Science.gov

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

  1. Stability indicating method for determination of nortriptyline hydrochloride using 3-methyl-2-benzothiazolinone hydrazone (MBTH).

    PubMed

    El Ragehy, N A; Abbas, S S; El-Khateeb, S Z

    2001-04-01

    A spectrophotometric procedure is described for determination of nortriptyline hydrochloride in pure and dosage form as well as in the presence of its degradate. 3-Methyl-2-benzothiazolinone hydrazone (MBTH) has been used as the chromogenic reagent, where aqueous solutions of the drug and reagent are treated with cerium(IV) ammonium sulphate in an acidic medium. Nortriptyline hydrochloride reacts to give a blue coloured product having two absorption maxima at 619 and 655 nm. Various parameters affecting the reaction have been studied. Beer's law is obeyed in the concentration range of 24-216 microg ml(-1) of nortriptyline hydrochloride, with mean percentage recoveries of 100.22+/-0.870 and 100.66+/-0.642% for both maxima, 619 and 655 nm, respectively. Results were statistically analyzed and compared with those obtained by applying the British Pharmacopoeia (1993) method. PMID:11274868

  2. Spectrophotometric determination of isoxsuprine hydrochloride using 3-methyl-2-benzothiazolinone hydrazone hydrochloride in spiked human urine and pharmaceuticals.

    PubMed

    Tharpa, Kalsang; Basavaiah, Kanakapura; Revanasiddappa, Hosakere Doddarevanna; Vinay, Kanakapura Basavaiah

    2010-06-15

    Two selective and sensitive spectrophotometric methods are proposed for the determination of isoxsuprine hydrochloride (ISX) in spiked human urine and in pharmaceuticals. The methods are based on the oxidative-coupling reaction between 3-methyl-2-benzothiazolinone hydrazone hydrochloride (MBTH) and ISX in the presence of Ce(SO(4))(2). The novelty of the proposed reaction is the formation of two different colored chromogens at two different pHs. The resulting product at pH<1.5 is a red colored chromogen peaking at 500nm (method A) and that formed between the pH 3.85 and 4.15, is violet colored with an absorption maximum at 580nm (method B). In both the methods, absorbance of the chromogen is found to increase linearly with the concentration of ISX as is corroborated by the correlation coefficients of 0.9989 and 0.9970, and the systems obey Beer's law over the ranges of 1.4-21.0 and 1.0-15.0microgml(-1), for method A and method B, respectively. The calculated molar absorptivities are 1.08 x 10(4) and 1.78 x 10(4)lmol(-1)cm(-1) for method A and method B, respectively with corresponding Sandell sensitivity values of 0.0311 and 0.0190microgcm(-2). The reaction stoichiometry, in both the methods, was evaluated by the limiting logarithmic method and was found to be 1:1 (ISX:MBTH). The methods were successfully applied to the determination of ISX in spiked human urine and pharmaceutical formulation. PMID:20441887

  3. Determination of airborne formaldehyde by active sampling on 3-methyl-2-benzothiazolinone hydrazone hydrochloride-coated glass fibre filters.

    PubMed

    Chan, W H; Shuang, S; Choi, M M

    2001-05-01

    Formaldehyde was sampled with the use of a standard miniature glass fibre filter coated with 3-methyl-2-benzothiazolinone hydrazone hydrochloride (MBTH). The formaldehyde hydrazone formed [i.e., the adduct of formaldehyde (HCHO) and MBTH] was desorbed from the filter with water and then oxidised by an iron(III) chloride-sulfamic acid solution to form a blue cationic dye in acidic medium which was subsequently determined by visible absorption at 628 nm. The recovery of HCHO as the cationic dye from MBTH-coated filters is 87-102% in the range 0.065-2.9 micrograms of HCHO. This corresponds to 4.3-193.3 micrograms m-3 in a 15 L air sample. The collection efficiency of the MBTH-coated filter is higher than 90%. When the filter sampling system is used in active mode, air can be sampled at a rate of up to 1 L min-1, affording an overall sensitivity of about 3 micrograms m-3, corresponding to about 2 ppb v/v HCHO at 1 atm and 273 K. The method was successfully applied to the determination of HCHO in samples of indoor and outdoor air with satisfactory results. PMID:11394322

  4. Highly sensitive reaction of nitrate with brucine and 3-methyl-2-benzothiazolinone hydrazone hydrochloride for the determination of nitrate in environmental samples.

    PubMed

    Nagaraja, Padmarajaiah; Kumar, Mattighatta Hemantha; Yathirajan, Hemmige; Prakash, Jainara

    2003-06-01

    A modified and highly sensitive spectrophotometric method for the determination of nitrate in trace quantities in environmental samples is described. The method is based on the reaction of nitrate ion with brucine and 3-methyl-2-benzothiazolinone hydrazone hydrochloride (MBTH) in sulfuric acid medium to yield a violet-colored product which is stable for over two days. The optimum photometric range for the determination of nitrate is 0.04-0.16 microg cm(-3) and the Sandell's sensitivity being 0.000279 microg cm(-2). The proposed method is applied to various water samples and the results indicate that the reaction is highly sensitive than the original brucine method. PMID:12834245

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

    PubMed

    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 R(2)=0.997. Beers law obeyed in the range of 0.068-17.2 μM with good linearity, absorbance y=0.044 C(bil)+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. PMID:20829101

  6. 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.

  7. Development of a selective and sensitive spectrophotometric method for the trace determination of thallium(III) using 3-methyl-2-benzothiazolinone hydrazone hydrochloride and N-(1-naphthyl)-ethylenediamine dihydrochloride.

    PubMed

    Nagaraja, Padmarajaiah; Al-Tayar, Naef Ghllab Saeed; Kumar, Anantharaman Shiva

    2008-01-01

    A simple, selective, sensitive, and rapid spectrophotometric method has been developed for the determination of thallium(III) using 3-methyl-2-benzothiazolinone hydrazone hydrochloride and N-(1-naphthyl)-ethylenediamine dihydrochloride. The obtained product had an absorption maximum of 590 nm. Beer's law was valid over the concentration range of 0.15-8 microg/mL. The molar absorptivity and Sandell's sensitivity of the colored system were 2.93 x 10(4) L/mol x cm and 0.00723 microg/mL, respectively. The effect of different acids on the sensitivity of the method, interference by foreign substances, the optimum reaction conditions, and other analytical parameters were evaluated. The proposed method has been successfully applied in the analysis of T1(III) in standard reference materials, synthetic mixtures, and water and urine samples. The performance of the proposed method was evaluated in terms of Student's t-test and variance ratio F-test, which indicated the significance of the proposed method over reported methods. PMID:18980127

  8. The acute toxicity and mutagenic potential of 3-methyl-2-benzothiazolinone hydrazone.

    PubMed

    Ballantyne, B; Slesinski, R S; Myers, R C

    1988-03-01

    3-Methyl-2-benzothiazolinone hydrazone (MBTH), widely used in analytical laboratories, was investigated for potential handling hazards. Tested as the hydrochloride, it was found to be of moderately high acute peroral toxicity with LD50 values in rabbits of 177 mg/kg (males) and 268 mg/kg (females), and in the rat 308 mg/kg (males) and 149 mg/kg (females). The major signs of toxicity, seen at peroral doses of 125 mg/kg and above, were convulsions. Although of low acute lethal percutaneous toxicity in rats (LD50 greater than 16 g/kg), rabbits were more sensitive with one of five males dying at an applied dose of 16 g/kg, and females having an LD50 of 12.3 g/kg; convulsions were seen in rabbits having applied cutaneous doses of 4 g/kg and above. There was no evidence for cutaneous inflammation after a 4 hour occluded contact with MBTH in rabbits, although following 24 hour occlusive contact in the acute percutaneous toxicity study there was erythema, edema, desquamation and, in a few animals, local necrosis. Ocular studies in rabbits indicated that, depending on the degree of contamination, MBTH produced mild to moderate eye irritation. In keeping with its low vapor pressure, there were no adverse effects from a 6 hour exposure of rats to an atmosphere saturated with any vapor produced from solid MBTH at ambient temperature. MBTH was positive in an Ames bacterial mutagenicity assay, particularly in the absence of metabolic activation. These studies indicate MBTH to be of moderately high acute peroral toxicity, of moderate percutaneous toxicity, a mild primary skin irritant, a mild to moderate eye irritant, and produced mutations in Salmonella. There is a need for skin and eye protection, and avoidance of swallowing, when handling MBTH. PMID:3291201

  9. Determination of manganese peroxidase activity with 3-methyl-2-benzothiazolinone hydrazone and 3-(dimethylamino)benzoic acid.

    PubMed

    Castillo, M P; Stenström, J; Ander, P

    1994-05-01

    This method was proposed earlier for measuring glucose in a peroxidase-glucose oxidase system but has not been studied for determination of manganese peroxidase (MnP) activity. The assay is based on the oxidative coupling of 3-methyl-2-benzothiazolinone hydrazone (MBTH) and 3-(dimethylamino)benzoic acid (DMAB). The reaction of MBTH and DMAB in the presence of H2O2, Mn2+, and MnP gives a deep purple-blue color with a broad absorption band with a peak at 590 nm. The extinction coefficient is high (53,000 M-1 cm-1), so low MnP activities can be detected. Lignin peroxidase and laccase, usually present in cultures of white rot fungi, gave little or no interference at the concentrations tested. However, slight interference from very high LiP activity may occur at very low MnP activity. PMID:8074299

  10. Badge-type diffusive sampler using 3-methyl-2-benzothiazolinone hydrazone for measuring formaldehyde in indoor air.

    PubMed

    Yim, Bongbeen; Jung, Euisuk

    2006-07-01

    The evaluation of a badge-type diffusive sampler for measuring formaldehyde using 3-methyl-2-benzothiazolinone hydrazone (MBTH) was investigated. On average, the formaldehyde concentration in blanks was reduced by approximately 31% by cleaning procedures. The cleaning techniques did not significantly differ in effectiveness. The maximum sampling rate was 22.4 +/- 3.5 mL min(-1) at MBTH concentrations of 0.05%. The formaldehyde concentration in blanks did not appreciably increase over a period of about 1 month at room temperature, and was 0.36 +/- 0.03 microg, with a relative standard deviation of 8%. The diffusive sampler had good precision and accuracy for measuring formaldehyde in indoor environments. For a 24-h exposure time, the limits of detection and quantification calculated with the field blanks were 9.7 and 13.8 ppb, respectively. The minimum exposure times were calculated based on the measured and calculated limits of quantification, the sampling rate, and the atmospheric formaldehyde concentration. The capacity of the diffusive sampler with 0.5% MBTH was 3 ppm h(-1), approximately 1.5-times the capacity when the MBTH concentrations were 0.05%. PMID:16837752

  11. A continuous spectrophotometric method for the determination of monophenolase activity of tyrosinase using 3-methyl-2-benzothiazolinone hydrazone.

    PubMed

    Rodríguez-López, J N; Escribano, J; García-Cánovas, F

    1994-01-01

    A continuous spectrophotometric method for the rapid determination of monophenolase activity of tyrosinase is described. This method is based on the coupling reaction between 3-methyl-2-benzothiazolinone hydrazone (MBTH) and the quinone products of the oxidation of various monophenols in the presence of tyrosinase. The chemical reaction between MBTH and o-quinone has been kinetically characterized, the lambda max and the molar absorptivity coefficients of the adducts have been calculated, and the stoichiometry of the reaction has been determined. The method is illustrated by measuring the enzymatic activity of mushroom tyrosinase during the hydroxylation of phenol and tyramine. The presence of MBTH in the reaction medium decreases the lag period present during the expression of monophenolase activity and the high epsilon values at 500-505 nm of the adducts make this method more sensitive than other continuous methods. The MBTH reaction in the presence of monophenols or o-diphenols has been optimized to stain tyrosinase obtained from different biological sources in electrophoresis gels. PMID:8135353

  12. A new peroxidase color reaction: oxidative coupling of 3-methyl-2-benzothiazolinone hydrazone (MBTH) with its formaldehyde azine. Application to glucose and choline oxidases.

    PubMed

    Capaldi, D J; Taylor, K E

    1983-03-01

    Hydrogen peroxide in the presence of horseradish peroxidase effects the oxidative coupling of 3-methyl-2-benzothiazolinone hydrazone with its formaldehyde azine to form a tetraazapentamethine dye. The blue chromophore, when formed at pH 3.5 and quenched with acetone or 1 N hydrochloric acid, has an extinction coefficient of 69 +/- 2 or 55 +/- 2 mM-1 cm-1, respectively. This chromogen system has been adapted for enzymatic determinations of hydrogen peroxide and of glucose in the 10- to 45-nmol range and of choline in the 5- to 20-nmol range. PMID:6342472

  13. Determination of ultratrace amounts of copper (II) by its catalytic effect on the oxidative coupling reaction of 3-methyl-2-benzothiazolinone hydrazone with N-ethyl-N-(2-hydroxy-3-sulfopropyl)-3,5-dimethoxyaniline.

    PubMed

    Ohno, S; Teshima, N; Watanabe, T; Itabashi, H; Nakano, S; Kawashima, T

    1996-10-01

    A spectrophotometric method was developed for the determination of ultratrace amounts of copper(II) based on its catalytic effect on the oxidative coupling reaction of 3-methyl-2-benzothiazolinone hydrazone with N-ethyl-N-(2-hydroxy-3-sulfopropyl)-3,5-dimethoxyaniline to produce an intensely coloured dye (lambda(max) = 525 nm) in the presence of hydrogen peroxide. In this reaction, pyridine acted as an effective activator for the catalysis of copper(II). By measuring the absorbance of the dye, copper(II) can be determined at the 0.002-0.1 ng cm(-3) (3.1 x 10(-11)-1.6 x 10(-9) mol dm(-3) level. The relative standard deviation for ten determinations of 0.06 ng cm(0-3) of copper(II) was 2.6%. The proposed method was successfully applied to the determination of copper(II) in tap water and biological material. PMID:9148646

  14. A rapid method for detection of tyrosinase activity in electrophoresis.

    PubMed

    Nellaiappan, K; Vinayagam, A

    1986-09-01

    This rapid and sensitive method for localizing tyrosinase in polyacrylamide slab gels is based on the condensation of Bestthorn's hydrazone (3 methyl-2-benzothiazolinone hydrazone hydrochloride) with the quinone obtained by enzymatic oxidation of phenol. Both monophenolase and diphenolase activities are localized by this method. PMID:3097880

  15. A method for demonstrating prophenoloxidase after electrophoresis.

    PubMed

    Nellaiappan, K; Vinayakam, A

    1993-07-01

    The demonstration of prophenoloxidase after electrophoresis is based on its activation by sodium dodecyl sulfate (SDS) or sodium oleate and staining the activated phenoloxidase with dopamine and 3-methyl-2-benzothiazolinone hydrazone hydrochloride (MBTH). A rapid method is presented for demonstrating the presence of activated phenoloxidase using polyacrylamide gel electrophoresis followed by staining in the presence of SDS or sodium oleate. PMID:7692984

  16. A new technique for staining catecholic residues in biological samples.

    PubMed

    Kalyani, R; Nellaiappan, K

    1989-01-01

    This technique for localizing catecholic residues in biological samples is based on the condensation of Besthorn's hydrazone (3-methyl-2-benzothiazolinone hydrazone hydrochloride (MBTH) with quinone residues obtained by the oxidation of catechols in the presence of ammonia. The product is a dark pink MBTH-quinone compound. This method is very sensitive and positive to catechol even at the 0.05 microgram level and the final product is chemically stable. PMID:2472680

  17. Flow-injection spectrophotometric determination of diclofenac sodium in pharmaceuticals and urine samples.

    PubMed

    García, M S; Albero, M I; Sánchez-Pedreño, C; Molina, J

    1998-06-01

    A sensitive and fast flow-injection spectrophotometric method for the determination of diclofenac sodium based on the formation of coloured compound with Ce(IV)-3-methyl-2-benzothiazolinone hydrazone hydrochloride (MBTH) in H2SO4 3 x 10(-2) M medium is proposed. Using the peak height as a quantitative parameter diclofenac was determined at 580 nm over the range 0.20-8.0 micrograms ml-1. The proposed method was successfully applied to the determination of diclofenac in pharmaceuticals and urine samples. PMID:9638579

  18. Spectrophotometric determination of pyridoxal and pyridoxal 5′-phosphate with 3-methyl-2-benzothiazolone hydrazone hydrochloride, and their selective assay

    PubMed Central

    Soda, Kenji; Yorifuji, Takamitsu; Misono, Haruo; Moriguchi, Mitsuaki

    1969-01-01

    A spectrophotometric method with 3-methyl-2-benzothiazolone hydrazone hydrochloride was developed for the determination of pyridoxal and pyridoxal 5′-phosphate, and for the selective determination of each in the presence of the other. Pyridoxal and pyridoxal 5′-phosphate react with the reagent to yield the azine derivatives, which give characteristic absorption spectra. The highest extinction values are obtained when pyridoxal and pyridoxal 5′-phosphate are incubated at pH values of about 3·4 and 8·0 respectively; their maxima are at 430nm. (∈ 2·74×104) and 380nm. (∈ 2·24×104) respectively. The azine of pyridoxal is only slightly soluble under the neutral and alkaline conditions, whereas that of pyridoxal 5′-phosphate is substantially insoluble in the acid pH range. This difference in solubility of the azines made possible the selective determination of pyridoxal and pyridoxal 5′-phosphate. α-Oxoglutarate and pyruvate are among the substances shown not to interfere with the assay of pyridoxal; their derivatives absorb appreciably only at wavelengths below 420nm. For the assay of pyridoxal 5′-phosphate in the presence of these compounds measurement at 390nm. is necessary. PMID:5820647

  19. Mixed ligand complex via zinc(II)-mediated in situ oxidative heterocyclization of hydrochloride salt of 2-chlorobenzaldehyde hydralazine hydrazone as potential of antihypertensive agent.

