FR 20685 - Determination That NOVANTRONE (Mitoxantrone Hydrochloride) Injection, Equivalent to 25 Milligrams...

    Federal Register 2010, 2011, 2012, 2013, 2014

    2011-04-13

    ...) Injection, Equivalent to 25 Milligrams Base/12.5 Milliliter and Equivalent to 30 Milligrams Base/15... NOVANTRONE (mitoxantrone hydrochloride) Injection, equivalent to (EQ) 25 milligrams (mg) base/12.5 milliliters (mL) and EQ 30 mg base/15 mL, was not withdrawn from sale for reasons of safety or...

  19. Fate and transport of the ß-adrenergic agonist ractopamine hydrochloride in soil-water systems

    Technology Transfer Automated Retrieval System (TEKTRAN)

    The feed additive ractopamine hydrochloride was fortified at four concentrations into batch vials containing soils that differed in both biological activity and organic matter (OM). Sampling of the liquid layer for 14 d demonstrated that ractopamine rapidly dissipated from the liquid layer. Less t...

  20. 77 FR 53892 - Determination That ALOXI (Palonosetron Hydrochloride) Capsules, 0.5 Milligram (Base), Were Not...

    Federal Register 2010, 2011, 2012, 2013, 2014

    2012-09-04

    ...The Food and Drug Administration (FDA) has determined that ALOXI (palonosetron hydrochloride (HCl)) Capsules, 0.5 milligram (mg) (base), were not withdrawn from sale for reasons of safety or effectiveness. This determination will allow FDA to approve abbreviated new drug applications (ANDAs) for palonosetron HCl capsules, 0.5 mg (base), if all other legal and regulatory requirements are...

  1. 40 CFR 721.5775 - Phenol, 5-amino-2,4-dicholoro-, hydrochloride.

    Code of Federal Regulations, 2013 CFR

    2013-07-01

    ... 40 Protection of Environment 32 2013-07-01 2013-07-01 false Phenol, 5-amino-2,4-dicholoro... Specific Chemical Substances § 721.5775 Phenol, 5-amino-2,4-dicholoro-, hydrochloride. (a) Chemical substance and significant new uses subject to reporting. (1) The chemical substance identified as phenol,...

  2. 40 CFR 721.5775 - Phenol, 5-amino-2,4-dicholoro-, hydrochloride.

    Code of Federal Regulations, 2014 CFR

    2014-07-01

    ... 40 Protection of Environment 31 2014-07-01 2014-07-01 false Phenol, 5-amino-2,4-dicholoro... Specific Chemical Substances § 721.5775 Phenol, 5-amino-2,4-dicholoro-, hydrochloride. (a) Chemical substance and significant new uses subject to reporting. (1) The chemical substance identified as phenol,...

  3. 40 CFR 721.5775 - Phenol, 5-amino-2,4-dicholoro-, hydrochloride.

    Code of Federal Regulations, 2012 CFR

    2012-07-01

    ... 40 Protection of Environment 32 2012-07-01 2012-07-01 false Phenol, 5-amino-2,4-dicholoro... Specific Chemical Substances § 721.5775 Phenol, 5-amino-2,4-dicholoro-, hydrochloride. (a) Chemical substance and significant new uses subject to reporting. (1) The chemical substance identified as phenol,...

  4. Simultaneous HPLC Determination of Butenafine Hydrochloride and Betamethasone in a Cream Formulation

    PubMed Central

    Ankam, R.; Mukkanti, K.; Durgaprasad, S.; Khan, M.

    2009-01-01

    A fast, specific, accurate and precise reverse phase high performance liquid chromatographic method was developed for the simultaneous determination of butenafine hydrochloride and betamethasone in cream formulation. The determination was carried out on licrocart licrosphere RP-select B (250×4.6 mm, 5 μ) column in isocratic mode, the mobile phase consisting of 50 mM ammonium acetate buffer and acetonitrile in the ratio of 60:40, adjusted to pH 4.5 ± 0.1 with glacial acetic acid. The flow rate was 2.0 ml/min and eluent was monitored at 254 nm. The retention times of butenafine hydrochloride and betamethasone were 4.70 min and 7.76 min, respectively, and the resolution factor was greater than 4.0. Linearity of butenafine hydrochloride and betamethasone were in the range of 100-300 μg/ml and 5-15 μg/ml, respectively. The proposed method is also found to be precise and robust for the simultaneous determination of butenafine hydrochloride and betamethasone in cream formulation. PMID:20502575

  5. Simultaneous HPLC determination of butenafine hydrochloride and betamethasone in a cream formulation.

    PubMed

    Ankam, R; Mukkanti, K; Durgaprasad, S; Khan, M

    2009-09-01

    A fast, specific, accurate and precise reverse phase high performance liquid chromatographic method was developed for the simultaneous determination of butenafine hydrochloride and betamethasone in cream formulation. The determination was carried out on licrocart licrosphere RP-select B (250x4.6 mm, 5 mu) column in isocratic mode, the mobile phase consisting of 50 mM ammonium acetate buffer and acetonitrile in the ratio of 60:40, adjusted to pH 4.5 +/- 0.1 with glacial acetic acid. The flow rate was 2.0 ml/min and eluent was monitored at 254 nm. The retention times of butenafine hydrochloride and betamethasone were 4.70 min and 7.76 min, respectively, and the resolution factor was greater than 4.0. Linearity of butenafine hydrochloride and betamethasone were in the range of 100-300 mug/ml and 5-15 mug/ml, respectively. The proposed method is also found to be precise and robust for the simultaneous determination of butenafine hydrochloride and betamethasone in cream formulation. PMID:20502575

  6. EPR study of free-radical structure and conformation in pyridoxine hydrochloride single crystal

    NASA Astrophysics Data System (ADS)

    Masiakowski, Jerzy T.; Krzyminiewski, Ryszard; Pietrzak, Jerzy

    1985-05-01

    Numerical analysis of experimental EPR spectra of γ-irradiated single crystals of pyridoxine hydrochloride (vitamin B 6) allowed determination of the structure of the radical formed. Six hyperfine couplings were distinguished. The geometrical model of the radical was found to be in good agreement with the geometry expected from the crystal structure. Semi-empirical INDO and CNDO calculations were performed.

  7. 21 CFR 520.1242c - Levamisole hydrochloride and piperazine dihydrochloride.

    Code of Federal Regulations, 2012 CFR

    2012-04-01

    ... an aqueous solution which contains in each fluid ounce 0.36 gram of levamisole hydrochloride and piperazine dihydrochloride equivalent to 3.98 grams of piperazine base. (2) The drug is a soluble powder which when reconstituted with water contains in each fluid ounce 0.45 gram of levamisole...