    PubMed

    Bakale, Raghavendra P; Naik, Ganesh N; Mangannavar, Chandrashekhar V; Muchchandi, Iranna S; Shcherbakov, I N; Frampton, Chris; Gudasi, Kalagouda B

    2014-02-12

    An unusual tetrahedral mixed ligand Zn(II) complex ZnT(L)Cl, where L = 2-chlorobenzaldehyde hydralazine hydrazone and T = in situ generated 3-(2-chlorophenyl)-1,2,4-triazolo[3,4-a]phthalazine is reported. Structure of the fused triazole has been confirmed by single crystal X-ray diffraction studies. Structure of Co(II), Ni(II), Cu(II) and Zn(II) complexes has been confirmed by spectral and analytical methods. Metal complexes have exhibited better activity in the fructose induced hypertension studies in animal model and are comparable with the standard. PMID:24378708

  20. 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

  1. 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.

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

    PubMed

    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 0.89×10(4) 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. PMID:25596545

  3. Spectrophotometric determination of some antidepressant drugs using 3-methylbenzothiazolin-2-one hydrazone.

    PubMed

    Revanasiddappa, H D; Manju, B

    1999-12-01

    A sensitive spectrophotometric method for the determination of amitriptyline hydrochloride, nortriptyline hydrochloride and doxepin hydrochloride in pure and dosage forms, is described. The method is based on the oxidative coupling of the drugs with 3-methylbenzothiazolin-2-one hydrazone in the presence of iron(III) chloride in 1 M hydrochloric acid. The commonly encountered excipients and additives do not interfere with the determinations. Results of the present method are comparable with those of official methods. The new method offers the advantage of simplicity and rapidity. PMID:10620735

  4. Development and validation of LC methods with visible detection using pre-column derivatization and mass detection for the assay of voglibose.

    PubMed

    Raman, Nanduri V V S S; Reddy, Kura Ratnakar; Prasad, Adapa V S S; Ramakrishna, Karipeddi

    2009-03-15

    Two sensitive and selective liquid chromatographic methods were developed for the assay of voglibose (VB) and validated as per International Conference on Harmonization (ICH) guidelines. First method is based on the pre-column derivatization of VB followed by visible detection (LC-VD) and second method involves mass spectrometric detection (LC-MS). In LC-VD method, VB was derivatized with sodium metaperiodate and 3-methyl-2-benzothiazolinone hydrazone hydrochloride monohydrate (MBTH). The derivatized color product of VB (DCPVB) was run through Novapak C18 (300 x 3.9 mm, 4 microm) column using the mobile phase containing buffer (0.01 M mixture of sodium di hydrogen orthophosphate and disodium hydrogen orthophosphate, pH 6.0) and acetonitrile in 35:65 v/v ratio. The eluted DCPVB was monitored at 667 nm. The fixation of optimum conditions in LC-VD method is described. DCPVB structure was confirmed by mass spectral analysis. In LC-MS method, VB was passed through Venusil XBPPH (150 x 4.6 mm, 5 microm) column using a 95:5 v/v mixture of 0.01% formic acid and methanol as mobile phase. The assay concentrations of VB in pure form and in tablets for LC-VD and LC-MS methods are 25 and 5 ngml(-1), respectively. PMID:19159812

  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. Selective and validated spectrophotometric methods for the determination of nicorandil in pharmaceutical formulations.

    PubMed

    Rahman, Nafisur; Ahmad, Yasmin; Azmi, Syed Najmul Hejaz

    2004-01-01

    Two simple and sensitive validated spectrophotometric methods have been described for the assay of nicorandil in drug formulations. Method A is based on the reaction of the drug with phloroglucinol-sulfanilic acid reagent in sulfuric acid medium to give yellow-colored product, which absorbs maximally at 425 nm. Method B uses the oxidative coupling of 3-methyl-2-benzothiazolinone hydrazone hydrochloride (MBTH) with DL- 3,4 - dihydroxyphenylalanine (DL-dopa) in the presence of nicorandil as oxidant in sulfuric acid medium to form an intensely colored product having maximum absorbance at 530 nm. Beer's law is obeyed in the concentration range 2.5 to 50.0 and 1.0 to 15.0 microg mL(-1) with methods A and B, respectively. Both methods have been successfully applied for the analysis of drug in pharmaceutical formulations. The reliability and the performance of the proposed methods are established by point and interval hypothesis and through recovery studies. The experimental true bias of all samples is smaller than +/-2%. PMID:15760099

  7. Kinetic spectrophotometric determination of ethamsylate in dosage forms.

    PubMed

    El-Enany, Nahed; Belal, Fathalla; Rizk, Mohamed

    2007-01-01

    A simple and sensitive kinetic method has been developed for the determination of ethamsylate (ESL) in its pharmaceutical preparations. The method is based upon oxidation of ESL with 3-methyl-2-benzothiazolinone hydrazone hydrochloride in presence of cerium (IV) ammonium sulfate at room temperature for 20 min. The absorbance of the reaction product is measured at 514 nm. The absorbance-concentration plot was rectilinear over the range of 4-30 microg/mL (r = 0.9999). The lower detection limit was 0.267 microl/mL (9.110 x 10(-6) M) and the lower quantitation limit was 0.808 microg/mL. The different experimental parameters affecting the development and stability of the reaction product were studied and optimized. The proposed method was applied to the determination of ESL in formulations, and the results obtained were in good agreement with those obtained using a reference method. The proposed method was also used for the in vitro detection of ESL in spiked human plasma at its therapeutic concentration level. PMID:17580619

  8. 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 ...

  9. A sensitive colorimetric method for the determination of imipramine hydrochloride and desipramine hydrochloride.

    PubMed

    el-Yazbi, F A; Korany, M A; Bedair, M

    1985-12-01

    A simple and rapid colorimetric method for the determination of imipramine hydrochloride and desipramine hydrochloride in their tablet formulations and in biological fluids is presented. The method is based on the reaction of these drugs with 3-methyl-2-benzothiazolone hydrazone in the presence of ferric chloride, with direct measurement at 635 nm. Cyclohexane was used to extract these drugs from serum and urine, at basic pH, by a single manual extraction. The method can detect 0.5 microgram/ml of each drug. The main advantages of this method are its simplicity and high sensitivity. PMID:4093508

  10. Development of a paper-type tyrosinase biosensor for detection of phenolic compounds.

    PubMed

    Şenyurt, Özge; Eyidoğan, Füsun; Yılmaz, Remziye; Öz, M Tufan; Özalp, V Cengiz; Arıca, Yakup; Öktem, Hüseyin A

    2015-01-01

    A low-cost, portable, and disposable paper-type tyrosinase biosensor was developed for determination of phenolic compounds, using a paper-strip absorption method. Tyrosinase and a chromophore (3-methyl-2-benzothiazolinone hydrazone) were immobilized on paper strips to manufacture the biosensor, which was tested on a nontoxic substrate (l-dopamine). The biosensor was responsive to phenolic compounds such as 4-chlorophenol, catechol, m-cresol, and p-cresol. The sensor showed stability for 70 days. The developed biosensor can be used for remote on-site qualitative monitoring of phenolic compounds in wastewater samples. PMID:24847915

  11. 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

  12. Hydrazones as substrates for cycloaddition reactions

    NASA Astrophysics Data System (ADS)

    Belskaya, N. P.; Eliseeva, A. I.; Bakulev, V. A.

    2015-12-01

    The [2+2]-, [4+2]- and [3+2]-cycloaddition reactions of hydrazones and 1,2-diazabuta-1,3-dienes, azomethine imines, nitrile imines and azomethine ylides formed upon hydrazone transformations with dienophiles, dipolarophiles and dienes are considered. The principal issues of structure and reactivity of active substrates and the influence of the reaction conditions and catalysts on the reaction regioselectivity and efficiency are discussed. The bibliography includes 288 references.

  13. 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

  14. Facile and sensitive spectrophotometric determination of synthetic pyrithroids in their formulations, water and grain samples.

    PubMed

    Kumar, K Suresh; Swaroop, B Lokanath; Suvardhan, K; Rekha, D; Jayaraj, B; Chiranjeevi, P

    2006-11-01

    A novel reagent was introduced for the facile and sensitive spectrophotometric determination of synthetic pyrethroids in their formulations (fenvalerate, cypermethrin and decamethrin), water and grain samples. These methods were based on the hydrolysis of synthetic pyrethroids under the alkaline conditions to form respective aldehyde groups. These groups were condensation with 3-methyl-2-benzothiazolinone hydrochloride (MBTH) to yield color derivatives having lambda(max) at 520 nm for fenvalerate, 516 nm for cypermethrin and 512 nm for decamethrin. The proposed method could be successfully applied for the determination of synthetic pyrethroids in their formulations, water and grain samples. PMID:16770503

  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. Cinacalcet hydrochloride.

    PubMed

    Barman Balfour, Julia A; Scott, Lesley J

    2005-01-01

    Oral cinacalcet hydrochloride (HCl) [Sensipar, Mimpara] is the first in a new class of therapeutic agents, the calcimimetics, and has a novel mechanism of action. It directly modulates the principal regulator of parathyroid hormone (PTH) secretion, namely the calcium-sensing receptor (CaR) on the chief cells in the parathyroid gland. Cinacalcet HCl reduces circulating PTH levels by increasing the sensitivity of the CaR to extracellular calcium. In three pivotal phase III, 26-week, randomised, double-blind, multicentre trials in chronic kidney disease (CKD) patients (n = 1136) on dialysis with uncontrolled secondary hyperparathyroidism (HPT), a significantly higher proportion of oral cinacalcet HCl 30-180 mg/day than placebo recipients achieved a reduction in intact PTH levels to < or =250 pg/mL. Cinacalcet HCl treatment also simultaneously lowered serum calcium and phosphorus, and calcium-phosphorous product levels. Notably, cinacalcet HCl proved effective in a broad range of CKD patients on dialysis with uncontrolled secondary HPT, regardless of disease severity, duration of dialysis treatment, dialysis modality, race, age, gender, or concurrent phosphate binder or vitamin D sterol use. Cinacalcet HCl (60-360 mg/day) also reduced elevated serum calcium levels by > or =1 mg/dL in 15 of 21 (71%) patients with parathyroid carcinoma in an open-label, multicentre, dose-titration trial. Cinacalcet HCl was generally well tolerated in clinical trials. Most treatment-emergent adverse events were mild to moderate in severity. PMID:15631545

  18. 4-Hydroxyanisole: the most suitable monophenolic substrate for determining spectrophotometrically the monophenolase activity of polyphenol oxidase from fruits and vegetables.

    PubMed

    Espn, J C; Tudela, J; Garca-Cnovas, F

    1998-05-15

    A continuous spectrophotometric method for determining the monophenolase activity of polyphenol oxidase from several plant sources is described. This assay method is based on the coupling reaction between 3-methyl-2-benzothiazolinone hydrazone and the quinone product of the oxidation of 4-hydroxyanisole in the presence of polyphenol oxidase. 4-Hydroxyanisole proved to be the best monophenol assayed to measure the monophenolase activity of polyphenol oxidase from apple, artichoke, avocado, medlar, pear, and strawberry. Kinetic constants of 4-hydroxyanisole were compared to those of p-hydroxyphenyl propionic acid, a very sensitive monophenol previously reported to assay the monophenolase activity of polyphenol oxidase from apple, pear, and mushroom. The high values of the maximum steady state rate obtained for 4-hydroxyanisole suggest the existence of high catalytic constant toward this monophenol. These kinetic values were supported by nuclear magnetic resonance assays which predicted the highest reactivity of 4-hydroxyanisole. Therefore nuclear magnetic resonance assays proved to be a valuable and useful tool to predict the best monophenolic substrate for plant polyphenol oxidases. The 3-methyl-2-benzothiazlolinone-adduct for 4-hydroxyanisole was stable, with high molar absorptivity at the optimum pHs of the polyphenol oxidases assayed. All this together makes the use of 4-hydroxyanisol as monophenolic substrate and 3-methyl-2-benzothiazolinone as coupling reagent the most sensitive and precise assay method up to date reported in the literature to determine the monophenolas activity of polyphenol oxidase from fruits and vegetables. PMID:9606152

  19. 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.

  20. 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.

  1. Hole mobilities in hydrazone-polycarbonate dispersions

    NASA Astrophysics Data System (ADS)

    Mack, J. X.; Schein, L. B.; Peled, A.

    1989-04-01

    Extensive characterization of the hole mobilities μ in dispersions of p-diethylamino- benzaldehyde-diphenyl hydrazone (DEH) in polycarbonate has been carried out. We report the effect of varying the electric field E, temperature T, and spacing between DEH molecules ρ on μ. These data are analyzed by a procedure that allows proper separation of the functional dependencies of the mobility on E, T, and ρ. It is found that lnμ is proportional to En(T-1-T-10), where n=0.5 and T0 is a fitted parameter which decreases with increasing ρ, behavior opposite to the dependence of the glass transition temperature on ρ. These experimental results are not yet understood theoretically. Our procedure for separating the ρ and T dependence is applied to data taken on DEH-polycarbonate and to data taken from the literature on another molecularly doped polymer system, N,N'-diphenyl-N,N'-bis (3-methylphenyl)-(1,1'-biphenyl)-4,4'-diamine (TPD) in polycarbonate. For DEH-polycarbonate, the activation energy is found to be independent of ρ. In contrast, for TPD-polycarbonate the activation energy is strongly dependent on ρ. Our data suggest that small-polaron hopping is occurring in molecularly doped polymers; this different dependence of the activation energy on ρ is consistent with different small-polaron hopping regimes, adiabatic and nonadiabatic, in these two systems.

  2. Optical determination of L-tyrosine based on eggshell membrane immobilized tyrosinase.

    PubMed

    Li, Yong Jin

    2010-01-01

    An optical biosensor based on the eggshell membrane immobilized tyrosinase is described for the detection of L-tyrosine (L-Tyr). The detection scheme was based on the measurement of absorption value of color adduct resulting from the reaction of 3-methyl-2-benzothiazolinone hydrazone and dopa-quinone produced from the enzymatic oxidation of L-Tyr. The prepared biosensor demonstrated optimum activity at pH 7, optimum temperature range of 20-40 degrees C and a linear response for the L-Tyr concentration in range of 5-200 microM. It also showed good operation stability for repeated measurements (over 300 times) and storage stability after it had been kept at 4 degrees C for 3 months. PMID:21313820

  3. Soybean lipoxygenases-1, -2a, -2b and -2c do not contain PQQ.

    PubMed

    Michaud-Soret, I; Daniel, R; Chopard, C; Mansuy, D; Cucurou, C; Ullrich, V; Chottard, J C

    1990-11-15

    Soybean isoenzymes lipoxygenases-1, -2a, -2b and -2c were examined spectroscopically for the presence of covalently bound pyrrolo quinoline quinone (PQQ) after derivatization by phenylhydrazine (PH), 2,4-dinitrophenylhydrazine (DNPH) and 3-methyl-2-benzothiazolinone hydrazone (MBTH). DNPH derivatization of PQQ after a pronase digestion step of lipoxygenase-1 in the presence of an anion exchange gel fixing the cofactor was also investigated. None of these experiments provided evidence for the presence of PQQ contrary to previous report by Van der Meer et al (1). We have checked, by EPR spectroscopy, that the three reactants used were able to reduce the active site ferric iron. Our results were confirmed by the absence of enzyme inhibition by cis- and trans-1,2-diaminocyclohexane or benzylamine in the presence of NaBH3CN which have been reported to react with PQQ and to inactivate quinoproteins (2,3). PMID:2173916

  4. Membrane solubilization technique for spectrophotometric determination of trace formaldehyde in rainwater.

    PubMed

    Murai, Keita; Okano, Mayumi; Kuramitz, Hideki; Hata, Noriko; Kawakami, Takanori; Taguchi, Shigeru

    2008-01-01

    A simple and sensitive spectrophotometry for formaldehyde in water by membrane solubilization technique was proposed. Formaldehyde was converted into a blue cationic dye with 3-methyl-2-benzothiazolinone hydrazone, and the dye was retained on a membrane filter as an ion-associate with tetraphenylborate anion. The filter retaining the blue dye was dissolved in 2-methoxyethanol containing sulfuric acid, and the absorbance of the solution was measured at 670 nm against the reagent blank. The formaldehyde from 0.007 to 0.2 mg L(-1) was determined with an RSD of less than 5%, and the detection limit was 0.002 mg L(-1). The proposed method was very simple and rapid. Twenty minutes was sufficient for the entire analytical procedure. When the method was applied to rainwater, the analytical results were in good agreement with those obtained by GC/MS. PMID:18997375

  5. Synthesis and anticancer activity of (E)-2-benzothiazole hydrazones.

    PubMed

    Lindgren, Eric B; de Brito, Monique A; Vasconcelos, Thatyana R A; de Moraes, Manuel O; Montenegro, Raquel C; Yoneda, Julliane D; Leal, Kátia Z

    2014-10-30

    Benzothiazole hydrazones have been synthesized and evaluated for their in vitro antiproliferative activity against three human cancer cell lines: HL-60 (leukemia), MDAMB-435 (breast) and HCT-8 (colon). The good cytotoxicity for the three cancer cell lines and theoretical profile of compounds 3o and 3p pointed them as promising lead molecules for anticancer drug design. PMID:25147145

  6. 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.