  8. 21 CFR 520.1242c - Levamisole hydrochloride and piperazine dihydrochloride.

    Code of Federal Regulations, 2014 CFR

    2014-04-01

    ... an aqueous solution which contains in each fluid ounce 0.36 gram of levamisole hydrochloride and piperazine dihydrochloride equivalent to 3.98 grams of piperazine base. (2) The drug is a soluble powder which when reconstituted with water contains in each fluid ounce 0.45 gram of levamisole...

  9. Kinetic spectrophotometric methods for the determination of dothiepin hydrochloride in bulk and in drug formulation.

    PubMed

    Taha, Elham A

    2003-08-01

    Two simple and sensitive kinetic methods for the determination of dothiepin hydrochloride are described. The first method is based on kinetic investigation of the oxidation reaction of the drug with alkaline potassium permanganate at room temperature for a fixed time of 25 min. The absorbance of the colored manganate ions is measured at 610 nm. The second method is based on the reaction of dothiepin hydrochloride with 4-chloro-7-nitrobenzofurazan (NBD-Cl) in the presence of 0.1 mol L(-1) sodium bicarbonate. Spectrophotometric measurement was achieved by recording the absorbance at 470 nm for a fixed time of 60 min. All variables affecting the development of the color were investigated and the conditions were optimized. Plots of absorbance against concentration in both procedures were rectilinear over the ranges 4-24 and 50-250 microg mL(-1), with mean recoveries 99.33+/-0.42 and 99.88+/-0.53, respectively. The proposed methods were successfully applied for the determination of dothiepin hydrochloride in bulk powder and in capsule dosage form. The results obtained were found to agree statistically with those given by the non-aqueous B.P. method. Furthermore the methods were validated according to USP guidelines and also assessed by applying the standard addition technique. The determination of dothiepin hydrochloride by the fixed concentration method is feasible with the calibration equations obtained, but the fixed time method proves to be more applicable. PMID:12856096

  10. 21 CFR 520.2345h - Tetracycline hydrochloride, sodium novobiocin, and prednisolone tablets.

    Code of Federal Regulations, 2012 CFR

    2012-04-01

    ... 21 Food and Drugs 6 2012-04-01 2012-04-01 false Tetracycline hydrochloride, sodium novobiocin, and prednisolone tablets. 520.2345h Section 520.2345h Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL DRUGS, FEEDS, AND RELATED PRODUCTS ORAL DOSAGE FORM NEW ANIMAL DRUGS § 520.2345h...

  11. 21 CFR 520.2345g - Tetracycline hydrochloride and sodium novobiocin tablets.

    Code of Federal Regulations, 2012 CFR

    2012-04-01

    ... 21 Food and Drugs 6 2012-04-01 2012-04-01 false Tetracycline hydrochloride and sodium novobiocin tablets. 520.2345g Section 520.2345g Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL DRUGS, FEEDS, AND RELATED PRODUCTS ORAL DOSAGE FORM NEW ANIMAL DRUGS § 520.2345g Tetracycline...

  12. A randomized, crossover design study of sevelamer carbonate powder and sevelamer hydrochloride tablets in chronic kidney disease patients on haemodialysis

    PubMed Central

    Fan, Stanley; Ross, Calum; Mitra, Sandip; Kalra, Philip; Heaton, Jeremy; Hunter, John; Plone, Melissa; Pritchard, Nick

    2009-01-01

    Background. Sevelamer carbonate is an improved, buffered form of sevelamer hydrochloride developed for the treatment of hyperphosphataemia in CKD patients. Sevelamer carbonate formulated as a powder for oral suspension presents a novel, patient-friendly alternative to tablet phosphate binders. This study compared the safety and efficacy of sevelamer carbonate powder with sevelamer hydrochloride tablets in CKD patients on haemodialysis. Methods. This was a multi-centre, open-label, randomized, crossover design study. Thirty-one haemodialysis patients were randomly assigned to either sevelamer carbonate powder or sevelamer hydrochloride tablets for 4 weeks followed by a crossover to the other regimen for an additional 4 weeks. Results. The mean serum phosphorus was 1.6 ± 0.5 mmol/L (5.0 ± 1.5 mg/dL) during sevelamer carbonate powder treatment and 1.7 ± 0.4 mmol/L (5.2 ± 1.1 mg/dL) during sevelamer hydrochloride tablet treatment. Sevelamer carbonate powder and sevelamer hydrochloride tablets are equivalent in controlling serum phosphorus; the geometric least square mean ratio was 0.95 (90% CI 0.87–1.03). No statistically significant or clinically meaningful differences were observed in calcium × phosphorus product and lipid levels between sevelamer carbonate powder and sevelamer hydrochloride tablets. Serum bicarbonate levels increased 2.7 ± 3.7 mmol/L (2.7 ± 3.7 mEq/L) during sevelamer carbonate treatment. No statistically significant change in bicarbonate was observed during sevelamer hydrochloride treatment. Sevelamer carbonate powder and sevelamer hydrochloride were well tolerated during this study. Conclusions. Sevelamer carbonate powder and sevelamer hydrochloride tablets are equivalent in controlling serum phosphorus and well tolerated in CKD patients on haemodialysis. Bicarbonate levels improved only during sevelamer carbonate treatment. Sevelamer carbonate powder should provide a welcomed new option for the treatment of hyperphosphataemia for CKD

  13. Bivalent transition metal complexes of o-hydroxyacetophenone [N-(3-hydroxy-2-naphthoyl)] hydrazone: Spectroscopic, antibacterial, antifungal activity and thermogravimetric studies

    NASA Astrophysics Data System (ADS)

    Zaky, R. R.; Ibrahim, K. M.; Gabr, I. M.

    2011-10-01

    Schiff base complexes of Cu(II), Ni(II) and Zn(II) with the o-hydroxyacetophenone [N-(3-hydroxy-2-naphthoyl)] hydrazone (H 2o-HAHNH) containing N and O donor sites have been synthesized. Both ligand and its metal complexes were characterized by different physicochemical methods, elemental analysis, molar conductivity ( 1H NMR, 13C NMR, IR, UV-visible, ESR, MS spectra) and also thermal analysis (TG and DTG) techniques. The discussion of the outcome data of the prepared complexes indicates that the ligand behave as a bidentate and/or tridentate ligand. The electronic spectra of the complexes as well as their magnetic moments suggest octahedral geometries for all isolated complexes. The room temperature solid state ESR spectrum of the Cu(II) complex shows d x2- y2 as a ground state, suggesting tetragonally distorted octahedral geometry around Cu(II) centre. The molar conductance measurements proved that the complexes are non-electrolytes. The kinetic thermodynamic parameters such as: E#, Δ H#, Δ G#, Δ S# are calculated from the DTG curves, for the [Ni(H O-HAHNH) 2] and [Zn(H 2 O-HAHNH)(OAc) 2]·H 2O complexes using the Coats-Redfern equation. Also, the antimicrobial properties of all compounds were studied using a wide spectrum of bacterial and fungal strains. The [Cu(H o-HAHNH)(OAc)(H 2O) 2] complex was the most active against all strains, including Aspergillus sp., Stemphylium sp. and Trichoderma sp. Fungi; E. coli and Clostridium sp. Bacteria.