  7. 21 CFR 520.2002 - Propiopromazine hydrochloride.

    Code of Federal Regulations, 2011 CFR

    2011-04-01

    ... Propiopromazine hydrochloride. (a) Chemical name. 1-Propanone, 1- phenothiazine-2-yl]-, monohydrochloride. (b... tranquilization desired. Note: Not for use with organophosphates and/or procaine hydrochloride, as...

  8. 21 CFR 520.2002 - Propiopromazine hydrochloride.

    Code of Federal Regulations, 2013 CFR

    2013-04-01

    ... Propiopromazine hydrochloride. (a) Chemical name. 1-Propanone, 1- phenothiazine-2-yl]-, monohydrochloride. (b... tranquilization desired. Note: Not for use with organophosphates and/or procaine hydrochloride, as...

  9. 21 CFR 520.2002 - Propiopromazine hydrochloride.

    Code of Federal Regulations, 2014 CFR

    2014-04-01

    ... Propiopromazine hydrochloride. (a) Chemical name. 1-Propanone, 1- phenothiazine-2-yl]-, monohydrochloride. (b... tranquilization desired. Note: Not for use with organophosphates and/or procaine hydrochloride, as...

  10. 21 CFR 520.2002 - Propiopromazine hydrochloride.

    Code of Federal Regulations, 2010 CFR

    2010-04-01

    ... Propiopromazine hydrochloride. (a) Chemical name. 1-Propanone, 1- phenothiazine-2-yl]-, monohydrochloride. (b... tranquilization desired. Note: Not for use with organophosphates and/or procaine hydrochloride, as...

  11. 21 CFR 520.2002 - Propiopromazine hydrochloride.

    Code of Federal Regulations, 2012 CFR

    2012-04-01

    ... Propiopromazine hydrochloride. (a) Chemical name. 1-Propanone, 1- phenothiazine-2-yl]-, monohydrochloride. (b... tranquilization desired. Note: Not for use with organophosphates and/or procaine hydrochloride, as...

  12. 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.

  13. 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

  14. Diaryl Hydrazones as Multifunctional Inhibitors of Amyloid Self-Assembly†

    PubMed Central

    Török, Béla; Sood, Abha; Bag, Seema; Tulsan, Rekha; Ghosh, Sanjukta; Borkin, Dmitry; Kennedy, Arleen R.; Melanson, Michelle; Madden, Richard; Zhou, Weihong; LeVine, Harry; Török, Marianna

    2013-01-01

    The design and application of an effective, new class of multifunctional small molecule inhibitors of amyloid self-assembly are described. Several compounds, based on the diaryl hydrazone scaffold were designed. Forty-four substituted derivatives of this core structure were synthesized using a variety of benzaldehydes and phenylhydrazines and were characterized. The inhibitor candidates were evaluated in multiple assays, including the inhibition of Aβ fibrillogenesis and oligomer formation and the reverse processes, the disassembly of preformed fibrils and oligomers. Since the structure of the hydrazone-based inhibitors mimic the redox features of the antioxidant resveratrol the radical scavenging effect of the compounds was evaluated by colorimetric assays against 2,2-diphenyl-lpicrylhydrazyl (DPPH) and superoxide radicals. The hydrazone scaffold was active in all of the different assays. The structure-activity relationship revealed that the substituents on the aromatic rings had considerable effect on the overall activity of the compounds. The inhibitors showed strong activity in the fibrillogenesis inhibition and disassembly, and even greater potency in the inhibition of oligomer formation and oligomer disassembly. Supporting the quantitative fluorometric and colorimetric assays, size exclusion chromatographic studies indicated that the best compounds practically eliminated or substantially inhibited the formation of soluble, aggregated Aβ species, as well. Atomic Force Microscopy was also applied to monitor the morphology of Aβ deposits. The compounds also possessed the predicted antioxidant properties; approximately 30% of the synthesized compounds showed equal or better radical scavenging effect than resveratrol or ascorbic acid. PMID:23346953

  15. 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(II) > Copper(II) ≈ Palladium(II) >> Iron(III). PMID:21708023

  16. 21 CFR 184.1676 - Pyridoxine hydrochloride.

    Code of Federal Regulations, 2014 CFR

    2014-04-01

    ... 21 Food and Drugs 3 2014-04-01 2014-04-01 false Pyridoxine hydrochloride. 184.1676 Section 184... as GRAS § 184.1676 Pyridoxine hydrochloride. (a) Pyridoxine hydrochloride (C8H11NO3·HCl, CAS Reg. No... foods as defined in § 170.3(n)(37) of this chapter. Pyridoxine hydrochloride may be used in...

  17. Catalytic enantioselective hydrogenation of N-alkoxycarbonyl hydrazones: a practical synthesis of chiral hydrazines.

    PubMed

    Yoshikawa, Naoki; Tan, Lushi; McWilliams, J Christopher; Ramasamy, Deepa; Sheppard, Ruth

    2010-01-15

    An enantioselective hydrogenation of hydrazones catalyzed by Rh complexes (Rh-Josiphos or Rh-Taniaphos) has been developed. The protocol can be applied to hydrazones with three different protective groups (Boc, Cbz, and methoxycarbonyl), allowing for selective deprotection and further elaboration of the hydrazine products in the presence of other functional groups. PMID:20017501

  18. 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

  19. Reductive Chlorination and Bromination of Ketones via Trityl Hydrazones.

    PubMed

    Reyes, Julius R; Rawal, Viresh H

    2016-02-01

    A method is presented for the direct transformation of a ketone to the corresponding reduced alkyl chloride or bromide. The process involves the reaction of a ketone trityl hydrazone with tBuOCl to give a diazene which readily collapses to the α-chlorocarbinyl radical, reduction of which by a hydrogen atom source gives the alkyl chloride product. The use of N-bromosuccinimide provides the corresponding alkyl bromide. This unique transformation provides a reductive halogenation that complements Barton's redox-neutral vinyl halide synthesis. PMID:26823122

  20. Metronidazole hydrazone conjugates: Design, synthesis, antiamoebic and molecular docking studies.

    PubMed

    Ansari, Mohammad Fawad; Siddiqui, Shadab Miyan; Agarwal, Subhash M; Vikramdeo, Kunwar Somesh; Mondal, Neelima; Azam, Amir

    2015-09-01

    Metronidazole hydrazone conjugates (2-13) were synthesized and screened in vitro for antiamoebic activity against HM1: IMSS strain of Entamoeba histolytica. Six compounds were found to be better inhibitors of E. histolytica than the reference drug metronidazole. These compounds showed greater than 50-60% viability against HeLa cervical cancer cell line after 72 h treatment. Also, molecular docking study was undertaken on E. histolytica thioredoxin reductase (EhTHRase) protein which showed significant binding affinity in the active site. Out of the six actives, some of the compounds showed lipophilic characteristics. PMID:26174554

  1. 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

  2. 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

  3. 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.

  4. 21 CFR 522.1222b - Ketamine hydrochloride with promazine hydrochloride and aminopentamide hydrogen sulfate injection.

    Code of Federal Regulations, 2011 CFR

    2011-04-01

    ... 21 Food and Drugs 6 2011-04-01 2011-04-01 false Ketamine hydrochloride with promazine 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...

  5. 21 CFR 522.1222b - Ketamine hydrochloride with promazine hydrochloride and aminopentamide hydrogen sulfate injection.

    Code of Federal Regulations, 2012 CFR

    2012-04-01

    ... 21 Food and Drugs 6 2012-04-01 2012-04-01 false Ketamine hydrochloride with promazine 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...

  6. 21 CFR 522.1222b - Ketamine hydrochloride with promazine hydrochloride and aminopentamide hydrogen sulfate injection.

    Code of Federal Regulations, 2013 CFR

    2013-04-01

    ... 21 Food and Drugs 6 2013-04-01 2013-04-01 false Ketamine hydrochloride with promazine 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...

  7. 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....

  8. 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...

  9. 21 CFR 582.5875 - Thiamine hydrochloride.

    Code of Federal Regulations, 2013 CFR

    2013-04-01

    ... 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...

  10. 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....

  11. 21 CFR 184.1676 - Pyridoxine hydrochloride.

    Code of Federal Regulations, 2013 CFR

    2013-04-01

    ... 21 Food and Drugs 3 2013-04-01 2013-04-01 false Pyridoxine hydrochloride. 184.1676 Section 184... Listing of Specific Substances Affirmed as GRAS § 184.1676 Pyridoxine hydrochloride. (a) Pyridoxine... foods as defined in § 170.3(n)(37) of this chapter. Pyridoxine hydrochloride may be used in...

  12. 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....

  13. 21 CFR 184.1676 - Pyridoxine hydrochloride.

    Code of Federal Regulations, 2011 CFR

    2011-04-01

    ... 21 Food and Drugs 3 2011-04-01 2011-04-01 false Pyridoxine hydrochloride. 184.1676 Section 184... Listing of Specific Substances Affirmed as GRAS § 184.1676 Pyridoxine hydrochloride. (a) Pyridoxine... foods as defined in § 170.3(n)(37) of this chapter. Pyridoxine hydrochloride may be used in...

  14. 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....

  15. 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....

  16. 21 CFR 184.1676 - Pyridoxine hydrochloride.

    Code of Federal Regulations, 2012 CFR

    2012-04-01

    ... 21 Food and Drugs 3 2012-04-01 2012-04-01 false Pyridoxine hydrochloride. 184.1676 Section 184... Listing of Specific Substances Affirmed as GRAS § 184.1676 Pyridoxine hydrochloride. (a) Pyridoxine... foods as defined in § 170.3(n)(37) of this chapter. Pyridoxine hydrochloride may be used in...

  17. 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.

  18. Gold(I)-Catalyzed Intermolecular Cycloaddition of Allenamides with α,β-Unsaturated Hydrazones: Efficient Access to Highly Substituted Cyclobutanes

    PubMed Central

    2014-01-01

    α,β-Unsaturated N,N-dialkyl hydrazones undergo a mild [2 + 2] cycloaddition to allenamides when treated with a suitable gold catalyst. The method, which represents the first application of N,N-dialkyl hydrazones in gold catalysis, is compatible with a wide variety of substituents at the alkenyl moiety of the hydrazone component, proceeds with excellent levels of regio- and diastereoselectivity, and provides densely substituted cyclobutanes with good to excellent yields. PMID:25406491

  19. Diastereo-Divergent Synthesis of Saturated Azaheterocycles Enabled by tBuOK-Mediated Hydroamination of Alkenyl Hydrazones.

    PubMed

    Kaga, Atsushi; Peng, Xingao; Hirao, Hajime; Chiba, Shunsuke

    2015-12-21

    Diastereo-divergent synthesis of saturated azaheterocycles has been achieved by tBuOK-mediated hydroamination of alkenyl hydrazones. DFT calculations suggested that the cation-π interactions between a potassium cation and aryl substituents on hydrazones give rise to 2,5-cis selectivity in pyrrolidines, which were synthesized by the reaction of γ,δ-unsaturated N-benzyl hydrazones. By contrast, 2,5-trans selectivity was observed when an isopropyl group was used as the substituent on hydrazones. An unusual 2,6-trans selectivity in piperidine formation was also realized using the present strategy. PMID:26568285

  20. Simple hydrazone building blocks for complicated functional materials.

    PubMed

    Tatum, Luke A; Su, Xin; Aprahamian, Ivan

    2014-07-15

    CONSPECTUS: The ability to selectively and effectively control various molecular processes via specific stimuli is a hallmark of the complexity of biological systems. The development of synthetic structures that can mimic such processes, even on the fundamental level, is one of the main goals of supramolecular chemistry. Having this in mind, there has been a foray of research in the past two decades aimed at developing molecular architectures, whose properties can be modulated using external inputs. In most cases, reversible conformational, configurational, or translational motions, as well as bond formation or cleavage reactions have been used in such modulations, which are usually initiated using inputs including, irradiation, metalation, or changes in pH. This research activity has led to the development of a diverse array of impressive adaptive systems that have been used in showcasing the potential of molecular switches and machines. That being said, there are still numerous obstacles to be tackled in the field, ranging from difficulties in getting molecular switches to communicate and work together to complications in integrating and interfacing them with surfaces and bulk materials. Addressing these challenges will necessitate the development of creative new approaches in the field, the improvement of the currently available materials, and the discovery of new molecular switches. This Account will describe how our quest to design new molecular switches has led us to the development of structurally simple systems that can be used for complicated functions. Our focus on the modular and tunable hydrazone functional group was instigated by the desire to simplify the structure and design of molecular switches in order to circumvent multistep synthesis. We hypothesized that by avoiding this synthetic bottleneck, which is one of the factors that hinder fast progress in the field, we can expedite the development and deployment of our adaptive materials. It should be noted though that designing structurally simple switches cannot be an end goal by itself! Therefore, we showed that our molecules can be used in applications that are beyond a simple molecular switching event (i.e., the control of the photophysical properties of liquid crystals and multistep switching cascades). While focusing on these switches, we discovered that the hydrazones can be easily transformed, using straightforward one-step reactions, into visible light activated azo switches, and two different families of fluorophores that can be used in sensing applications. These findings demonstrate that our approach of developing simple systems for sophisticated functions is not limited to the field of molecular switches and machines but can also encompass other adaptive materials. PMID:24766362

  1. 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

  2. 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

  3. 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).

  4. 21 CFR 522.2002 - Propiopromazine hydrochloride injection.

    Code of Federal Regulations, 2013 CFR

    2013-04-01

    ... § 522.2002 Propiopromazine hydrochloride injection. (a) Chemical name. 1-Propanone, 1- phenothiazine-2... and/or procaine hydrochloride since phenothiazines may potentiate the toxicity of organophosphates...

  5. 21 CFR 522.2002 - Propiopromazine hydrochloride injection.

    Code of Federal Regulations, 2012 CFR

    2012-04-01

    ... § 522.2002 Propiopromazine hydrochloride injection. (a) Chemical name. 1-Propanone, 1- phenothiazine-2... and/or procaine hydrochloride since phenothiazines may potentiate the toxicity of organophosphates...

  6. 21 CFR 522.2002 - Propiopromazine hydrochloride injection.

    Code of Federal Regulations, 2010 CFR

    2010-04-01

    ... § 522.2002 Propiopromazine hydrochloride injection. (a) Chemical name. 1-Propanone, 1- phenothiazine-2... and/or procaine hydrochloride since phenothiazines may potentiate the toxicity of organophosphates...

  7. 21 CFR 522.2002 - Propiopromazine hydrochloride injection.

    Code of Federal Regulations, 2011 CFR

    2011-04-01

    ... § 522.2002 Propiopromazine hydrochloride injection. (a) Chemical name. 1-Propanone, 1- phenothiazine-2... and/or procaine hydrochloride since phenothiazines may potentiate the toxicity of organophosphates...

  8. 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.

  9. Asymmetric Synthesis of 2-Substituted Oxetan-3-ones via Metalated SAMP/RAMP Hydrazones

    PubMed Central

    2013-01-01

    2-Substituted oxetan-3-ones can be prepared in good yields and enantioselectivities (up to 84% ee) by the metalation of the SAMP/RAMP hydrazones of oxetan-3-one, followed by reaction with a range of electrophiles that include alkyl, allyl, and benzyl halides. Additionally, both chiral 2,2- and 2,4-disubstituted oxetan-3-ones can be made in high ee (86–90%) by repetition of this lithiation/alkylation sequence under appropriately controlled conditions. Hydrolysis of the resultant hydrazones with aqueous oxalic acid provides the 2-substituted oxetan-3-ones without detectable racemization. PMID:24152298

  10. Optimized protocol for the radioiodination of hydrazone-type polymer drug delivery systems.

    PubMed

    Sedláček, Ondřej; Kučka, Jan; Hrubý, Martin

    2014-10-27

    Hydrazone conjugates of polymers with doxorubicin represent a very promising tool for cancer chemotherapy. However, these conjugates are very difficult to radiolabel with iodine radionuclides, which possess otherwise very advantageous nuclear properties to, e.g., follow biodistribution. In this study, we developed a robust protocol for the high-yield radioiodination of hydrazone-type drug delivery systems with doxorubicin. In particular, it is crucial that the polymer radioiodination step be performed before the deprotection of the hydrazide and doxorubicin binding. PMID:25464189

  11. Linear copper 'chain' complexes with bulky tritopic hydrazone ligands--structural and magnetic studies.

    PubMed

    Tandon, Santokh S; Dawe, Louise N; Milway, Victoria A; Collins, Julie L; Thompson, Laurence K

    2007-05-21

    Tritopic 2,6-picolyl-bis-hydrazone ligands with bulky terminal groups derived from phenyl-pyridyl ketone do not form the expected [3 x 3] grids on reaction with copper(II), but instead form Cu8 'pinwheels', and in the present case linear trinuclear, pentanuclear and chain structures also. Direct bridging between copper ions occurs through micro2-N-N diazine groups, and longer O-C-N hydrazone connections, leading to moderately strong antiferromagnetic exchange between adjacent metal centres. Structural and magnetic properties are discussed in the context of specific orthogonal and non-orthogonal bridges, which can be distinguished and quantified. PMID:17702175

  12. 21 CFR 520.222 - Bunamidine hydrochloride.