  14. Design, Synthesis, and Evaluation of 2-Amino-6-nitrobenzothiazole-Derived Hydrazones as MAO Inhibitors: Role of the Methylene Spacer Group.

    PubMed

    Tripathi, Rati K P; Ayyannan, Senthil R

    2016-07-19

    A series of 2-amino-6-nitrobenzothiazole-derived extended hydrazones were designed, synthesized, and investigated for their ability to inhibit monoamine oxidase A and B (MAO-A/MAO-B). The compounds were found to exhibit inhibitory activities in the nanomolar to micromolar range. Some of the compounds showed excellent potency and selectivity against the MAO-B isoform. N'-(5-Chloro-2-oxoindolin-3-ylidene)-2-(6-nitrobenzothiazol-2-ylamino)acetohydrazide (compound 31) showed the highest MAO-B inhibitory activity (IC50 =1.8±0.3 nm, selectivity index [SI]=766.67), whereas compound 6 [N'-(1-(4-bromophenyl)ethylidene)-2-(6-nitrobenzothiazol-2-ylamino)acetohydrazide] was found to be the most active MAO-A inhibitor (IC50 =0.42±0.003 μm). Kinetic studies revealed that compounds 6 and 31 exhibit competitive-type reversible inhibition against both MAO-A and MAO-B, respectively. Structure-activity relationship (SAR) studies disclosed several structural aspects significant for potency and the contribution of the methylene spacer toward MAO-B inhibitory potency, with minimal or no neurotoxicity. Molecular modeling studies yielded a good correlation between experimental and theoretical inhibitory data. Binding pose analysis revealed the significance of cumulative effects of π-π stacking and hydrogen bond interactions for effective stabilization of virtual ligand-protein complexes. Further optimization studies of compound 31, including co-crystallization of inhibitor-MAO-B complexes, are essential to develop these compounds as potential therapeutic agents for MAO-B-associated neurodegenerative diseases. PMID:27332045

  15. Synthesis and quantitative structure-activity relationship (QSAR) study of novel N-arylsulfonyl-3-acylindole arylcarbonyl hydrazone derivatives as nematicidal agents.

    PubMed

    Che, Zhiping; Zhang, Shaoyong; Shao, Yonghua; Fan, Lingling; Xu, Hui; Yu, Xiang; Zhi, Xiaoyan; Yao, Xiaojun; Zhang, Rui

    2013-06-19

    In continuation of our program aimed at the discovery and development of natural-product-based pesticidal agents, 54 novel N-arylsulfonyl-3-acylindole arylcarbonyl hydrazone derivatives were prepared, and their structures were well characterized by ¹H NMR, ¹³C NMR, HRMS, ESI-MS, and mp. Their nematicidal activity was evaluated against that of the pine wood nematode, Bursaphelenchus xylophilus in vivo. Among all of the derivatives, especially V-12 and V-39 displayed the best promising nematicidal activity with LC₅₀ values of 1.0969 and 1.2632 mg/L, respectively. This suggested that introduction of R¹ and R² together as the electron-withdrawing substituents, R³ as the methyl group, and R⁴ as the phenyl with the electron-donating substituents could be taken into account for further preparation of these kinds of compounds as nematicidal agents. Six selected descriptors are a WHIM descriptor (E1m), two GETAWAY descriptors (R1m+ and R3m+), a Burden eigenvalues descriptor (BEHm8), and two edge-adjacency index descriptors (EEig05x and EEig13d). Quantitative structure-activity relationship (QSAR) studies demonstrated that the structural factors, such as molecular mass (a negative correlation with the bioactivity) and molecular polarity (a positive correlation with bioactivity), are likely to govern the nematicidal activities of these compounds. For this model, the correlation coefficient (R²(training set)), the leave-one-out cross-validation correlation coefficient (Q²(LOO)), and the 7-fold cross-validation correlation coefficient (Q²(7-fold)) were 0.791, 0.701, and 0.715, respectively. The external cross-validation correlation coefficient (Q²ext) and the root-mean-square error for the test set (RMSE(test set)) were 0.774 and 3.412, respectively. This study will pave the way for future design, structural modification, and development of indole derivatives as nematicidal agents. PMID:23738496

  16. Application of 3-methylbenzothiazolin-2-one hydrazone for the quantitative spectrophotometric determination of oxcarbazepine in pharmaceuticals with cerium(IV) and periodate

    NASA Astrophysics Data System (ADS)

    Rajendraprasad, N.; Basavaiah, K.; Vinay, K. B.

    2012-09-01

    Two simple, sensitive, selective, accurate, and cost-effective spectrophotometric methods are described for the assay of oxcarbazepine (OXC) in bulk drug and in tablets. The methods are based on an oxidative coupling reaction involving OXC, 3-methylbenzothiazolin-2-one hydrazone (MBTH), and cerium(IV) sulfate at pH 4.28 ± 0.07 (method A) or sodium periodate at pH > 4.0 (method B) to form an orange colored product with an absorption maximum at 450 nm. Under optimized experimental conditions, the calibration graphs are linear over the ranges of 4-80 and 2-32 μg/ml for methods A and B, respectively, with correlation coefficient (r) values of 0.9984 and 0.9976. The apparent molar absorptivity values are 3.13ṡ103 and 9.13ṡ103 l/molṡcm for methods A and B, respectively. The other optical characteristics such as Sandell's sensitivity, limits of detection (LOD) and quantification (LOQ) values are also reported. The accuracy and precision of the methods were evaluated based on intra-day and inter-day variations. The proposed methods were successfully applied to the determination of OXC in tablets: the results were comparable with the published data obtained using the reference method. The reaction stoichiometry of OXC with MBTH (1:1 in method A and 1:2 in method B) was also evaluated using the limiting logarithmic method, and a possible reaction pathway is presented for the both methods.

  17. In vitro and in vivo genotoxicity assessment of the dopamine receptor antagonist molindone hydrochloride.

    PubMed

    Krishna, Gopala; Gopalakrishnan, Gopa; Goel, Saryu

    2016-05-01

    Molindone hydrochloride is a dihydroindolone neuroleptic with dopamine D2 and D5 receptor antagonist activity. As an integral component of its preclinical safety evaluation, molindone hydrochloride was evaluated in a series of in vitro and in vivo genetic toxicology assays. In the bacterial reverse gene mutation assays employing four Salmonella tester strains (TA98, TA100, TA1535, and TA1537) and the E. coli tester strain WP2uvrA, molindone hydrochloride was negative in all strains, except TA100, in which it induced a positive response (up to 3-fold) in the presence of rat liver S9. With human S9, a small (2-fold), but nonreproducible, increase in revertants was observed in TA100 at the highest concentration of molindone tested (5,000 µg/plate). The mutagenicity was completely abrogated by the addition of glutathione and UDP-glucuronic acid to rat liver S9, suggesting detoxification of the mutagenic metabolite(s) by Phase II conjugation reactions, pathways commonly operational in humans. Molindone hydrochloride did not induce chromosomal aberrations in human lymphocyte cultures, did not elicit a positive response in a rat bone marrow micronucleus test for clastogencity/aneugenicity, and did not give a positive response in the rat liver comet assay for DNA damage. Collectively, the weight of evidence from these studies, combined with a large margin of safety and efficient detoxification through Phase II conjugation supports the interpretation that molindone hydrochloride does not pose a genotoxic risk to humans at the anticipated clinical dose levels. Environ. Mol. Mutagen. 57:288-298, 2016. © 2016 Wiley Periodicals, Inc. PMID:27040600

  18. Optimization of mesoporous carbons for efficient adsorption of berberine hydrochloride from aqueous solutions.

    PubMed

    Li, Yin; Fu, Jie; Deng, Shuguang; Lu, Xiuyang

    2014-06-15

    Sixteen mesoporous carbon adsorbents were synthesized by varying the ratio of soft to hard templates in order to optimize the pore textural properties of these adsorbents. The mesoporous carbon adsorbents have a high BET specific surface area (1590.3-2193.5 m(2)/g), large pore volume (1.72-2.56 cm(3)/g), and uniform pore size distribution with a median pore diameter ranging from 3.51 nm to 4.52 nm. It was observed that pore textural properties of the carbon adsorbents critically depend on the molar ratio of carbon sources to templates, and the hard template plays a more important role than the soft template in manipulating the pore textures. Adsorption isotherms of berberine hydrochloride at 303 K were measured to evaluate the adsorption efficacy of these adsorbents. The adsorption of berberine hydrochloride from aqueous solutions on the sixteen mesoporous carbon adsorbents synthesized in this work is very efficient, and the adsorption equilibrium capacities on all samples are more than double the adsorption capacities of berberine hydrochloride of the benchmark adsorbents (polymer resins and spherical activated carbons) at similar conditions. It was observed from the adsorption experiments that the equilibrium adsorption amounts of berberine hydrochloride are strongly correlated with the BET specific surface area and pore volume of the adsorbents. The adsorbent with the highest BET of 2193.5 m(2)/g displayed the largest adsorption capacity of 574 mg/g at an equilibrium concentration of 0.10mg/mL of berberine hydrochloride in an aqueous solution. PMID:24767505

  19. Stability studies of lincomycin hydrochloride in aqueous solution and intravenous infusion fluids

    PubMed Central

    Czarniak, Petra; Boddy, Michael; Sunderland, Bruce; Hughes, Jeff D

    2016-01-01

    Purpose The purpose of this study was to evaluate the chemical stability of Lincocin® (lincomycin hydrochloride) in commonly used intravenous fluids at room temperature (25°C), at accelerated-degradation temperatures and in selected buffer solutions. Materials and methods The stability of Lincocin® injection (containing lincomycin 600 mg/2 mL as the hydrochloride) stored at 25°C±0.1°C in sodium lactate (Hartmann’s), 0.9% sodium chloride, 5% glucose, and 10% glucose solutions was investigated over 31 days. Forced degradation of Lincocin® in hydrochloric acid, sodium hydroxide, and hydrogen peroxide was performed at 60°C. The effect of pH on the degradation rate of lincomycin hydrochloride stored at 80°C was determined. Results Lincomycin hydrochloride w as found to maintain its shelf life at 25°C in sodium lactate (Hartmann’s) solution, 0.9% sodium chloride solution, 5% glucose solution, and 10% glucose solution, with less than 5% lincomycin degradation occurring in all intravenous solutions over a 31-day period. Lincomycin hydrochloride showed less rapid degradation at 60°C in acid than in basic solution, but degraded rapidly in hydrogen peroxide. At all pH values tested, lincomycin followed first-order kinetics. It had the greatest stability near pH 4 when stored at 80°C (calculated shelf life of 4.59 days), and was least stable at pH 2 (calculated shelf life of 0.38 days). Conclusion Lincocin® injection was chemically found to have a shelf life of at least 31 days at 25°C when added to sodium lactate (Hartmann’s) solution, 0.9% sodium chloride solution, 5% glucose solution, and 10% glucose solution. Solutions prepared at approximately pH 4 are likely to have optimum stability. PMID:27022242

  20. Effect of local application of delmopinol hydrochloride on developing and early established supragingival plaque in humans.

    PubMed

    Klinge, B; Matsson, L; Attström, R; Edwardsson, S; Sjödin, T

    1996-06-01

    The aim of the study was to investigate the effect of delmopinol hydrochloride on the development of dental plaque and on newly established plaque. In addition, the influence of this compound on the composition of the microbiota colonizing the gingival mucous membrane was studied. 14 healthy male volunteers took part. After a 3 week pre-experimental period of intense oral hygiene, the participants refrained from all oral hygiene for 14 days. The buccal surfaces of cuspids and bicuspids on one side of the jaws were treated with a 1% aqueous solution of delmopinol hydrochloride (applied with a paint brush) 2 x a day for 7 days, while the contralateral side received placebo solution. On day 7, the application procedures were changed in that the test compound was applied on the teeth previously treated with placebo and vice versa. Plaque development was assessed clinically and by photo-based planimetric determination. The clinical recordings revealed that 89.3% of the placebo-treated surfaces displayed visible plaque on day 7, compared to 6.0% of the delmopinol hydrochloride treated surfaces. Delmopinol hydrochloride treatment of the previously placebo-treated surfaces resulted in a decrease in the number of surfaces with visible plaque from 89.3% on day 7 to 6% on day 14. These results were confirmed by the planimetric data. No significant change in the composition of the mucosal flora was observed during the experimental period. The present results indicate that delmopinol hydrochloride markedly reduces the formation of dental plaque on a clean tooth surface exposed to conditions which favour bacterial colonization. Furthermore, the substance appears to possess plaque-dissolving properties. PMID:8811473

  1. [Pharmacokinetic interaction of pioglitazone hydrochloride and atorvastatin calcium in Beagle dogs].