    Code of Federal Regulations, 2014 CFR

    2014-04-01

    ... 21 Food and Drugs 6 2014-04-01 2014-04-01 false Bunamidine hydrochloride. 520.222 Section 520.222 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 § 520.222 Bunamidine hydrochloride. (a) Chemical name....

  13. Catalytic asymmetric construction of chiral hydropyridazines via conjugate addition of N-monosubstituted hydrazones to enones.

    PubMed

    Wu, Wenbin; Yuan, Xiaoqian; Hu, Juan; Wu, Xinxin; Wei, Yuan; Liu, Zunwu; Lu, Junzhu; Ye, Jinxing

    2013-09-01

    The first example of a highly enantioselective and scalable formal diaza-ene reaction between N-monosubstituted hydrazones and enones catalyzed by a simple chiral primary-second diamine salt has been developed. The catalytic process provides a highly practical and stereoselective synthetic method for chiral hydropyridazines. PMID:23964662

  14. 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...

  15. Quantification of acetaminophen by oxidation with tyrosinase in the presence of Besthorn's hydrazone.

    PubMed

    Valero, Edelmira; Carrión, Pedro; Varón, Ramón; García-Carmona, Francisco

    2003-07-15

    A method for the quantitative determination of acetaminophen by measuring the kinetics of its oxidation by the enzyme tyrosinase in the presence of the nucleophilic agent 3-methyl-2-benzothiazolone hydrazone (Besthorn's hydrazone) is described. The hydrazone traps the o-quinone product of the catalytic activity, 4-acetamido-o-benzoquinone, thus increasing the level of the catecholic intermediate, 3'-hydroxyacetaminophen, in the pathway, as was shown by liquid chromatography. This reduces the time necessary for the steady state to be reached and increases the steady state oxidation rate, reaching activations of 124 times at an initial concentration of 3mM hydrazone. Despite being rapid and simple the method is thorough and provides a linear range of quantification of the drug from 10 nmol/ml to 1.4 micromol/ml. The assay can be performed in continuous or discontinuous form, meaning that it can be used with the immobilized enzyme for the design of specific biosensors. PMID:12814621

  16. Colorimetric assay of sialic acid by a methyl-3-benzothiazolinone-2-hydrazone reactant.

    PubMed

    Massamiri, Y; Beljean, M; Durand, G; Feger, J; Pays, M; Agneray, J

    1978-12-01

    A colorimetric assay of sialic acid has been developed in which bound sialic acid is oxidized by periodic acid so as to quantitatively release formaldehyde. In the second step of the reaction formaldehyde reacts with methyl-3-benzothiazolinone-2-hydrazone, giving a colored compound. This method does not require a prior hydrolysis and presents the advantage of great accuracy. PMID:9762148

  17. 21 CFR 522.883 - Etorphine hydrochloride injection.

    Code of Federal Regulations, 2013 CFR

    2013-04-01

    ... 21 Food and Drugs 6 2013-04-01 2013-04-01 false Etorphine hydrochloride injection. 522.883 Section... § 522.883 Etorphine hydrochloride injection. (a) Chemical name. 6,7,8,14 - tetrahydro - alpha - methyl... milliliter of etorphine hydrochloride injection, veterinary, contains 1 mg of etorphine hydrochloride...

  18. 21 CFR 522.883 - Etorphine hydrochloride injection.

    Code of Federal Regulations, 2012 CFR

    2012-04-01

    ... 21 Food and Drugs 6 2012-04-01 2012-04-01 false Etorphine hydrochloride injection. 522.883 Section... § 522.883 Etorphine hydrochloride injection. (a) Chemical name. 6,7,8,14 - tetrahydro - alpha - methyl... milliliter of etorphine hydrochloride injection, veterinary, contains 1 mg of etorphine hydrochloride...

  19. 21 CFR 522.883 - Etorphine hydrochloride injection.

    Code of Federal Regulations, 2011 CFR

    2011-04-01

    ... 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....

  20. 21 CFR 522.883 - Etorphine hydrochloride injection.

    Code of Federal Regulations, 2010 CFR

    2010-04-01

    ... 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....

  1. 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 Naloxone hydrochloride injection. (a) Specifications. Naloxone hydrochloride injection is an aqueous sterile solution containing 0.4 milligram of naloxone hydrochloride per milliliter. (b)...

  2. Comparison of Hydrazone Heterobifunctional Crosslinking Agents for Reversible Conjugation of Thiol-Containing Chemistry

    PubMed Central

    Christie, R. James; Anderson, Diana J.; Grainger, David W.

    2010-01-01

    Reversible covalent conjugation chemistries that allow site- and condition-specific coupling and uncoupling reactions are attractive components in nanotechnologies, bioconjugation methods, imaging and drug delivery systems. Here, we compare three heterobifunctional crosslinkers, containing both thiol- and amine- reactive chemistry, to form pH-labile hydrazones with hydrazide derivatives of the known and often published water-soluble polymer, poly[N-(2-hydroxypropyl methacrylamide)] (pHPMA), while subsequently coupling thiol-containing molecules to the crosslinker via maleimide addition. Two novel crosslinkers were prepared from the popular heterobifunctional crosslinking agent, succinimidyl-4-(N-maleimidomethyl) cyclohexane-1-carboxylate (SMCC), modified to contain either terminal aldehyde groups (i.e., 1-(N-3-propanal)-4-(N-maleimidomethyl) cyclohexane carboxamide, PMCA) or methylketone groups (i.e., 1-(N-3-butanone)-4-(N-maleimidomethyl) cyclohexane carboxamide, BMCA). A third crosslinking agent was the commercially available N-4-acetylphenyl maleimide (APM). PMCA and BMCA exhibited excellent reactivity towards hydrazide-derivatized pHPMA with essentially complete hydrazone conjugation to polymer reactive sites, while APM coupled only ~ 60% of available reactive sites on the polymer despite a 3-fold molar excess relative to polymer hydrazide groups. All polymer hydrazone conjugates bearing these bifunctional agents were then further reacted with thiol-modified tetramethylrhodamine dye, confirming crosslinker maleimide reactivity after initial hydrazone polymer conjugation. Incubation of dye-labeled polymer conjugates in phosphate buffered saline at 37°C showed that hydrazone coupling resulting from APM exhibited the greatest difference in stability between pH 7.4 and 5.0, with hydrolysis and dye release increased at pH 5.0 over a 24hr incubation period. Polymer conjugates bearing hydrazones formed from crosslinker BMCA exhibited intermediate stability with hydrolysis much greater at pH 5.0 at early time points, but hydrolysis at pH 7.4 was significant after 5 hrs. Hydrazones formed with the PMCA crosslinker showed no difference in release rates at pH 7.4 and 5.0. PMID:20695431

  3. Cardiovascular responses to mianserin hydrochloride

    PubMed Central

    Burgess, C. D.; Turner, P.; Wadsworth, Jane

    1978-01-01

    1 The cardiovascular responses of mianserin hydrochloride and tricyclic antidepressant drugs were investigated using non-invasive methods of cardiac investigation. A study of the interaction of mianserin and antihypertensive drug therapy is reported. 2 In six normal volunteers, mianserin hydrochloride 20 mg was shown to prolong the corrected Q-T interval at 150 min (P<0.001). It did not affect heart rate, systolic time intervals or the peak normalized derivative of the apexcardiogram. Amitriptyline 50 mg increased the corrected pre-ejection period interval (PEPI) and the PEP/left ventricular ejection time (LVET) ratio of the systolic time intervals at 150 min (P<0.001). Q-T interval was shortened at 90 minutes. 3 In a double-blind patient study, clomipramine increased heart rate, P-R interval, QRS and corrected Q-T interval in one patient at 2 weeks. Mianserin prolonged corrected Q-T interval at 1 week but this returned to the pretreatment time by 2 weeks in two patients. 4 In an open study, mianserin 20 mg three times daily did not antagonize the hypotensive action of propranolol or propranolol and hydrallazine in three patients. 5 In a double-blind study in three patients with desmethylimipramine 25 mg three times daily, mianserin 20 mg three times daily did not antagonize the hypotensive action of either guanethidine or bethanidine. PMID:341940

  4. 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.

  5. 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.

  6. 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

  7. 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.

  8. Palladium-Catalyzed C(sp(2) )-H Alkylation of Aldehyde-Derived Hydrazones with Functionalized Difluoromethyl Bromides.

    PubMed

    Prieto, Alexis; Melot, Romain; Bouyssi, Didier; Monteiro, Nuno

    2016-01-01

    A palladium-catalyzed C(sp(2) )-H difluoromethylation of aldehyde-derived hydrazones using bromodifluoromethylated compounds to afford the corresponding functionalized difluoromethylketone hydrazones has been established. It is proposed that a radical/SET mechanism proceeding via a difluoroalkyl radical may be involved in the catalytic cycle. Applications of the methodology to the synthesis of ?,?-difluoro-?-ketoesters and ?,?-difluoroketones (RCOCF2 H) have been illustrated. PMID:26676834

  9. A novel asymmetric synthesis of cinacalcet hydrochloride

    PubMed Central

    Gorentla, Laxminarasimhulu; Dubey, Pramod K

    2012-01-01

    Summary A novel route to asymmetric synthesis of cinacalcet hydrochloride by the application of (R)-tert-butanesulfinamide and regioselective N-alkylation of the naphthyl ethyl sulfinamide intermediate is described. PMID:23019473

  10. 21 CFR 522.2470 - Tiletamine hydrochloride and zolazepam hydrochloride for injection.

    Code of Federal Regulations, 2011 CFR

    2011-04-01

    ... 21 Food and Drugs 6 2011-04-01 2011-04-01 false Tiletamine hydrochloride and zolazepam hydrochloride for injection. 522.2470 Section 522.2470 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT... analgesia. (2) Amount. Expressed as milligrams of the drug combination: (i) In healthy dogs: An...

  11. 21 CFR 522.2470 - Tiletamine hydrochloride and zolazepam hydrochloride for injection.

    Code of Federal Regulations, 2012 CFR

    2012-04-01

    ... 21 Food and Drugs 6 2012-04-01 2012-04-01 false Tiletamine hydrochloride and zolazepam hydrochloride for injection. 522.2470 Section 522.2470 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT... analgesia. (2) Amount. Expressed as milligrams of the drug combination: (i) In healthy dogs: An...

  12. 21 CFR 522.2470 - Tiletamine hydrochloride and zolazepam hydrochloride for injection.

    Code of Federal Regulations, 2013 CFR

    2013-04-01

    ... 21 Food and Drugs 6 2013-04-01 2013-04-01 false Tiletamine hydrochloride and zolazepam hydrochloride for injection. 522.2470 Section 522.2470 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT... analgesia. (2) Amount. Expressed as milligrams of the drug combination: (i) In healthy dogs: An...

  13. 21 CFR 522.2470 - Tiletamine hydrochloride and zolazepam hydrochloride for injection.

    Code of Federal Regulations, 2010 CFR

    2010-04-01

    ... 21 Food and Drugs 6 2010-04-01 2010-04-01 false Tiletamine hydrochloride and zolazepam hydrochloride for injection. 522.2470 Section 522.2470 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 §...

  14. Synthesis and evaluation of antioxidant activity of new quinoline-2-carbaldehyde hydrazone derivatives: bioisosteric melatonin analogues.

    PubMed

    Puskullu, M Orhan; Shirinzadeh, Hanif; Nenni, Merve; Gurer-Orhan, Hande; Suzen, Sibel

    2016-02-01

    Overproduction of reactive oxygen species results in oxidative stress that can cause fatal damage to vital cell structures. It is known that the use of antioxidants could be beneficial in the prevention or delay of numerous diseases associated with oxidative stress. Melatonin (MLT) is known as a powerful free-radical scavenger and antioxidant. It was found that indole ring of MLT can be employed by bioisosteric replacement by other aromatic rings. Quinoline derivatives constitute an important class of compounds for new drug development. Owing to quinoline and hydrazones appealing physiological properties and are mostly found in numerous biologically active compounds a series of quinoline-2-carbaldehyde hydrazone derivatives were synthesized as bioisosteric analogues of MLT, characterized and in vitro antioxidant activity was investigated by evaluating their reducing effect against oxidation of a redox-sensitive fluorescent probe. Cytotoxicity potential of all compounds was investigated both by lactate dehydrogenase leakage assay and by MTT assay. PMID:25942363

  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. Novel hydrazone derivatives containing pyridine amide moiety: Design, synthesis, and insecticidal activity.

    PubMed

    Yang, Zai-Bo; Hu, De-Yu; Zeng, Song; Song, Bao-An

    2016-02-15

    A series of novel hydrazone derivatives containing pyridine amide moiety were designed, synthesized, and evaluated for their insecticidal activity. Bioassays indicated that some of the target compounds exhibited good insecticidal activities against Nilaparvata lugens (N. lugens), Plutella xylostella (P. xylostella), Mythimna separata (M. separata), Helicoverpa armigera (H. armigera), Pyrausta nubilalis (P. nubilalis), and Culex pipiens pallens (C. pipiens pallens). In particular, compound 5j revealed excellent insecticidal activity against C. pipiens pallens, with the 50% lethal concentration (LC50) and the 95% lethal concentration (LC95) values of 2.44 and 5.76mg/L, respectively, which were similar to those of chlorpyrifos (3.26 and 6.98mg/L, respectively), tebufenozide (1.22 and 2.49mg/L, respectively), and RH-5849 (2.61 and 6.37mg/L, respectively). These results indicated that hydrazone derivatives containing pyridine amide moiety could be developed as novel and promising insecticides. PMID:26832221

  17. 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.

  18. 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

  19. Synthesis of an enlarged library of dynamic DNA activators with oxime, disulfide and hydrazone bridges.

    PubMed

    Montenegro, Javier; Bang, Eun-Kyoung; Sakai, Naomi; Matile, Stefan

    2012-08-13

    Dynamic amphiphiles have a "bridge" between their charged head and their hydrophobic tails. The presence of dynamic covalent bonds is of interest for differential and biosensing applications as well as for rapid access to the libraries needed to screen for gene delivery or cellular uptake of siRNA. However, efforts to develop libraries have so far concentrated on hydrazone bridges to monocationic heads. Here, we report synthesis efforts to enlarge this focused library with oxime and disulfide bridges and dynamic amphiphiles with more than one positive charge. Evaluation in fluorogenic vesicles reveals best activation of DNA as ion transporters by dynamic amphiphiles with dendritic scaffolds, doubly charged heads and four tails. Moreover, oximes, contrary to hydrazones, remain active under acidic conditions. Linear elongation of dendritic head-groups seems to cause increasing detergent effects and should therefore be avoided. PMID:22589231

  20. Hydrazone self-crosslinking of multiphase elastin-like block copolymer networks.

    PubMed

    Krishna, Urlam Murali; Martinez, Adam W; Caves, Jeffrey M; Chaikof, Elliot L

    2012-03-01

    Biosynthetic strategies for the production of recombinant elastin-like protein (ELP) triblock copolymers have resulted in elastomeric protein hydrogels, formed through rapid physical crosslinking upon warming of concentrated solutions. However, the strength of physically crosslinked networks can be limited, and options for non-toxic chemical crosslinking of these networks are not optimal. In this report, we modify two recombinant elastin-like proteins with aldehyde and hydrazide functionalities. When combined, these modified recombinant proteins self-crosslink through hydrazone bonding without requiring initiators or producing by-products. Crosslinked materials are evaluated for water content and swelling upon hydration, and subject to tensile and compressive mechanical tests. Hydrazone crosslinking is a viable method for increasing the mechanical strength of elastin-like protein polymers, in a manner that is likely to lend itself to the biocompatible in situ formation of chemically and physically crosslinked ELP hydrogels. PMID:22154858

  1. Caffeine-hydrazones as anticancer agents with pronounced selectivity toward T-lymphoblastic leukaemia cells.

    PubMed

    Kaplánek, Robert; Jakubek, Milan; Rak, Jakub; Kejík, Zdeněk; Havlík, Martin; Dolenský, Bohumil; Frydrych, Ivo; Hajdúch, Marián; Kolář, Milan; Bogdanová, Kateřina; Králová, Jarmila; Džubák, Petr; Král, Vladimír

    2015-06-01

    We report design and synthesis of set of novel anticancer agents based on caffeine-hydrazones bearing 2-hydroxyaryl- or 2-N-heteroaryl moiety. Anticancer activity evaluation using seven cancer cell lines and two non-malignant cell lines demonstrated that several derivatives display significant anticancer activity and great selectivity index toward T-lymphoblastic leukaemia cells. In general, hydrazones bearing 2-N-heteroaryl moiety are more active and selective than those with 2-hydroxyaryl moiety. Tested compounds exhibit dose-dependent inhibition of both RNA and DNA synthesis, with some exceptions. Antimicrobial activities were tested on set of twelve bacterial and yeast strains, however prepared compounds were not active, suggesting for a molecular target specific for eukaryotic cells. PMID:25912310

  2. The anion recognition properties of a novel hydrazone based on colorimetric and potentiometric studies.

    PubMed

    Singhal, Divya; Gupta, Neha; Singh, Ashok Kumar

    2016-01-01

    A novel hydrazone, 1,3-bis (2-formylphenoxy) propane bis (2,4-dinitrophenyl hydrazine) (S) has been synthesized and characterized by the NMR, IR, CHNS, UV-Vis, Raman, TEM and XPS analysis. Upon the addition of monohydrogen phosphate (MHP) ion, sudden color change from light yellow to dark violet has occurred. The binding constant of S-MHP was determined by Hill plot. Hydrazone also showed potential response with MHP ion. A number of polymeric membrane electrodes (PME) and coated graphite electrode (CGE) were also fabricated and found that the CGE has revealed better results in comparison to PME in terms of the detection limit of 7.58 × 10(-9) mol L(-1) and Nernstian response. PMID:26478343

  3. Synthesis and characterization of platinum-sterol hydrazone complexes with biological activity against Leishmania (L.) mexicana.