    PubMed

    Chen, He-Li; Zhang, Wen-Ping; Yang, Fu-Ying; Wang, Xin-Yu; Yang, Wen-Cheng; Dang, Hong-Wan

    2013-05-01

    The object of this study is to investigate the pharmacokinetic interaction of pioglitazone hydrochloride and atorvastatin calcium in healthy adult Beagle dogs following single and multiple oral dose administration. A randomized, cross-over study was conducted with nine healthy adult Beagle dogs assigned to three groups. Each group was arranged to take atorvastatin calcium (A), pioglitazone hydrochloride (B), atorvastatin calcium and pioglitazone hydrochloride (C) orally in the first period, to take B, C, A in the second period, and to take C, A, B in the third period for 6 days respectively. The blood samples were collected at the first and the sixth day after the administration, plasma drug concentrations were determined by LC-MS/MS, a one-week wash-out period was needed between each period. The pharmacokinetic parameters of drug combination group and the drug alone group were calculated by statistical moment method, calculation of C(max) and AUC(0-t) was done by using 90% confidence interval method of the bioequivalence and bioavailability degree module DAS 3.2.1 software statistics. Compared with the separate administration, the main pharmacokinetic parameters (C(max) and AUC(0-t)) of joint use of pioglitazone hydrochloride and atorvastatin calcium within 90% confidence intervals for bioequivalence statistics were unqualified, the mean t(max) with standard deviation used paired Wilcoxon test resulted P > 0.05. There was no significant difference within t1/2, CL(int), MRT, V/F. Pioglitazone hydrochloride and atorvastatin calcium had pharmacokinetic interaction in healthy adult Beagle dogs. PMID:23888699

  2. 40 CFR Appendix A to Subpart Ddd... - Free Formaldehyde Analysis of Insulation Resins by the Hydroxylamine Hydrochloride Method

    Code of Federal Regulations, 2013 CFR

    2013-07-01

    ... be in the polymeric form. The hydrolysis of these polymers is catalyzed by hydrogen ions. 2.2The... hydroxylamine hydrochloride will produce sufficient hydrogen ions to catalyze the depolymerization of...

  3. 40 CFR Appendix A to Subpart Ddd... - Free Formaldehyde Analysis of Insulation Resins by the Hydroxylamine Hydrochloride Method

    Code of Federal Regulations, 2011 CFR

    2011-07-01

    ... be in the polymeric form. The hydrolysis of these polymers is catalyzed by hydrogen ions. 2.2The... hydroxylamine hydrochloride will produce sufficient hydrogen ions to catalyze the depolymerization of...

  4. 40 CFR Appendix A to Subpart Ddd... - Free Formaldehyde Analysis of Insulation Resins by the Hydroxylamine Hydrochloride Method

    Code of Federal Regulations, 2010 CFR

    2010-07-01

    ... be in the polymeric form. The hydrolysis of these polymers is catalyzed by hydrogen ions. 2.2The... hydroxylamine hydrochloride will produce sufficient hydrogen ions to catalyze the depolymerization of...

  5. Pharmacokinetics of hydromorphone hydrochloride after intravenous and intramuscular administration of a single dose to American kestrels (Falco sparverius)

    USGS Publications Warehouse

    Sanchez-Migallon Guzman, David; KuKanich, Butch; Drazenovich, Tracy L.; Olsen, Glenn H.; Paul-Murphy, Joanne R.

    2014-01-01

    Conclusion and Clinical Relevance—Results indicated hydromorphone hydrochloride had high bioavailability and rapid elimination after IM administration, with a short terminal half-life, rapid plasma clearance, and large volume of distribution in American kestrels. Further studies regarding the effects of other doses, other administration routes, constantrate infusions, and slow release formulations on the pharmacokinetics of hydromorphone hydrochloride and its metabolites in American kestrels may be indicated.

  6. Penetration enhancing effect of menthol on the percutaneous flux of nicardipine hydrochloride through excised rat epidermis from hydroxypropyl cellulose gels.

    PubMed

    Krishnaiah, Y S R; Satyanarayana, V; Karthikeyan, R S

    2002-01-01

    The aim of the present investigation is to study the penetration enhancing effect of menthol on the percutaneous flux of nicardipine hydrochloride through the excised rat epidermis from 2% w/w hydroxypropyl cellulose (HPC) gel system. The HPC gel formulations containing nicardipine hydrochloride and selected concentrations of menthol (0-12% w/w) were prepared, and evaluated for in vitro permeation of the drug through excised rat abdominal epidermis. The percutaneous flux of nicardipine hydrochloride across rat epidermis was enhanced markedly by the addition of menthol to the HPC gels. A maximum flux of nicardipine hydrochloride (227.70 +/- 1.30 micrograms cm-2 hr-1) was observed with an enhancement ratio of 7.12 when menthol was incorporated at a concentration of 8% w/w in a reservoir HPC system. The differential scanning calorimetry and Fourier transform-infrared spectroscopy data indicated that menthol increased the percutaneous flux of nicardipine hydrochloride through the rat skin by partial extraction of lipids in the stratum corneum. The results suggest that menthol may be useful for increasing the skin permeability of nicardipine hydrochloride from transdermal therapeutic system containing HPC gel as a reservoir. PMID:12229262

  7. Synthesis, characterisation, reactivity and in vitro antiamoebic activity of hydrazone based oxovanadium(IV), oxovanadium(V) and mu-bis(oxo)bis{oxovanadium(V)} complexes.