    PubMed

    Visbal, Gonzalo; Marchán, Edgar; Maldonado, Alexis; Simoni, Zulay; Navarro, Maribel

    2008-03-01

    Leishmaniasis is a parasitic zoonosis caused by protozoans of the genus Leishmania transmitted by insects known as phlebotomines, which are found in wild or urban environments. The disease occurs in tropical and sub-tropical areas, mainly in Asia, Europe, Africa and the Americas. At present, there is no effective treatment for this disease. In the search for new rational chemotherapeutic alternatives, two novel trans [Pt(Hpy1)(2)(Cl)(2)] (1) and trans [Pt(Hpy2)(2) (Cl)(2)] (2) complexes were synthesized by the reaction of K(2)PtCl(4) with sterol hydrazone ligands 20-hydrazone-pyridin-2-yl-5alpha-pregnan-3beta-ol (Hpy1) and 22-hydrazone-pyridin-2-yl-chol-5-ene-3beta-ol (Hpy2). These organic compounds are specific inhibitors of sterol methyl transferase (SMT). The new platinum complexes were characterized by a combination of ESI-MS (electrospray ionization-mass spectroscopy), UV-vis, infrared and NMR spectroscopies; elemental analysis and molar conductivity. Promastigotes of Leishmania (L.) mexicana were treated for 48 h with 10 microM of the sterol hydrazones Hpy1 or Hpy2 alone or coordinated to Pt. Hpy1 produced higher leishmanistatic activity than Hpy2 (39% growth inhibition vs. 16%), which significatively increased (71%, p<0.001) when the complex trans-[Pt(Hpy1)(2)(Cl)(2)] was used. This complex represents a new chemotherapeutic alternative to be evaluated in depth in experimental models of leishmaniasis. PMID:18164763

  4. A hydrazone ligation strategy to assemble multifunctional viral nanoparticles for cell imaging and tumor targeting

    PubMed Central

    Brunel, Florence M.; Lewis, John D.; Destito, Giuseppe; Steinmetz, Nicole F.; Manchester, Marianne; Stuhlmann, Heidi; Dawson, Philip E.

    2013-01-01

    Multivalent nanoparticle platforms are attractive for biomedical applications because of their improved target specificity, sensitivity and solubility. However, their controlled assembly remains a considerable challenge. An efficient hydrazone ligation chemistry was applied to the assembly of Cowpea mosaic virus (CPMV) nanoparticles with individually tunable levels of a VEGFR-1 ligand and a fluorescent PEGylated peptide. The nanoparticles recognized VEGFR-1 on endothelial cell lines and VEGFR1-expressing tumor xenografts in mice, validating targeted CPMV as a nanoparticle platform in vivo. PMID:20163184

  5. 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.

  6. 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

  7. An Optical Test Strip for the Detection of Benzoic Acid in Food

    PubMed Central

    Hamzah, Hairul Hisham; Yusof, Nor Azah; Salleh, Abu Bakar; Bakar, Fatimah Abu

    2011-01-01

    Fabrication of a test strip for detection of benzoic acid was successfully implemented by immobilizing tyrosinase, phenol and 3-methyl-2-benzothiazolinone hydrazone (MBTH) onto filter paper using polystyrene as polymeric support. The sensing scheme was based on the decreasing intensity of the maroon colour of the test strip when introduced into benzoic acid solution. The test strip was characterized using optical fiber reflectance and has maximum reflectance at 375 nm. It has shown a highly reproducible measurement of benzoic acid with a calculated RSD of 0.47% (n = 10). The detection was optimized at pH 7. A linear response of the biosensor was obtained in 100 to 700 ppm of benzoic acid with a detection limit (LOD) of 73.6 ppm. At 1:1 ratio of benzoic acid to interfering substances, the main interfering substance is boric acid. The kinetic analyses show that, the inhibition of benzoic is competitive inhibitor and the inhibition constant (Ki) is 52.9 ppm. The activity of immobilized tyrosinase, phenol, and MBTH in the test strip was fairly sustained during 20 days when stored at 3 °C. The developed test strip was used for detection of benzoic acid in food samples and was observed to have comparable results to the HPLC method, hence the developed test strip can be used as an alternative to HPLC in detecting benzoic acid in food products. PMID:22164018

  8. An Optical Biosensor based on Immobilization of Laccase and MBTH in Stacked Films for the Detection of Catechol

    PubMed Central

    Abdullah, Jaafar; Ahmad, Musa; Heng, Lee Yook; Karuppiah, Nadarajah; Sidek, Hamidah

    2007-01-01

    The fabrication of an optical biosensor by using stacked films where 3-methyl-2-benzothiazolinone hydrazone (MBTH) was immobilized in a hybrid nafion/sol-gel silicate film and laccase in a chitosan film for the detection of phenolic compounds was described. Quinone and/or phenoxy radical product from the enzymatic oxidation of phenolic compounds was allowed to couple with MBTH to form a colored azo-dye product for spectrophometric detection. The biosensor demonstrated a linear response to catechol concentration range of 0.5-8.0 mM with detection limit of 0.33 mM and response time of 10 min. The reproducibility of the fabricated biosensor was good with RSD value of 5.3 % (n = 8) and stable for at least 2 months. The use of the hybrid materials of nafion/sol-gel silicate to immobilize laccase has altered the selectivity of the enzyme to various phenolic compounds such as catechol, guaicol, o-cresol and m-cresol when compared to the non-immobilized enzyme. When immobilized in this hybrid film, the biosensor response only to catechol and not other phenolic compounds investigated. Immobilization in this hybrid material has enable the biosensor to be more selective to catechol compared with the non-immobilized enzyme. This shows that by a careful selection of different immobilization matrices, the selectivity of an enzyme can be modified to yield a biosensor with good selectivity towards certain targeted analytes.

  9. Stacked films immobilization of MBTH in nafion/sol-gel silicate and horseradish peroxidase in chitosan for the determination of phenolic compounds.

    PubMed

    Abdullah, Jaafar; Ahmad, Musa; Heng, Lee Yook; Karuppiah, Nadarajah; Sidek, Hamidah

    2006-11-01

    The stacked-film immobilization of 3-methyl-2-benzothiazolinone hydrazone (MBTH) in hybrid nafion/sol-gel silicate film and horseradish peroxidase (HRP) in chitosan, performed in order to allow the determination of phenolic compounds, was investigated via an optical method. The stacked films were deposited onto a microscope glass slide by a spin-coating technique. The quinone or free radical product formed by the enzymatic reactions of phenolic compounds interacts with MBTH to form azo-dye products, which can be measured spectrophotometrically at a wavelength of 500 nm. The color intensity of the product was found to increase in proportion to the phenolic concentration after 5 min of exposure. The response of the biosensor was linear over concentration ranges of 0.025-0.500, 0.010-0.070 and 0.050-0.300 mM for guaiacol, resorcinol and o-cresol, respectively, and gave detection limits of 0.010, 0.005 and 0.012 mM. The sensor exhibited good sensitivity and stability for at least two months. PMID:17031625

  10. Flow injection determination of hydrogen peroxide using catalytic effect of cobalt(II) ion on a dye formation reaction.

    PubMed

    Kurihara, Makoto; Muramatsu, Miyuki; Yamada, Mari; Kitamura, Naoya

    2012-07-15

    A novel flow injection photometric method was developed for the determination of hydrogen peroxide in rainwater. This method is based on a cobalt(II)-catalyzed oxidative coupling of 3-methyl-2-benzothiazolinone hydrazone (MBTH) with N-ethyl-N-(2-hydroxy-3-sulfopropyl)-3,5-dimethoxyaniline (DAOS) as a modified Trinder's reagent to produce intensely colored dye (λ(max)=530nm) in the presence of hydrogen peroxide at pH 8.4. In this method, 1,2-dihydroxy-3,5-benzenedisulfonic acid (Tiron) acted as an activator for the cobalt(II)-catalyzed reaction and effectively increased the peak height for hydrogen peroxide. The linear calibration graphs were obtained in the hydrogen peroxide concentration range 5×10(-8) to 2.2×10(-6)mol dm(-3) at a sampling rate of 20h(-1). The relative standard deviations for ten determinations of 2.2×10(-6) and 2×10(-7)mol dm(-3) hydrogen peroxide were 1.1% and 3.7%, respectively. The proposed method was successfully applied to the determination of hydrogen peroxide in rainwater samples and the analytical results agreed fairly well with the results obtained by different two reference methods; peroxidase method and hydrogen peroxide electrode method. PMID:22817947

  11. 21 CFR 522.723 - Diprenorphine hydrochloride injection.

    Code of Federal Regulations, 2012 CFR

    2012-04-01

    ... 21 Food and Drugs 6 2012-04-01 2012-04-01 false Diprenorphine hydrochloride injection. 522.723... § 522.723 Diprenorphine hydrochloride injection. (a) Chemical name. N-(Cyclopropyl-methyl)-6,7,8,14...) Specifications. Each milliliter of diprenorphine hydrochloride injection, veterinary, contains 2 mg...

  12. 21 CFR 522.1462 - Naloxone hydrochloride injection.

    Code of Federal Regulations, 2012 CFR

    2012-04-01

    ... 21 Food and Drugs 6 2012-04-01 2012-04-01 false Naloxone hydrochloride injection. 522.1462 Section... § 522.1462 Naloxone hydrochloride injection. (a) Specifications. Naloxone hydrochloride injection is an... antagonist in dogs. (2) It is administered by intravenous, intramuscular, or subcutaneous injection at...

  13. 21 CFR 522.1462 - Naloxone hydrochloride injection.

    Code of Federal Regulations, 2011 CFR

    2011-04-01

    ... 21 Food and Drugs 6 2011-04-01 2011-04-01 false Naloxone hydrochloride injection. 522.1462 Section... § 522.1462 Naloxone hydrochloride injection. (a) Specifications. Naloxone hydrochloride injection is an... antagonist in dogs. (2) It is administered by intravenous, intramuscular, or subcutaneous injection at...

  14. 21 CFR 522.723 - Diprenorphine hydrochloride injection.

    Code of Federal Regulations, 2013 CFR

    2013-04-01

    ... 21 Food and Drugs 6 2013-04-01 2013-04-01 false Diprenorphine hydrochloride injection. 522.723... § 522.723 Diprenorphine hydrochloride injection. (a) Chemical name. N-(Cyclopropyl-methyl)-6,7,8,14...) Specifications. Each milliliter of diprenorphine hydrochloride injection, veterinary, contains 2 mg...

  15. 40 CFR 721.10687 - Fatty acid amide hydrochlorides (generic).

    Code of Federal Regulations, 2014 CFR

    2014-07-01

    ... 40 Protection of Environment 31 2014-07-01 2014-07-01 false Fatty acid amide hydrochlorides... Specific Chemical Substances 721.10687 Fatty acid amide hydrochlorides (generic). (a) Chemical substance... fatty acid amide hydrochlorides (PMNs P-13-201, P-13-203, P-13-204, P-13-205, P-13-206, P-13-207,...

  16. Structural studies and investigation on the activity of imidazole-derived thiosemicarbazones and hydrazones against crop-related fungi.

    PubMed

    Reis, Débora C; Despaigne, Angel A Recio; Da Silva, Jeferson G; Silva, Nayane F; Vilela, Camila F; Mendes, Isolda C; Takahashi, Jacqueline A; Beraldo, Heloisa

    2013-01-01

    New imidazole derived thiosemicarbazones and hydrazones were prepared by condensation of 4(5)-imidazole carboxaldehyde, 4-(1H-imidazole-1-yl)benzaldehyde and 4-(1H-imidazole-1-yl)acetophenone with a thiosemicarbazide or hydrazide. All compounds were characterized by quantitative elemental analysis, IR and NMR techniques. Eight structures were determined by single crystal X-ray diffraction. The antifungal activities of the compounds were evaluated. None of the compounds exhibited significant activity against Aspergillus flavus and Candida albicans, while 4(5)-imidazolecarboxaldehyde thiosemicarbazone (ImT) and 4-(1H-imidazole-1-yl)benzaldehyde thiosemicabazone (4ImBzT) were highly and selectively active against Cladosporium cladosporioides. 4(5)-Imidazolecarboxaldehyde benzoyl hydrazone (4(5)ImPh), 4(5)-imidazolecarboxaldehyde-para-chlorobenzoyl hydrazone (4(5)ImpClPh), 4(5)-imidazolecarboxaldehyde-para-nitrobenzoyl hydrazone (4(5)ImpNO2Ph), 4-(imidazole-1-yl)acetophenone-para-chloro-benzoyl hydrazone (4ImAcpClPh) and 4-(imidazole-1-yl)acetophenone-para-nitro-benzoylhydrazone (4ImAcpNO2Ph) were highly active against Candida glabrata. 4(5)ImpClPh and 4(5)ImpNO2Ph were very effective against C. cladosporioides. In many cases, activity was superior to that of the reference compound nystatin. PMID:24129274

  17. Simultaneous HPLC analysis of pseudophedrine hydrochloride, codeine phosphate, and triprolidine hydrochloride in liquid dosage forms.

    PubMed

    Manassra, Adnan; Khamis, Mustafa; El-Dakiky, Magdy; Abdel-Qader, Zuhair; Al-Rimawi, Fuad

    2010-03-11

    An HPLC method using UV detection is proposed for the simultaneous determination of pseudophedrine hydrochloride, codeine phosphate, and triprolidine hydrochloride in liquid formulation. C18 column (250mmx4.0mm) is used as the stationary phase with a mixture of methanol:acetate buffer:acetonitrile (85:5:10, v/v) as the mobile phase. The factors affecting column separation of the analytes were studied. The calibration graphs exhibited a linear concentration range of 0.06-1.0mg/ml for pseudophedrine hydrochloride, 0.02-1.0mg/ml for codeine phosphate, and 0.0025-1.0mg/ml for triprolidine hydrochloride for a sample size of 5microl with correlation coefficients of better than 0.999 for all active ingredients studied. The results demonstrate that this method is reliable, reproducible and suitable for routine use with analysis time of less than 4min. PMID:19954915

  18. Chromatographic Determination of Aminoacridine Hydrochloride, Lidocaine Hydrochloride and Lidocaine Toxic Impurity in Oral Gel.

    PubMed

    Bebawy, Lories I; Elghobashy, Mohamed R; Abbas, Samah S; Shokry, Rafeek F

    2016-04-01

    Two sensitive and selective analytical methods were developed for simultaneous determination of aminoacridine hydrochloride and lidocaine hydrochloride in bulk powder and pharmaceutical formulation. Method A was based on HPLC separation of the cited drugs with determination of the toxic lidocaine-related impurity 2,6-dimethylaniline. The separation was achieved using reversed-phase column C18, 250 × 4.6 mm, 5 µm particle size and mobile phase consisting of 0.05 M disodium hydrogen phosphate dihydrate (pH 6.0 ± 0.2 adjusted with phosphoric acid) and acetonitrile (55 : 45, v/v). Quantitation was achieved with UV detection at 240 nm. Linear calibration curve was in the range of 1.00-10.00, 13.20-132.00 and 1.32-13.20 µg mL(-1) for aminoacridine hydrochloride, lidocaine hydrochloride and 2,6-dimethylaniline, respectively. Method B was based on TLC separation of the cited drugs followed by densitometric measurement at 365 nm on the fluorescent mode for aminoacridine hydrochloride and 220 nm on the absorption mode for lidocaine hydrochloride. The separation was carried out using ethyl acetate-methanol-acetic acid (65 : 30 : 5 by volume) as a developing system. The calibration curve was in the range of 25.00-250.00 ng spot(-1) and 0.99-9.90 µg spot(-1) for aminoacridine hydrochloride and lidocaine hydrochloride, respectively. The results obtained were statistically analyzed and compared with those obtained by applying the manufacturer's method. PMID:26671412

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

    PubMed Central

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

    2008-01-01

    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-C18 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

  20. 21 CFR 522.234 - Butamisole hydrochloride.

    Code of Federal Regulations, 2012 CFR

    2012-04-01

    ... subcutaneously at the rate of 0.1 milliliter per pound of body weight. In problem cases, retreatment for... 21 Food and Drugs 6 2012-04-01 2012-04-01 false Butamisole hydrochloride. 522.234 Section 522.234 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED)...

  1. 21 CFR 522.234 - Butamisole hydrochloride.

    Code of Federal Regulations, 2011 CFR

    2011-04-01

    ... subcutaneously at the rate of 0.1 milliliter per pound of body weight. In problem cases, retreatment for... 21 Food and Drugs 6 2011-04-01 2011-04-01 false Butamisole hydrochloride. 522.234 Section 522.234 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED)...

  2. 21 CFR 522.234 - Butamisole hydrochloride.