    PubMed

    Maurya, Mannar R; Agarwal, Shalu; Abid, Mohammad; Azam, Amir; Bader, Cerstin; Ebel, Martin; Rehder, Dieter

    2006-02-21

    Binuclear, mu-bis(oxo)bis{oxovanadium(V)} complexes [(VOL)2(mu-O)2](2 and 7)(where HL are the hydrazones Hacpy-nah I or Hacpy-fah II; acpy = 2-acetylpyridine, nah = nicotinic acid hydrazide and fah = 2-furoic acid hydrazide) were prepared by the reaction of [VO(acac)2] and the ligands in methanol followed by aerial oxidation. The paramagnetic intermediate complexes [VO(acac)(acpy-nah)](1) and [VO(acac)(acpy-fah)](6) have also been isolated. Treatment of [VO(acac)(acpy-nah)] and [VO(acac)(acpy-fah)] with aqueous H2O2 yields the oxoperoxovanadium(V) complexes [VO(O2)(acpy-nah)](3) and [VO(O2)(acpy-fah)](8). In the presence of catechol (H2cat) or benzohydroxamic acid (H2bha), 1 and 6 give the mixed chelate complexes [VO(cat)L](HL =I: 4, HL =II: 9) or [VO(bha)L](HL =I: 5, HL =II: 10). Complexes 4, 5, 9 and 10 slowly convert to the corresponding oxo-mu-oxo species 2 and 7 in DMF solution. Ascorbic acid enhances this conversion under aerobic conditions, possibly through reduction of these complexes with concomitant removal of coordinated catecholate or benzohydroxamate. Acidification of 7 with HCl dissolved in methanol afforded a hydroxo(oxo) complex. The crystal and molecular structure of 2.1.5H2O has been determined, and the structure of 7 re-determined, by single crystal X-ray diffraction. Both of these binuclear complexes contain the uncommon asymmetrical {VO(mu-O)}2 diamond core. The in vitro tests of the antiamoebic activity of ligands I and II and their binuclear complexes 2 and 7 against the protozoan parasite Entamoeba histolytica show that the ligands have no amoebicidal activity while their vanadium complexes 2 and 7 display more effective amoebicidal activity than the most commonly used drug metronidazole (IC50 values are 1.68 and 0.45 microM, respectively vs 1.81 microM for metronidazole). Complexes 2 and 7 catalyse the oxidation of styrene and ethyl benzene effectively. Oxidation of styrene, using H2O2 as an oxidant, gives styrene epoxide, 2

  8. A hydrazone covalent organic polymer based micro-solid phase extraction for online analysis of trace Sudan dyes in food samples.

    PubMed

    Zhang, Chengjiang; Li, Gongke; Zhang, Zhuomin

    2015-11-01

    Covalent organic polymers (COPs) connected by covalent bonds are a new class of porous network materials with large surface area and potential superiority in sample pretreatment. In this study, a new hydrazone linked covalent organic polymer (HL-COP) adsorbent was well-designed and synthesized based on a simple Schiff-base reaction. The condensation of 1,4-phthalaldehyde and 1,3,5-benzenetricarbohydrazide as organic building blocks led to the synthesis of HL-COP with uniform particle size and good adsorption performance. This HL-COP adsorbent with high hydrophobic property and rich stacking π electrons contained abundant phenyl rings and imine (CN) groups throughout the entire molecular framework. The adsorption mechanism was explored and discussed based on π-π affinity, hydrophobic effect, hydrogen bonding and electron-donor-acceptor (EDA) interaction, which contributed to its strong recognition affinity to target compounds. Enrichment factors were 305-757 for six Sudan dyes by HL-COP micro-solid phase extraction (μ-SPE), indicating its remarkable preconcentration ability. Furthermore, the adsorption amounts by HL-COP μ-SPE were 1.0-11.0 folds as those by three commonly used commercial adsorbents. Then, HL-COP was applied as adsorbent of online μ-SPE coupled with high performance liquid chromatography (HPLC) for enrichment and analysis of trace Sudan dyes in food samples with detection limit of 0.03-0.15μg/L. The method was successfully applied for online analysis of chilli powder and sausage samples. Sudan II and Sudan III in one positive chilli powder sample were actually found and determined with concentrations of 8.3 and 6.8μg/kg, respectively. The recoveries of chilli powder and sausage samples were in range of 75.8-108.2% and 73.8-112.6% with relative standard deviations of 1.2-8.5% and 1.9-9.4% (n=5), respectively. The proposed method was accurate, reliable and convenient for the online simultaneous analysis of trace Sudan dyes in food samples. PMID

  9. Vanadium complexes having [VO]2+, [VO]3+ and [VO2]+ cores with hydrazones of 2,6-diformyl-4-methylphenol: synthesis, characterization, reactivity, and catalytic potential.

    PubMed

    Maurya, Mannar R; Haldar, Chanchal; Kumar, Amit; Kuznetsov, Maxim L; Avecilla, Fernando; Costa Pessoa, João

    2013-09-01

    The Schiff bases H3dfmp(L)2 obtained by the condensation of 2,6-diformyl-4-methylphenol and hydrazones [L = isonicotinoylhydrazide (inh), nicotinoylhydrazide (nah) and benzoylhydrazide (bhz)] are prepared and characterized. By reaction of [V(IV)O(acac)2] and the H3dfmp(L)2 in methanol the V(IV)O-complexes [V(IV)O{Hdfmp(inh)2}(H2O)] (1), [V(IV)O{Hdfmp(nah)2}(H2O)] (2) and [V(IV)O{Hdfmp(bhz)2}(H2O)] (3) were obtained. Upon their aerial oxidation in methanol [V(V)O(OMe)(MeOH){Hdfmp(inh)2}] (4), [V(V)O(OMe)(MeOH){Hdfmp(nah)2}] (5) and [V(V)O(OMe)(MeOH){Hdfmp(bhz)2}] (6) were isolated. In the presence of KOH, oxidation of 1-3 results in the formation of [V(V)O2{H2dfmp(inh)2}]n·5H2O (7), K[V(V)O2{Hdfmp(nah)2}] (8) and K[V(V)O2{Hdfmp(bhz)2}] (9). All compounds are characterized in the solid state and in solution, namely by spectroscopic techniques (IR, UV-Vis, EPR, (1)H, (13)C and (51)V NMR), and DFT is also used to calculate the V(IV) hyperfine coupling constants of V(IV)-compounds and (51)V NMR chemical shifts of several V(V)-species and assign them to those formed in solution. Single crystal X-ray analysis of [V(V)O(OMe)(MeOH){Hdfmp(bhz)2}] (6) and [V(V)O2{H2dfmp(inh)2}]n·5H2O (7) confirm the coordination of the ligand in the dianionic (ONO(2-)) enolate tautomeric form, one of the hydrazide moieties remaining non-coordinated. In the case of 7 the free N(pyridine) atom of the inh moiety coordinates to the other vanadium center yielding a polynuclear complex in the solid state. It is also demonstrated that the V(V)O2-complexes are catalyst precursors in the oxidative bromination of styrene by H2O2, therefore acting as functional models of vanadium dependent haloperoxidases. Plausible intermediates involved in the catalytic process are established by UV-Vis, (51)V NMR and DFT studies. PMID:23680862

  10. Bismuth(III) complexes with 2-acetylpyridine- and 2-benzoylpyridine-derived hydrazones: Antimicrobial and cytotoxic activities and effects on the clonogenic survival of human solid tumor cells.