    Code of Federal Regulations, 2013 CFR

    2013-04-01

    ... subcutaneously at the rate of 0.1 milliliter per pound of body weight. In problem cases, retreatment for... 21 Food and Drugs 6 2013-04-01 2013-04-01 false Butamisole hydrochloride. 522.234 Section 522.234 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED)...

  3. 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,...

  4. 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,...

  5. 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...

  6. 21 CFR 582.5676 - Pyridoxine hydrochloride.

    Code of Federal Regulations, 2010 CFR

    2010-04-01

    ... 21 Food and Drugs 6 2010-04-01 2010-04-01 false Pyridoxine hydrochloride. 582.5676 Section 582.5676 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL DRUGS, FEEDS, AND RELATED PRODUCTS SUBSTANCES GENERALLY RECOGNIZED AS SAFE Nutrients and/or Dietary Supplements 1 582.5676...

  7. 21 CFR 522.234 - Butamisole hydrochloride.

    Code of Federal Regulations, 2010 CFR

    2010-04-01

    ... 21 Food and Drugs 6 2010-04-01 2010-04-01 false Butamisole hydrochloride. 522.234 Section 522.234 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 §...

  8. 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 DRUGS, FEEDS, AND RELATED PRODUCTS TOLERANCES FOR RESIDUES OF NEW ANIMAL DRUGS IN FOOD...

  9. 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...

  10. Unexpected Formation of Highly Functionalized Dihydropyrans via Addition-Cyclization Reactions Between Dimethyl Oxoglutaconate and α,β-Unsaturated Hydrazones.

    PubMed

    Mullins, Jason E; Etoga, Jean-Louis G; Gajewski, Mariusz; Degraw, Joseph I; Thompson, Charles M

    2009-05-20

    The condensation between dienophiles and α,β-unsaturated hydrazone azadienes was previously reported to afford piperidines. During an attempt to adapt this reaction to the preparation of piperidine-based conformationally-restricted analogs of glutamate, it was discovered that the electrophile, dimethyl oxoglutaconate (DOG) led to highly substituted dihydropyrans in 20-50% yield. The unexpected pyran product likely results from an initial 1,4-addition of the hydrazone to the oxoglutaconate followed by intramolecular cyclization of the resultant enolate oxygen to the α,β-unsaturated iminium ion. Further manipulations afford substituted tetrahydropyran 6-methamino-2,4-dicarboxylic acids. PMID:20161237

  11. Unexpected Formation of Highly Functionalized Dihydropyrans via Addition-Cyclization Reactions Between Dimethyl Oxoglutaconate and α,β-Unsaturated Hydrazones

    PubMed Central

    Mullins, Jason E.; Etoga, Jean-Louis G.; Gajewski, Mariusz; DeGraw, Joseph I.; Thompson, Charles M.

    2009-01-01

    The condensation between dienophiles and α,β-unsaturated hydrazone azadienes was previously reported to afford piperidines. During an attempt to adapt this reaction to the preparation of piperidine-based conformationally-restricted analogs of glutamate, it was discovered that the electrophile, dimethyl oxoglutaconate (DOG) led to highly substituted dihydropyrans in 20–50% yield. The unexpected pyran product likely results from an initial 1,4-addition of the hydrazone to the oxoglutaconate followed by intramolecular cyclization of the resultant enolate oxygen to the α,β-unsaturated iminium ion. Further manipulations afford substituted tetrahydropyran 6-methamino-2,4-dicarboxylic acids. PMID:20161237

  12. 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

  13. 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

  14. Synthesis, antifungal activities and qualitative structure activity relationship of carabrone hydrazone derivatives as potential antifungal agents.

    PubMed

    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

  15. 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

  16. Treatment of allergic conjunctivitis with olopatadine hydrochloride eye drops.

    PubMed

    Uchio, Eiichi

    2008-09-01

    Olopatadine hydrochloride exerts a wide range of pharmacological actions such as histamine H(1) receptor antagonist action, chemical mediator suppressive action, and eosinophil infiltration suppressive action. Olopatadine hydrochloride 0.1% ophthalmic solution (Patanol((R))) was introduced to the market in Japan in October 2006. In a conjunctival allergen challenge (CAC) test, olopatadine hydrochloride 0.1% ophthalmic solution significantly suppressed ocular itching and hyperemia compared with levocabastine hydrochloride 0.05% ophthalmic solution, and the number of patients who complained of ocular discomfort was lower in the olopatadine group than in the levocabastine group. Conjunctival cell membrane disruption was observed in vitro in the ketotifen fumarate group, epinastine hydrochloride group, and azelastine hydrochloride group, but not in the olopatadine hydrochloride 0.1% ophthalmic solution group, which may potentially explain the lower discomfort felt by patients on instillation. Many other studies in humans have revealed the superiority of olopatadine 0.1% hydrochloride eye drops to several other anti-allergic eye drops. Overseas, olopatadine hydrochloride 0.2% ophthalmic solution for a once-daily regimen has been marketed under the brand name of Pataday((R)). It is expected that olopatadine hydrochloride ophthalmic solutions may be used in patients with a more severe spectrum of allergic conjunctival diseases, such as vernal keratoconjunctivitis or atopic keratoconjunctivitis, in the near future. PMID:19668750

  17. Treatment of allergic conjunctivitis with olopatadine hydrochloride eye drops

    PubMed Central

    Uchio, Eiichi

    2008-01-01

    Olopatadine hydrochloride exerts a wide range of pharmacological actions such as histamine H1 receptor antagonist action, chemical mediator suppressive action, and eosinophil infiltration suppressive action. Olopatadine hydrochloride 0.1% ophthalmic solution (Patanol®) was introduced to the market in Japan in October 2006. In a conjunctival allergen challenge (CAC) test, olopatadine hydrochloride 0.1% ophthalmic solution significantly suppressed ocular itching and hyperemia compared with levocabastine hydrochloride 0.05% ophthalmic solution, and the number of patients who complained of ocular discomfort was lower in the olopatadine group than in the levocabastine group. Conjunctival cell membrane disruption was observed in vitro in the ketotifen fumarate group, epinastine hydrochloride group, and azelastine hydrochloride group, but not in the olopatadine hydrochloride 0.1% ophthalmic solution group, which may potentially explain the lower discomfort felt by patients on instillation. Many other studies in humans have revealed the superiority of olopatadine 0.1% hydrochloride eye drops to several other anti-allergic eye drops. Overseas, olopatadine hydrochloride 0.2% ophthalmic solution for a once-daily regimen has been marketed under the brand name of Pataday®. It is expected that olopatadine hydrochloride ophthalmic solutions may be used in patients with a more severe spectrum of allergic conjunctival diseases, such as vernal keratoconjunctivitis or atopic keratoconjunctivitis, in the near future. PMID:19668750

  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. 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

  20. 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

  1. 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.

  2. 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.

  3. 40 CFR 721.10682 - Fatty acid amide hydrochlorides (generic).

    Code of Federal Regulations, 2014 CFR

    2014-07-01

    ... 40 Protection of Environment 31 2014-07-01 2014-07-01 false Fatty acid amide hydrochlorides... Specific Chemical Substances 721.10682 Fatty acid amide hydrochlorides (generic). (a) Chemical substances... fatty acid amide hydrochlorides (PMNs P-13-63, P-13-64, P-13-65, P-13-69, P-13-70, P-13-71, P-13-72,...

  4. Alteration in Bacterial Morphology by Optochin and Quinine Hydrochlorides1

    PubMed Central

    Kreger, Arnold S.; Swartzendruber, D. C.; Olsen, R. H.

    1969-01-01

    Incubation of washed bacterial and ribosomal suspensions with optochin or quinine hydrochloride caused an increase in the turbidity of the suspensions and the appearance of electron-dense cytoplasmic aggregates in the treated cells. These effects were more pronounced with optochin hydrochloride than with quinine hydrochloride, and they did not correlate with the relative sensitivities of different bacteria to growth inhibition by optochin or quinine. Images PMID:4974397

  5. Nalfurafine hydrochloride to treat pruritus: a review

    PubMed Central

    Inui, Shigeki

    2015-01-01

    Uremic pruritus has a great negative influence on quality of life in hemodialysis (HD) patients and, importantly, negatively affects mortality risk. Recently, nalfurafine hydrochloride, an opioid κ-selective agonist, has been officially approved for resistant pruritus in HD patients on the basis of a well-evidenced clinical trial in Japan. From clinical observation, it has been suggested that the upper neuron system plays a role in its pathogenesis. According to previous experimental results, using mice injected with opioids, dynorphin suppresses itch through binding κ-opioid receptors, suggesting that κ-opioid opioid receptor agonists act as potential therapeutic reagents for pruritus in HD patients. In Japan, a large-scale placebo-controlled study was performed to examine the efficacy and safety of oral nalfurafine hydrochloride for intractable pruritus in 337 HD patients. Two daily doses of 2.5 or 5 μg nalfurafine or placebo were orally administered for 2 weeks, and clinical responses were analyzed. The results showed that the mean decrease in the visual analog scale for pruritus from baseline was 22 mm in the 5 μg nalfurafine hydrochloride group (n=114) and 23 mm in the 2.5 μg group (n=112). These reductions were statistically significant compared with 13 mm, which is the mean decrease of visual analog scale in the placebo group (n=111), demonstrating that nalfurafine is an effective and safe drug for uremic pruritus in HD patients. Moreover, another open-label trial (n=145) examining the long-term effect of 5 μg oral nalfurafine revealed the maintenance of the antipruritic effect of nalfurafine for 52 weeks. In addition, on the basis of recent data showing κ-opioid receptor expression in the epidermis of atopic dermatitis and psoriasis, nalfurafine hydrochloride also can be potentially used for these two skin diseases. PMID:26005355

  6. [Antiseptics on the base of Octenidine Hydrochloride].

    PubMed

    Malinovskií, N N; Reshetnikov, E A; Rubashnaia, I E; Mal'nikova, G N; Mitiukov, A P

    1997-01-01

    Comparative evaluation of laboratory and clinical investigation of antiseptic preparations on the base of octenidin-hydrochloride and bigluconate chlorhexidine in 537 patients was carried out. Statistically valid decrease in dissemination through the operation field and surgical wound after application of octenidin containing solutions was determined. It was established as well that these preparations were more effective fools of protection of the operation wound from its microbial contamination in comparison with antiseptic solutions widely spread to date in surgical practice. PMID:9480391

  7. 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

  8. 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

  9. Synthesis, spectroscopic, thermal and antifungal studies on lanthanum(III) and praseodymium(III) derivatives of 1,1-diacetylferrocenyl hydrazones

    NASA Astrophysics Data System (ADS)

    Sengupta, S. K.; Pandey, O. P.; Rai, Anita; Sinha, A.

    2006-09-01

    A series of new coordination complexes of La(III) and Pr(III) with hydrazones, derived from 1,1-diacetylferrocene and different aromatic acid hydrazides have been synthesized and characterized by elemental analyses, electrical conductance, magnetic moment, IR, 1H NMR, UV-vis spectra and molar conductance. The thermal behaviour of the complexes under non-isothermal condition was investigated by TG and DTG techniques. The antifungal activity of hydrazones and their corresponding complexes were also investigated.

  10. 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 CN or double CN 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 (0.05-2μg/mL). Five compounds demonstrated appreciable activity against the INH-resistant M. tuberculosis CN-40 clinical isolate (MICs: 2-5μg/mL), providing justification for further in vivo studies. PMID:26725953

  11. Benzaldehyde, 2-hydroxybenzoyl hydrazone derivatives as inhibitors of the corrosion of aluminium in hydrochloric acid.

    PubMed

    Fouda, A S; Gouda, M M; El-Rahman, S I

    2000-05-01

    The effect of benzaldehyde, 2-hydroxybenzoyl hydrazone derivatives on the corrosion of aluminium in hydrochloric acid has been investigated using thermometric and polarization techniques. The inhibitive efficiency ranking of these compounds from both techniques was found to be: 2>3>1>4. The inhibitors acted as mixed-type inhibitors but the cathode is more polarized. The relative inhibitive efficiency of these compounds has been explained on the basis of structure of the inhibitors and their mode of interaction at the surface. Results show that these additives are adsorbed on an aluminium surface according to the Langmuir isotherm. Polarization measurements indicated that the rate of corrosion of aluminium rapidly increases with temperature over the range 30-55 degrees C both in the absence and in the presence of inhibitors. Some thermodynamic data of the adsorption process are calculated and discussed. PMID:10823698

  12. Verification of the dispersive charge transport in a hydrazone:polycarbonate molecularly doped polymer

    NASA Astrophysics Data System (ADS)

    Tyutnev, Andrey P.; Saenko, Vladimir S.; Pozhidaev, Evgenii D.; Kolesnikov, Vladislav A.

    2009-03-01

    We report results of specially planned experiments intended to verify the dispersive character of the charge carrier transport in polycarbonate molecularly doped with hydrazone at 30 wt% loading, using for this purpose samples specifically featuring a well-defined plateau on a linear-linear plot. For this purpose we propose a new variant of the time-of-flight technique which allows easy changing of the generation zone width from about 0.5 µm (surface excitation) through intermediate values to full sample thickness (bulk excitation). To achieve this, we use electron pulses of 3-50 keV energy rather than traditional light pulses provided by lasers. Experimental results corroborated by numerical calculations uniquely prove that carrier transport in this molecularly doped polymer is dispersive, with the dispersion parameter equal to 0.75. Nevertheless, the mobility field dependence follows the famous Poole-Frenkel law.

  13. Synthesis and antitubercular activity of a series of hydrazone and nitrovinyl analogs derived from heterocyclic aldehydes.

    PubMed

    Sonar, Vijayakumar N; Crooks, Peter A

    2009-02-01

    A series of hydrazone and 3-nitrovinyl analogs of indole-3-carboxaldehydes and related compounds were synthesized and screened for antitubercular activity against Mycobacterium tuberculosis H37R(V) in BACTEC 12B medium using the Microplate Alamar Blue Assay (MABA). Several compounds showed inhibitory activity against M. tuberculosis in primary screening assays at a concentration of 6.25 microg/mL; subsequent dose-response studies indicated that the most active compounds, 3d, 3e & 8b, had IC(50) values of 5.96, 5.4 & 1.6 microg/mL, respectively. These compounds represent potential leads for the further development of novel antitubercular agents. PMID:18629678

  14. Synthesis, activity evaluation, and docking analysis of barbituric acid aryl hydrazone derivatives as RSK2 inhibitors.

    PubMed

    Xue, Mengzhu; Xu, Minghao; Lu, Weiqiang; Huang, Jin; Li, Honglin; Xu, Yufang; Liu, Xiaofeng; Zhao, Zhenjiang

    2013-08-01

    The 90 kDa ribosomal S6 kinases (RSKs), especially RSK2, have attracted attention for the development of new anticancer agents. Through structural optimization of the hit compound 1 from our previous study, a series of barbituric acid aryl hydrazone analogues were designed and synthesized as potential RSK2 inhibitors. The most potent one, compound 9, showed a higher activity against RSK2 with an IC50 value of 1.95 μM. To analyze and elucidate their structure-activity relationship, the homology model of RSK2 N-terminal kinase domain was built and molecular docking simulations were performed, which provide helpful clues to design new inhibitors with desired activities. PMID:22545939

  15. Methyl and ethyl ketone analogs of salicylaldehyde isonicotinoyl hydrazone: novel iron chelators with selective antiproliferative action.

    PubMed

    Macková, Eliška; Hrušková, Kateřina; Bendová, Petra; Vávrová, Anna; Jansová, Hana; Hašková, Pavlína; Kovaříková, Petra; Vávrová, Kateřina; Simůnek, Tomáš

    2012-05-30

    Salicylaldehyde isonicotinoyl hydrazone (SIH) is a lipophilic, orally-active tridentate iron chelator providing both effective protection against various types of oxidative stress-induced cellular injury and anticancer action. However, the major limitation of SIH is represented by its labile hydrazone bond that makes it prone to plasma hydrolysis. Recently, nine new SIH analogues derived from aromatic ketones with improved hydrolytic stability were developed. Here we analyzed their antiproliferative potential in MCF-7 breast adenocarcinoma and HL-60 promyelocytic leukemia cell lines. Seven of the tested substances showed greater selectivity than the parent agent SIH towards the latter cancer cell lines compared to non-cancerous H9c2 cardiomyoblast-derived cells. The tested chelators induced a dose-dependent dissipation of the inner mitochondrial membrane potential, an induction of apoptosis as evidenced by Annexin V positivity or significant increases of activities of caspases 3, 7, 8 and 9 and cell cycle arrest. With the exception of nitro group-bearing NHAPI, the studies of iron complexes of the chelators confirmed the crucial role of iron in the mechanism of their antiproliferative action. Finally, all the assayed chelators inhibited the oxidation of ascorbate by iron ions indicating lack of redox activity of the chelator-iron complexes. In conclusion, this study identified several important design criteria for improvement of the antiproliferative selectivity of the aroylhydrazone iron chelators. Several of the novel compounds--in particular the ethylketone-derived HPPI, NHAPI and acetyl-substituted A2,4DHAPI--merit deeper investigation as promising potent and selective anticancer agents. PMID:22521999

  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, 2012 CFR

    2012-04-01

    ... 21 Food and Drugs 6 2012-04-01 2012-04-01 false Tolazoline hydrochloride injection. 522.2474... § 522.2474 Tolazoline hydrochloride injection. (a) Specifications. Each milliliter of sterile aqueous...—(i) Amount. Administer slowly by intravenous injection 4 milligrams per kilogram of body weight or...