    PubMed

    Ferreira, Isabella P; Piló, Elisa D L; Recio-Despaigne, Angel A; Da Silva, Jeferson G; Ramos, Jonas P; Marques, Lucas B; Prazeres, Pedro H D M; Takahashi, Jacqueline A; Souza-Fagundes, Elaine M; Rocha, Willian; Beraldo, Heloisa

    2016-07-01

    Complexes [Bi(2AcPh)Cl2]·0.5H2O (1), [Bi(2AcpClPh)Cl2] (2), [Bi(2AcpNO2Ph)Cl2] (3), [Bi(2AcpOHPh)Cl2]·2H2O (4), [Bi(H2BzPh)Cl3]·2H2O (5), [Bi(H2BzpClPh)Cl3] (6), [Bi(2BzpNO2Ph)Cl2]·2H2O (7) and [Bi(H2BzpOHPh)Cl3]·2H2O (8) were obtained with 2-acetylpyridine phenylhydrazone (H2AcPh), its -para-chloro-phenyl- (H2AcpClPh), -para-nitro-phenyl (H2AcpNO2Ph) and -para-hydroxy-phenyl (H2AcpOHPh) derivatives, as well as with the 2-benzoylpyridine phenylhydrazone analogues (H2BzPh, H2BzpClPh, H2BzpNO2Ph, H2BzpOHPh). Upon coordination to bismuth(III) antibacterial activity against Gram-positive and Gram-negative bacterial strains significantly improved except for complex (4). The cytotoxic effects of the compounds under study were evaluated on HL-60, Jurkat and THP-1 leukemia, and on MCF-7 and HCT-116 solid tumor cells, as well as on non-malignant Vero cells. In general, 2-acetylpyridine-derived hydrazones proved to be more potent and more selective as cytotoxic agents than the corresponding 2-benzoylpyridine-derived counterparts. Exposure of HCT-116 cells to H2AcpClPh, H2AcpNO2Ph and complex (3) led to 99% decrease of the clonogenic survival. The IC50 values of these compounds were three-fold smaller when cells were cultured in soft-agar (3D) than when cells were cultured in monolayer (2D), suggesting that they constitute interesting scaffolds, which should be considered in further studies aiming to develop new drug candidates for the treatment of colon cancer. PMID:27209169

  11. Pharmacokinetics of high-dose oral thiamine hydrochloride in healthy subjects

    PubMed Central

    2012-01-01

    Background High dose oral thiamine may have a role in treating diabetes, heart failure, and hypermetabolic states. The purpose of this study was to determine the pharmacokinetic profile of oral thiamine hydrochloride at 100 mg, 500 mg and 1500 mg doses in healthy subjects. Methods This was a randomized, double-blind, single-dose, 4-way crossover study. Pharmacokinetic measures were calculated. Results The AUC0-10 hr and Cmax values increased nonlinearly between100 mg and 1500 mg. The slope of the AUC0-10 hr vs dose, as well as the Cmax vs dose, plots are steepest at the lowest thiamine doses. Conclusion Our study demonstrates that high blood levels of thiamine can be achieved rapidly with oral thiamine hydrochloride. Thiamine is absorbed by both an active and nonsaturable passive process. Trial Registration ClinicalTrials.gov: NCT00981877 PMID:22305197

  12. Esterification of pseudoephedrine hydrochloride by citric acid in a solid dose pharmaceutical preparation.

    PubMed

    Goel, Alok; Zhao, Zhicheng; Sørensen, Dan; Zhou, Jay; Zhang, Fa

    2016-09-10

    Esterification of pseudoephedrine hydrochloride (PSE) by citric acid was observed in a solid dose pharmaceutical preparation at room temperature and accelerated stability condition (40°C/75% relative humidity). The esterification of PSE with citric acid was confirmed by a solid-state binary reaction in the presence of minor level of water at elevated temperature to generate three isomeric esters. The structures of the pseudoephedrine citric acid esters were elucidated using high-resolution mass spectrometry and nuclear magnetic resonance spectroscopy (NMR). Occurrence of esterification in solid state, instead of amidation which is generally more favorable than esterification, is likely due to remaining HCl salt form of solid pseudoephedrine hydrochloride to protect its amino group from amidation with citric acid. In contrast, the esterification was not observed from solution reaction between PSE and citric acid. PMID:27474946

  13. Simultaneous determination of roxithromycin and ambroxol hydrochloride in a new tablet formulation by liquid chromatography.

    PubMed

    Qi, Meiling; Wang, Peng; Cong, Ruihua; Yang, Jianjun

    2004-09-01

    A rapid and accurate liquid chromatographic method is described for the simultaneous determination of roxithromycin and ambroxol hydrochloride in a new tablet formulation. Chromatographic separation of the two drugs was achieved on a Diamonsil C(18) column (200 mm x 4.6 mm, 5 microm). The mobile phase consisting of a mixture of acetonitrile, methanol and 0.5% ammonium acetate (39:11:50 (v/v), pH 5.5) was delivered at a flow rate of 1.0 ml/min. Detection was performed at 220 nm. Linearity, accuracy and precision were found to be acceptable over the concentration range of 201.2-2012.0 microg/ml for roxithromycin and 42.7-427.0 microg/ml for ambroxol hydrochloride, respectively. Separation was complete in less than 10 min. The proposed method can be used for the quality control of formulation products. PMID:15336374

  14. Evaluation of genotoxic effects of Apitol (cymiazole hydrochloride) in vitro by measurement of sister chromatid exchange.

    PubMed

    Stanimirovic, Zoran; Stevanovic, Jevrosima; Jovanovic, Slobodan; Andjelkovic, Marko

    2005-12-30

    Apitol, with cymiazole hydrochloride as the active ingredient, is used in bee-keeping against the ectoparasitic mite Varroa destructor. The preparation was evaluated for genotoxicity in cultured human peripheral blood lymphocytes. Sister chromatid exchange, the mitotic index and the cell proliferation index were determined for three experimental concentrations of Apitol (0.001, 0.01 and 0.1 mg/ml). All concentrations significantly (p < 0.001) increased the mitotic index (MI = 7.35+/-0.18%, 8.31+/-0.20% and 12.33+/-0.25%, respectively), the proliferative index (PI = 1.83+/-0.01, 1.84+/-0.01 and 1.88+/-0.02, respectively) and the frequency of sister chromatid exchange (SCE = 8.19+/-1.81, 8.78+/-1.80 and 13.46+/-1.88, respectively), suggesting that cymiazole hydrochloride has genotoxic potential. PMID:16309949

  15. Transdermal delivery of betahistine hydrochloride using microemulsions: physical characterization, biophysical assessment, confocal imaging and permeation studies.