  18. 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... § 522.1465 Naltrexone hydrochloride injection. (a) Specifications. Each milliliter of sterile...

  19. 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 Section 522.1465 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES... § 522.1465 Naltrexone hydrochloride injection. (a) Specifications. Each milliliter of sterile...

  20. 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... § 522.2474 Tolazoline hydrochloride injection. (a) Specifications. Each milliliter of sterile aqueous...—(i) Amount. Administer slowly by intravenous injection 4 milligrams per kilogram of body weight or...

  1. 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... § 522.2615 Tripelennamine hydrochloride injection. (a) Specifications. Each milliliter of...

  2. 21 CFR 522.2615 - Tripelennamine hydrochloride injection.

    Code of Federal Regulations, 2013 CFR

    2013-04-01

    ... 21 Food and Drugs 6 2013-04-01 2013-04-01 false Tripelennamine hydrochloride injection. 522.2615 Section 522.2615 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES... § 522.2615 Tripelennamine hydrochloride injection. (a) Specifications. Each milliliter of...

  3. 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... § 522.2474 Tolazoline hydrochloride injection. (a) Specifications. Each milliliter of sterile aqueous...—(i) Amount. Administer slowly by intravenous injection 4 milligrams per kilogram of body weight or...

  4. 21 CFR 522.863 - Ethylisobutrazine hydrochloride injection.

    Code of Federal Regulations, 2013 CFR

    2013-04-01

    ... 21 Food and Drugs 6 2013-04-01 2013-04-01 false Ethylisobutrazine hydrochloride injection. 522.863 Section 522.863 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES... § 522.863 Ethylisobutrazine hydrochloride injection. (a) Specifications. The drug is a sterile...

  5. 21 CFR 522.2615 - Tripelennamine hydrochloride injection.

    Code of Federal Regulations, 2012 CFR

    2012-04-01

    ... 21 Food and Drugs 6 2012-04-01 2012-04-01 false Tripelennamine hydrochloride injection. 522.2615 Section 522.2615 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES... § 522.2615 Tripelennamine hydrochloride injection. (a) Specifications. Each milliliter of...

  6. 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 Section 522.1465 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES... § 522.1465 Naltrexone hydrochloride injection. (a) Specifications. Each milliliter of sterile...

  7. 21 CFR 522.863 - Ethylisobutrazine hydrochloride injection.

    Code of Federal Regulations, 2011 CFR

    2011-04-01

    ... 21 Food and Drugs 6 2011-04-01 2011-04-01 false Ethylisobutrazine hydrochloride injection. 522.863 Section 522.863 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES... § 522.863 Ethylisobutrazine hydrochloride injection. (a) Specifications. The drug is a sterile...

  8. 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... § 522.2474 Tolazoline hydrochloride injection. (a) Specifications. Each milliliter of sterile aqueous...—(i) Amount. Administer slowly by intravenous injection 4 milligrams per kilogram of body weight or...

  9. 21 CFR 522.863 - Ethylisobutrazine hydrochloride injection.

    Code of Federal Regulations, 2012 CFR

    2012-04-01

    ... 21 Food and Drugs 6 2012-04-01 2012-04-01 false Ethylisobutrazine hydrochloride injection. 522.863 Section 522.863 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES... § 522.863 Ethylisobutrazine hydrochloride injection. (a) Specifications. The drug is a sterile...

  10. 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 Section 522.1465 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES... § 522.1465 Naltrexone hydrochloride injection. (a) Specifications. Each milliliter of sterile...

  11. 21 CFR 522.2615 - Tripelennamine hydrochloride injection.

    Code of Federal Regulations, 2011 CFR

    2011-04-01

    ... 21 Food and Drugs 6 2011-04-01 2011-04-01 false Tripelennamine hydrochloride injection. 522.2615 Section 522.2615 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES... § 522.2615 Tripelennamine hydrochloride injection. (a) Specifications. Each milliliter of...

  12. 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 (CONTINUED) ANIMAL DRUGS, FEEDS, AND RELATED PRODUCTS ORAL DOSAGE FORM NEW ANIMAL DRUGS § 520.2582 Triflupromazine hydrochloride tablets....

  13. 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....

  14. 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 (CONTINUED) ANIMAL DRUGS, FEEDS, AND RELATED PRODUCTS ORAL DOSAGE FORM NEW ANIMAL DRUGS § 520.1263c Lincomycin hydrochloride soluble powder....

  15. 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 (CONTINUED) ANIMAL DRUGS, FEEDS, AND RELATED PRODUCTS ORAL DOSAGE FORM NEW ANIMAL DRUGS § 520.1263c Lincomycin hydrochloride soluble powder....

  16. 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...

  17. 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....

  18. 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....

  19. 21 CFR 520.1242e - Levamisole hydrochloride effervescent tablets.

    Code of Federal Regulations, 2011 CFR

    2011-04-01

    ... 21 Food and Drugs 6 2011-04-01 2011-04-01 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;...

  20. 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...

  1. 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...

  2. Naratriptan hydrochloride in extemporaneosly compounded oral suspensions.

    PubMed

    Zhang, Y P; Trissel, L A; Fox, J L

    2000-01-01

    The purpose of this study was to determine the pharmaceutical acceptability and chemical stability of naratriptan hydrochloride in three extemporaneously compounded suspension formulations. The naratriptan-hydrochloride oral suspensions were prepared from 2.5-mg commercial tablets yielding a nominal naratriptan concentration of 0.5 mg/mL. The suspension vehicles selected for testing were Syrpalta, an equal-parts mixture of Ora-Plus and Ora-Sweet, and an equal-parts mixture of Ora-Plus and Ora-Sweet SF. The tablets were crushed and thoroughly triturated to a fine powder using a porcelain mortar and pestle. The powder was incorporated into a portion of the Syrpalta or Ora-Plus suspension vehicle and mixed until homogeneous. The mixtures were then brought to volume with Syrpalta, Ora-Sweet or Ora-Sweet SF, as appropriate. The suspensions were packaged in amber, plastic, screw-cap prescription bottles and stored at 23 deg C for seven days and 4 deg C for 90 days. An adequate suspension was never achieved in Syrpalta. The crushed-tablet powder did not produce a uniformly dispersed mixture and exhibited clumping and a high rate of sedimentation. A distinct layer of the solid tablet material settled immediately after shaking. Over the next four hours, a densely packed, yellow, caked layer formed at the bottom of the containers, making resuspension difficult. During storage, the caking became worse. Chemical analysis was not performed. The Ora-Plus and Ora-Sweet or Ora-Sweet SF suspensions had a slight greenish cast and were resuspended without difficulty by shaking for approximately ten seconds, yielding easily poured and homogeneous mixtures throughout the study. Visible settling and layering did not begin for four hours with the Ora-Sweet suspension and 24 hours for the Ora-Sweet SF suspension. High pressure liquid chromatographic analysis found that the naratriptan concentration in both suspension-vehicle combinations exhibited little or no loss for seven days at 23 deg C and 90 days at 4 deg C. At least 96% of the inital concentration remained at all time points. Naratriptan hydrochloride extemporaneously prepared as oral suspensions from tablets in equal-parts mixtures of Ora-Plus suspension vehicle with Ora-Sweet and with Ora-Sweet SF syrups was pharmaceutically acceptable and chemically stable for at least seven days at 23 deg C and 90 days at 4 deg C. Syrpalta was unacceptable for use as a vehicle for naratriptan hydrochloride suspensions prepared from tablets. PMID:23985892

  3. Treatment of gonorrheal urethritis with spectinomycin hydrochloride

    PubMed Central

    Brown, J.; Tabert, O.; Hanna, J. D.; Rentiers, P. L.

    1974-01-01

    One hundred and eighty-seven males with uncomplicated gonorrheal urethritis were treated with spectinomycin hydrochloride in a dosage of 2 g. given intramuscularly. A failure rate of 3.2% was observed and no complications of therapy were encountered. In addition, 310 strains of N. gonorrhoeae were tested for susceptibility to penicillin G and spectinomycin. All strains were sensitive to 20 μg./ml. of spectinomycin and this susceptibility appeared to decrease as penicillin resistance increased. A greater incidence of relative resistance to penicillin G was observed than in similar studies from other Canadian areas. PMID:4272505

  4. Conformation and conformational exchange of Olopatadine hydrochloride

    NASA Astrophysics Data System (ADS)

    Lei, Lian-di; Zhu, Chuan-jun; Yang, Chun-hui; Cui, Yu-xin

    2008-12-01

    Besides the assignments of the 13C and 1H shifts by 1D and 2D NMR, the experiment 1H spectra of Olopatadine hydrochloride were recorded at temperature range 228-338 K. The variable-temperature spectra revealed a dynamic NMR effect which is attributed to conformational interconversion of the drug. At low temperature, the solution was shown to contain two conformers and the ration of them was 1:1. A conformational process with a free energy of activation of 56.7 kJ mol -1, coalescence temperature 298 K, was interpreted as geminal 1H exchange. Using molecule simulation, conformational candidates for two conformers are proposed.

  5. Synthesis and biological activity evaluation of hydrazone derivatives based on a Tröger's base skeleton.

    PubMed

    Kaplánek, Robert; Havlík, Martin; Dolenský, Bohumil; Rak, Jakub; Džubák, Petr; Konečný, Petr; Hajdúch, Marián; Králová, Jarmila; Král, Vladimír

    2015-04-01

    We report the design and synthesis of novel anticancer agents based on bis-hydrazones separated by a rigid Tröger's base skeleton. This novel approach combines a biologically active moiety (hydrazone) with this scaffold (Tröger's base) to construct DNA intercalators. Evaluation of the anticancer activity of these agents using seven cancer cell lines and two healthy cell lines found that several derivatives had potent anticancer activity and excellent selectivity indexes toward cancer cells. The antimicrobial activities were tested on a set of thirteen bacterial stains, but the prepared compounds were not active. Complexation studies using biologically important metal ions demonstrated that these compounds are able to bind Cu(2+), Fe(3+), Co(2+), Ni(2+) and Zn(2+). DNA intercalation studies showed that the compounds themselves do not interact with DNA, but their metallocomplexes do interact, most likely via intercalation into DNA. PMID:25737088

  6. Molecular oxygen reduction catalyzed by a highly oxidative resistant complex of cobalt-hydrazone at the liquid/liquid interface.

    PubMed

    Kamyabi, Mohammad Ali; Soleymani-Bonoti, Fatemeh; Bikas, Rahman; Hosseini-Monfared, Hassan; Arshadi, Nematollah; Siczek, Milosz; Lis, Tadeusz

    2015-12-28

    A new complex of Co(III) using an oxidative stable hydrazone ligand, CoL, was synthesized and characterized by elemental analysis, spectroscopic methods and single crystal X-ray analysis where HL is bis-[(E)-N'-(phenyl(pyridin-2-yl)methylene)]carbohydrazide. X-ray analysis revealed that the complex is mononuclear and the coordination environment around the Co(III) core is trans-[CoN4Cl2]. The catalytic activity of the complex in the oxygen reduction reaction was investigated. The complex is a highly oxidative resistant cobalt-hydrazone which can efficiently catalyze the reduction of oxygen (O2) by a weak electron donor ferrocene, (Fc), at the polarized water/1,2-dichloroethane (DCE) interface. Oxygen reduction is coupled with proton transfer from water to the organic phase to form hydrogen peroxide, which is extracted into the aqueous phase. PMID:26377052

  7. 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.

  8. Stereoselective synthesis, spectral and antimicrobial studies of some cyanoacetyl hydrazones of 3-alkyl-2,6-diarylpiperidin-4-ones

    NASA Astrophysics Data System (ADS)

    Velayutham Pillai, M.; Rajeswari, K.; Vidhyasagar, T.

    2014-11-01

    A series of novel cyanoacetyl hydrazones of 3-alkyl-2,6-diarylpiperidin-4-ones were synthesized stereoselectively and characterized by IR, Mass, 1H NMR, 13C NMR, 1H-1H COSY and 1H-13C COSY spectra. The stereochemistry of the synthesized compounds was established using NMR spectra. Antimicrobial screening of the synthesized compounds revealed their antibacterial and antifungal potencies. Growth inhibition of Enterobacter Aerogenes by compound 15 was found to be superior to the standard drug.

  9. 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

  10. Synthesis, characterization, biological activity and equilibrium studies of metal(II) ion complexes with tridentate hydrazone ligand derived from hydralazine

    NASA Astrophysics Data System (ADS)

    El-Sherif, Ahmed A.; Shoukry, Mohamed M.; Abd-Elgawad, Mohamed M. A.

    2012-12-01

    In the present study, a new hydrazone ligand (2-((2-phthalazin-1-yl)hydrazono)methyl)phenol) prepared by condensation of hydralazine (1-Hydralazinophthalazine) with salicylaldehyde (SAH). The synthesized SAH-hydrazone and its metal complexes have been characterized by elemental analyses, IR, 1H NMR, solid reflectance, magnetic moment, molar conductance, mass spectra, UV-vis and thermal analysis (TGA). The analytical data of the complexes show the formation of 1:1 [M:L] ratio, where M represents Ni(II), Co(II) and Cu(II) ions, while L represents the deprotonated hydrazone ligand. IR spectra show that SAH is coordinated to the metal ions in a tridentate manner through phthalazine-N, azomethine-N and phenolic-oxygen groups. The ligand and their metal chelates have been screened for their antimicrobial activities using the disc diffusion method against the selected bacteria and fungi. Proton-ligand association constants of (SAH) and the stepwise stability constants of its metal complexes are determined potentiometrically in 0.1 M NaNO3 at different temperatures and the corresponding thermodynamic parameters were derived and discussed. The order of -ΔG° and -ΔH° were found to obey Mn2+ < Co2+ < Ni2+ < Cu2+, in accordance with the Irving-Williams order. The complexes were stabilized by enthalpy changes and the results suggest that the complexation is an enthalpy-driven process. The concentration distribution diagrams of the complexes are evaluated.

  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. Structural, electrochemical and optical properties of di-2-pyridyl ketone 2-furoic acid hydrazone (dpkfah)

    NASA Astrophysics Data System (ADS)

    Bakir, Mohammed; Gyles, Colin

    2003-04-01

    Crystals of di-2-pyridyl ketone 2-furoic acid hydrazone (dpkfah), obtained from a dmso (dimethylsulfoxide) solution of dpkfah, are in the monoclinic space group, P2 1/ n. Structural analysis reveals planar hydrazone moiety, non-coplanar pyridine rings and infinite chains of anti-parallel dpkfah dimers interlocked via a web of hydrogen bonds. Electrochemical measurements on dpkfah in non-aqueous solvents show solvent dependence, single and multi-electronic transfers and electrochemical transformation(s) following the first oxidative or reductive electronic transfer. Optical measurements on dpkfah in non-aqueous solvents show strong solvent dependence. In non-polar solvent such as CH 2Cl 2 a single electronic absorption band with extinction coefficient of 18,600±2000 M -1 cm -1 appeared at 325 nm and in polar solvents a low-energy absorption band at ˜396 nm and a high-energy absorption band at ˜320-335 nm appeared that are concentration, temperature and salt dependent. In the presence and absence of NaBF 4 and NaBH 4, extinction coefficients of 21,000±2000 and 22,500 M -1 cm -1, and 17,200±2,000 and 23,000 M -1 cm -1 were calculated for the low and high energy electronic states of dpkfah in dmf and dmso, respectively at 295 K. Thermo-optical measurements on dpkfah in dmso and dmf confirmed the reversible interconversion between the high and low energy electronic states of dpkfah and allowed calculations of their thermodynamic activation parameters and gave changes in enthalpy (Δ H∅) of +47.5±1.2 and -16.3±0.4 kJ mol -1, entropy (Δ S∅) of +147.7±3.8 and -64.4±1.64 J mol -1 K -1 and free energy (Δ G∅) of +3.49±0.2 and +2.85±0.2 kJ mol -1 and hence equilibrium constant ( K) of +0.25±0.05 and +0.32±0.05 in dmso and dmf, respectively. The reversible BH 4-/BF 4- interconversion of the electronic states of dpkfah points to weak non-covalent interactions between these species and dpkfah and possible use of dpkfah as a spectrophotometric sensor for a variety of physical and chemical stimuli. Chemical stimuli in concentrations <1.00×10 -6 M can be detected and determined using dpkfah in non-aqueous media.

  13. 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

  14. 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...

  15. 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...

  16. 21 CFR 522.723 - Diprenorphine hydrochloride injection.

    Code of Federal Regulations, 2010 CFR

    2010-04-01

    ...) Specifications. Each milliliter of diprenorphine hydrochloride injection, veterinary, contains 2 mg of... injection, veterinary, the use of which is provided for in § 522.883, in wild and exotic animals. (2) It...

  17. 21 CFR 522.723 - Diprenorphine hydrochloride injection.

    Code of Federal Regulations, 2011 CFR

    2011-04-01

    ...) Specifications. Each milliliter of diprenorphine hydrochloride injection, veterinary, contains 2 mg of... injection, veterinary, the use of which is provided for in § 522.883, in wild and exotic animals. (2) It...

  18. 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

  19. 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

  20. 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...

  1. 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...

  2. 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...

  3. 21 CFR 520.1660b - Oxytetracycline hydrochloride capsules.