    PubMed

    Hathout, Rania M; Nasr, Maha

    2013-10-01

    Transdermal delivery of betahistine hydrochloride encapsulated in various ethyl oleate, Capryol 90(®), Transcutol(®) and water microemulsion formulations was studied. Two different kinds of phase diagrams were constructed for the investigated microemulsion system. Pseudoplastic flow that is preferable for skin delivery was recorded for the investigated microemulsions. A balanced and bicontinuous microemulsion formulation was suggested and showed the highest permeation flux (0.50±0.030mgcm(-2)h(-1)). The effect of the investigated microemulsions on the skin electrical resistance was used to explain the high permeation fluxes obtained. Confocal laser scanning microscopy was used to confirm the permeation enhancement and to reveal the penetration pathways. The results obtained suggest that the proposed microemulsion system highlighted in the current work can serve as a promising alternative delivery means for betahistine hydrochloride. PMID:23732802

  16. [Successful anesthetic management of a patient with giant pheochromocytoma using high-dose landiolol hydrochloride].

    PubMed

    Kitano, Manabu; Komasawa, Nobuyasu; Sawai, Toshiyuki; Minami, Toshiaki

    2014-08-01

    We report successful anesthetic management of a patient with pheochromocytoma using high-dose landiolol hydrochloride. A 55-year-old man was scheduled to undergo resection of giant pheochromocytoma. Epidural anesthesia was not performed due to anticoagulant therapy for lower limb thrombus. Tracheal intubation was performed with the Pentax-AWS Airwayscope. Preoperative screening revealed urine adrenaline 2.567.0 microg x day(-1) urine noradrenaline 1,734.0 microg x day(-1), and a tumor diameter of 96 x 60 mm. Catecholamine surge was controlled with 50 microg x kg(-1) x min(-1) continuous infusion of landiolol hydrochloride and IV bolus phentolamine. On tumor resection, although systemic blood pressure increased to 294 mmHg and was unresponsive to repeated phentolamine administration, the heart rate remained at 70-105 beats x min(-1) and there were no significant ST changes. PMID:25199327

  17. Study on the Interaction of β-Cyclodextrin and Berberine Hydrochloride and Its Analytical Application

    PubMed Central

    Jia, Baoxiu; Li, Yuqin; Wang, Decai; Duan, Rui

    2014-01-01

    The fluorescence enhancement of berberine hydrochloride (BBH) as a result of complex with β-cyclodextrin (β-CD) is investigated. The mechanism of the inclusion was studied and discussed by spectrofluoremetry and infrared spectrograms. The results showed that a 1∶1 (β-CD: BBH) complex was formed with an apparent association constant of 4.23×102 L/mol. Based on the enhancement of the fluorescent intensity of berberine hydrochloride, a new spectrofluorimetric method for the determination of BBH in the presence of β-CD was developed. The linear range was 1.00∼4.00 µg/mL with the detection limit of 5.54 ng/mL. The proposed method was successfully applied to the determination of BBH in tablets. PMID:24810601

  18. Effects of butenafine hydrochloride, a new benzylamine derivative, on experimental dermatophytosis in guinea pigs.

    PubMed Central

    Arika, T; Yokoo, M; Hase, T; Maeda, T; Amemiya, K; Yamaguchi, H

    1990-01-01

    Butenafine hydrochloride, N-4-tert-butylbenzyl-N-methyl-1-naphthalenemethylamine hydrochloride (butenafine), is a novel antifungal agent of the class of benzylamine derivatives. Butenafine was investigated for its activity against guinea pig dermatophytosis caused by Trichophyton mentagrophytes or Microsporum canis in comparison with those of naftifine, tolnaftate, clotrimazole, and bifonazole. Topical butenafine showed excellent efficacy against dermatophytosis when it was applied once daily, and the effect was superior to those of all four reference drugs. When applied once at 24 or 48 h before infection, the drug exhibited excellent prophylactic efficacy against experimental T. mentagrophytes infection. The concentrations of butenafine in animal skin at 24 and 48 h after application of 0.2 ml of a 1% solution were several hundred times higher than those required to kill T. mentagrophytes and M. canis. The good efficacy of butenafine against dermatophytosis may be attributable to its fungicidal activity and long retention in the skin after topical application. PMID:2073116

  19. [Synthesis and antifungal activity of butenafine hydrochloride (KP-363), a new benzylamine antifungal agent].

    PubMed

    Maeda, T; Takase, M; Ishibashi, A; Yamamoto, T; Sasaki, K; Arika, T; Yokoo, M; Amemiya, K

    1991-02-01

    In screening of new antifungal agents, bis(naphthalenemethyl)amines were found to have more potent antifungal activity than clotrimazole. Studies on their structure-activity relationships indicated that benzylamines had potent antifungal activity. Among them, butenafine hydrochloride (N-p-tert-butylbenzyl-N-methyl-1-naphthalenemethylamine hydrochloride, KP-363) has proved to show the strongest activity. It exhibits a wide spectrum activity in vitro against particularly dermatophytes (87 strains; minimal inhibitory concentration (MIC) range, 0.0015 to 0.05 microgram/ml), and also against Aspergillus (15 strains; MIC range, 0.025 to 0.78 microgram/ml), Cryptococcus neoformans (4 strains; MICs 0.78 and 1.56 micrograms/ml) and yeasts of genus Candida (67 strains; MIC range, 3.13 to greater than 100 micrograms/ml). PMID:2056447

  20. Effects of butenafine hydrochloride, a new benzylamine derivative, on experimental dermatophytosis in guinea pigs.

    PubMed

    Arika, T; Yokoo, M; Hase, T; Maeda, T; Amemiya, K; Yamaguchi, H

    1990-11-01

    Butenafine hydrochloride, N-4-tert-butylbenzyl-N-methyl-1-naphthalenemethylamine hydrochloride (butenafine), is a novel antifungal agent of the class of benzylamine derivatives. Butenafine was investigated for its activity against guinea pig dermatophytosis caused by Trichophyton mentagrophytes or Microsporum canis in comparison with those of naftifine, tolnaftate, clotrimazole, and bifonazole. Topical butenafine showed excellent efficacy against dermatophytosis when it was applied once daily, and the effect was superior to those of all four reference drugs. When applied once at 24 or 48 h before infection, the drug exhibited excellent prophylactic efficacy against experimental T. mentagrophytes infection. The concentrations of butenafine in animal skin at 24 and 48 h after application of 0.2 ml of a 1% solution were several hundred times higher than those required to kill T. mentagrophytes and M. canis. The good efficacy of butenafine against dermatophytosis may be attributable to its fungicidal activity and long retention in the skin after topical application. PMID:2073116