    Code of Federal Regulations, 2014 CFR

    2014-04-01

    ... containing 125 or 250 milligrams of oxytetracycline hydrochloride. Oxytetracycline is the antibiotic substance produced by growth of Streptomyces rimosus or the same antibiotic substance produced by any other... continuation of compatible antibiotic therapy following parenteral oxytetracycline administration where...

  4. 21 CFR 520.1660b - Oxytetracycline hydrochloride capsules.

    Code of Federal Regulations, 2010 CFR

    2010-04-01

    ... containing 125 or 250 milligrams of oxytetracycline hydrochloride. Oxytetracycline is the antibiotic substance produced by growth of Streptomyces rimosus or the same antibiotic substance produced by any other... continuation of compatible antibiotic therapy following parenteral oxytetracycline administration where...

  5. 21 CFR 520.1660b - Oxytetracycline hydrochloride capsules.

    Code of Federal Regulations, 2012 CFR

    2012-04-01

    ... containing 125 or 250 milligrams of oxytetracycline hydrochloride. Oxytetracycline is the antibiotic substance produced by growth of Streptomyces rimosus or the same antibiotic substance produced by any other... continuation of compatible antibiotic therapy following parenteral oxytetracycline administration where...

  6. 21 CFR 520.1660b - Oxytetracycline hydrochloride capsules.

    Code of Federal Regulations, 2011 CFR

    2011-04-01

    ... containing 125 or 250 milligrams of oxytetracycline hydrochloride. Oxytetracycline is the antibiotic substance produced by growth of Streptomyces rimosus or the same antibiotic substance produced by any other... continuation of compatible antibiotic therapy following parenteral oxytetracycline administration where...

  7. 21 CFR 520.1660b - Oxytetracycline hydrochloride capsules.

    Code of Federal Regulations, 2013 CFR

    2013-04-01

    ... containing 125 or 250 milligrams of oxytetracycline hydrochloride. Oxytetracycline is the antibiotic substance produced by growth of Streptomyces rimosus or the same antibiotic substance produced by any other... continuation of compatible antibiotic therapy following parenteral oxytetracycline administration where...

  8. 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.

  9. Antitumor activity of a 2-pyridinecarboxaldehyde 2-pyridinecarboxylic acid hydrazone copper complex and the related mechanism.

    PubMed

    Yang, Yingli; Huang, Tengfei; Zhou, Sufeng; Fu, Yun; Liu, Youxun; Yuan, Yanbin; Zhang, Qiongqing; Li, Shaoshan; Li, Changzheng

    2015-09-01

    In the present study, 2-pyridinecarboxaldehyde 2-pyridinecarboxylic acid hydrazone (PPAH) was prepared and its antitumor activity was evaluated. The inhibition of proliferation of PPAH against the HepG2 and HCT-116 cell lines was less effective, yet in the presence of copper ions, the mixture demonstrated excellent antitumor activity (IC50 at 2.75±0.30 µM for the HepG2 cell line, and 1.90±0.20 µM for the HCT-116 cell line, respectively) and the new active species was confirmed to be a PPAH copper complex with a 1:1 ratio by spectral analysis. The excellent antitumor activity of the copper complex prompted us to investigate the underlying mechanism. RT-PCR was performed to detect the changes in the expression of apoptotic genes induced by PPAH and its copper complex. However, no changes were observed when the cells were treated by the agents for 24 or 48 h, indicating that ROS were unlikely involved. Cell cycle analysis showed that both PPAH and its copper complex led to S phase arrest of the cells. The sDNA relaxation assay revealed that the PPAH-copper complex displayed dual topoisomerase inhibition for type I and II. The data suggest that the inhibition of proliferation exhibited by the PPAH copper complex may stem from its dual topoisomerase inhibition, which is rarely observed for a metal complex. PMID:26135482

  10. Design, synthesis, and insecticidal activities of phthalamides containing a hydrazone substructure.

    PubMed

    Liu, Ming; Wang, Yi; Wangyang, Wei-zi; Liu, Feng; Cui, Yong-liang; Duan, You-sheng; Wang, Min; Liu, Shang-zhong; Rui, Chang-hui

    2010-06-01

    Fluobendiamide is the first commercialized artificial synthetic insecticide acting on the ryanodine receptor. This new molecule possesses a combination of excellent insecticidal activity and eco-friendly characteristics with a skeleton structure of phthalamide. In this study, we incorporated hydrazone, present in many pesticidal compounds reported during the last two decades, into phthalamide derivatives via Schiff-base condensation and aminolysis to obtain 21 new compounds; these compounds were characterized by proton nuclear magnetic resonance ((1)H NMR), infrared spectroscopy (IR), and high-resolution mass spectrometry (HRMS) or elemental analysis. A preliminary bioassay against peach aphids ( Myzus persicae ) revealed that the title compounds exhibited good stomach toxicity at 600 mg/L. Twelve new compounds were found to display higher activity than postive control flubendiamide (LC(50) = 184.099 mg/L), however, LC(50) was less than 100 mg/L only for compounds 4e, 4o, 4s, 4t (59-77 mg/L). That is, combinations of a p-fluorophenyl or (methyl)thienyl group at the Ar position with an isopropyl or cyclohexyl group at the R position might improve the lethality of the designed phthalamide derivative. Preliminary results of a bioassay at 600 mg/L against diamondback moth ( Plutella xylostella , Linnaeus) showed that only the title compound 4e possessed good larvicidal activity. On comparison of the bioassay results of stomach toxicity and larvicidal activity, it is noteworthy that the compound incorporating phenylpyrazolyl exhibited good larvicidal activity and poor stomach activity. PMID:20450195

  11. 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.

  12. 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

  13. 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.

  14. 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.

  15. 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

  16. 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

  17. 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

  18. Canine olfactory sensitivity to cocaine hydrochloride and methyl benzoate

    NASA Astrophysics Data System (ADS)

    Waggoner, L. Paul; Johnston, James M.; Williams, Marc; Jackson, Jan; Jones, Meredith H.; Boussom, Teresa; Petrousky, James A.

    1997-02-01

    Methyl benzoate is a consistent product of cocaine hydrochloride exposed to humid air. The detection responses of dogs trained to detect illicit cocaine hydrochloride may be controlled by vapor from cocaine, methyl benzoate, or other constituents of illicit cocaine. The present study addressed the following questions: 1) How capable are dogs of detecting methyl benzoate compared to cocaine hydrochloride, 2) When dogs are trained to detect methyl benzoate, do they respond to cocaine hydrochloride as being the same or different from methyl benzoate. These questions were investigated using random source dogs trained and tested under laboratory conditions. Odor stimuli were generated and delivered by a vapor generation systems, the outputs from which were characterized by thermal desorption GC/MS. ONe group of dogs was trained to discriminate pharmaceutical grade and illicit cocaine hydrochloride from clean air and tested using a two lever procedure to determine their sensitivity to these substances. A second group of dogs was trained to discriminate between methyl benzoate and clean air and tested for their sensitivity to the substance. The dogs in this second group were then tested using a three lever procedure to determine their sensitivity to these substances. A second group of dogs was trained to discriminate between methyl benzoate and clean air and tested for their sensitivity to the substance. The dogs in this second group were then tested using a three lever procedure to determine whether they responded to cocaine hydrochloride as the same or different from methyl benzoate.

  19. 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

  20. 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.

  1. 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…

  2. 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

  3. Fast and catalyst-free hydrazone ligation via ortho-halo-substituted benzaldehydes for protein C-terminal labeling at neutral pH.

    PubMed

    Xu, Yang; Xu, Ling; Xia, Yuan; Guan, Chao-Jian; Guo, Qing-Xiang; Fu, Yao; Wang, Chen; Li, Yi-Ming

    2015-08-28

    Rapid and catalyst-free hydrazone ligation reaction between ortho-halobenzaldehyde derivatives and peptide/protein hydrazides was observed at neutral pH and room temperature. 2-Chlorobenzaldehyde exhibited the fastest reaction and highest conversion rates among the series of ortho-halobenzaldehydes. The resulting hydrazone-containing bioconjugation products were also found to be fairly stable under experimental conditions. The new ligation strategy was successfully used for protein C-terminal labeling and should provide a practical approach for the modification of proteins. PMID:26195073

  4. Synthesis of novel diflunisal hydrazide-hydrazones as anti-hepatitis C virus agents and hepatocellular carcinoma inhibitors.

    PubMed

    Şenkardeş, Sevil; Kaushik-Basu, Neerja; Durmaz, İrem; Manvar, Dinesh; Basu, Amartya; Atalay, Rengül; Küçükgüzel, Ş Güniz

    2016-01-27

    Hepatitis C virus (HCV) infection is a main cause of chronic liver disease, leading to liver cirrhosis and hepatocellular carcinoma (HCC). The objective of our research was to develop effective agents against viral replication. We have previously identified the hydrazide-hydrazone scaffold as a promising hepatitis C virus (HCV) and hepatocelluler inhibitor. Herein we describe the design a number of 2',4'-difluoro-4-hydroxy-N'-(arylmethylidene) biphenyl-3-carbohydrazide (3a-t) as anti-HCV and anticancer agents. Results from evaluation of anti-HCV activity indicated that most of the synthesized hydrazone derivatives inhibited viral replication in the Huh7/Rep-Feo1b and Huh 7.5-FGR-JCI-Rluc2A reporter systems. Antiproliferative activities of increasing concentrations of 2',4'-difluoro-4-hydroxy-N'-(2-pyridyl methylidene)biphenyl-3-carbohydrazide 3b and diflunisal (2.5-40 μM) were assessed in liver cancer cell lines (Huh7, HepG2, Hep3B, Mahlavu, FOCUS and SNU-475) with sulforhodamine B assay for 72 h. Compound 3b with 2-pyridinyl group in the hydrazone part exhibited promising cytotoxic activity against all cell lines with IC50 values of 10, 10.34 16.21 4.74, 9.29 and 8.33 μM for Huh7, HepG2, Hep3B, Mahlavu, FOCUS and SNU-475 cells, respectively, and produced dramatic cell cycle arrest at SubG1/G0 phase as an indicator of apoptotic cell death induction. PMID:26695731

  5. Synthesis and absorption and luminescence spectral properties of 3-formyl and 3-acetyl-7- (diethylamino) coumarin hydrazones

    SciTech Connect

    Komlev, I.V.; Khrolova, O.R.; Mikhailova, T.A.; Tavrizova, M.A.

    1985-10-10

    Various substitued coumarins are of interest as organic luminphors, many of which are effective laser dyes for the blue-green region of the spectrum. This paper attempts to extend the range of fluorescent coumarin dyes by synthesizing and investigating substitued hydrazones of 3-formyl- and 3-acetyl-coumarins (III). The absorption and luminescence spectral properties of the coumarins synthesized are discussed. Some lowering of the quantum yield of fluorescence in comparison with known coumarins is explained by the nonradiative degradation of the energy of electron excitation, which competes with the fluorescence.

  6. A spectrophotometric method for the quantification of an enzyme activity producing 4-substituted phenols: determination of toluene-4-monooxygenase activity.

    PubMed

    Nolan, Louise C; O'Connor, Kevin E

    2005-09-15

    A spectrophotometric method for the quantitative determination of an enzyme activity resulting in the accumulation of 4-substituted phenols is described in this article. Toluene-4-monooxygenase (T4MO) activity in whole cells of Pseudomonas mendocina KR1 is used to demonstrate this method. This spectrophotometric assay is based on the coupling of T4MO activity with tyrosinase activity. The 4-substituted phenol, produced by the action of T4MO on the aromatic ring of a substituted arene, is a substrate for tyrosinase, which converts phenols to o-quinones. The latter react with the nucleophile 3-methyl-2-benzothiazolinone hydrazone (MBTH) to produce intensely colored products that absorb light maximally at different wavelengths, depending on the phenolic substrate used. The incubation of whole cells of P. mendocina KRI with fluorobenzene resulted in the accumulation of 4-fluorophenol. The coupling of T4MO activity with tyrosinase activity in the presence of fluorobenzene resulted in the formation of a colored product absorbing maximally at 480 nm. The molar absorptivity (epsilon) value for the o-quinone-MBTH adduct formed from 4-fluorophenol was determined experimentally to be 12,827 M(-1) cm(-1) with a linear range of quantification between 2.5 and 75 microM. The whole cell assay was run as a continuous indirect assay. The initial rates of T4MO activity toward fluorobenzene, as determined spectrophotometrically, were 61.8+/-4.4 nmol/min/mg P. mendocina KR1 protein (using mushroom tyrosinase), 64.9+/-4.6 nmol/min/mg P. mendocina KR1 protein (using cell extracts Pseudomonas putida F6), and, as determined by HPLC analysis, 62.6+/-1.4 nmol/min/mg P. mendocina KR1 protein. PMID:16061193

  7. [Colorimetric determination of sulfite in "kanpyo" (dried gourd shavings) and "konnyakuseiko" (devil's-tongue fine powder) using sulfite oxidase and catalase].

    PubMed

    Aoki, Kazuko; Ueno, Seiichi; Ishizaki, Mutsuo

    2002-06-01

    A simple and convenient method for colorimetric determination of sulfite in foods based on its conversion to formaldehyde with sulfite oxidase and catalase was developed. Sulfite in a sample was extracted with water and then diluted with methanol. One mL of sample solution containing about 5-10 micrograms of sulfite was taken into a test tube with a ground-glass stopper, and 3 mL of 0.04 mol/L borate buffer (pH 8.7), 1 mL of 0.4% 3-methyl-2-benzothiazolinone hydrazone (MBTH) solution, 2,000 units of catalase solution and 1.0 units of sulfite oxidase were added. The mixture was incubated for 35 minutes at 37 degrees C. Then 0.15 mL of 1 mol/L hydrochloric acid and 5 mL of 0.2% iron(III) nitrate solution were added. The reaction mixture was transferred to a measuring flask after standing for 5 minutes at room temperature, and diluted to 20 mL with methanol. The absorbance of this solution was measured using a spectrophotometer at the wavelength of 635 nm. The calibration curve prepared with sodium sulfite showed linearity between 0 to 16 micrograms/mL as sulfur dioxide. The recoveries of sulfite in "Kanpyo" (dried gourd shavings) and "Konnyaku-seiko" (devil's-tongue fine powder) by the proposed method were 97-104%, and the coefficients of variation were below 6%. The sulfite values in these foods determined by the proposed method were reasonably consistent with those obtained by the bubbling distillation-alkaline titration method. PMID:12238155

  8. 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

  9. A new enzymo-chemical method for simultaneous assay of methanol and formaldehyde.

    PubMed

    Gonchar, M V; Grabek, D; Oklejewich, B; Pavlishko, H M; Shamlian, O V; Sybirny, V A; Kotylak, Z; Rudke, K; Csöregi, E; Sibirny, A A

    2005-01-01

    A new enzymo-chemical method for the simultaneous assay of methanol and formaldehyde in mixtures is described which exploits alcohol oxidase (AO) and aldehyde-selective reagent, 3-methyl-2-benzothiazolinone hydrazone (MBTH). The enzyme is used for methanol oxidation to formaldehyde and MBTH plays a double role: 1) at the first step of reaction, it forms a colorless azine adduct with pre-existing and enzymatically formed formaldehyde and masks it from oxidation by AO; 2) at the second step of reaction, non-enzymatic oxidation of azine product to cyanine dye occurs in the presence of ferric ions in acid medium. Pre-existing formaldehyde content is assayed by colorimetric reaction with MBTH without treating samples by AO, and methanol content is determined by a gain in a colored product due to methanol-oxidising reaction. Possibility of differential assay of methanol and formaldehyde by the proposed method has been proved for model solutions as well as for real samples of industrial waste and technical formaline. A threshold sensitivity of the assay method for both analytes is near 1 microM that responds to 30-32 ng analyte in 1 ml of reaction mixture and is 3.2-fold higher when compared to the chemical method with the use of permanganate and chromotropic acid. Linearity of the calibration curve is reliable (p < 0.0001) and standard deviation for parallel measurements for real samples does not exceed 7%. The proposed method, in contrast to the standard chemical approach, does not need the use of aggressive chemicals (concentrated sulfuric, phosphoric, chromotropic acids, permanganate), it is more simple in fulfillment and can be used for industrial wastes control and certification of formaline-contained stuffs. PMID:16566143

  10. UV analysis of Amadori-glycated phosphatidylethanolamine in foods and biological samples.

    PubMed

    Oak, Jeong-Ho; Nakagawa, Kiyotaka; Miyazawa, Teruo

    2002-03-01

    Maillard reactions are among the most important of the chemical and oxidative changes occurring in food and biological samples that contribute to food deterioration and to the pathophysiology of human disease. Although the association of lipid glycation with this process has recently been shown, the number of lipid glycation products in food and biological materials has not been clear. In this study, we synthesized the Amadori products derived from the glycation of phosphatidylethanolamine (PE), i.e., Amadori-PEs. Dioleoyl PE was incubated with glucose and lactose for 15 days, and the resultant Amadori-PEs were purified and isolated using solid phase extraction followed by HPLC. With this procedure, essentially pure (>98% purity) Amadori-PEs glycated with glucose (Glc-PE) and with lactose (Lac-PE) were obtained and used as standards in the subsequent studies. To determine the presence of Amadori-PEs in food and biological samples, the carbonyl group of Amadori-PEs was ultraviolet (UV)-labeled with 3-methyl-2-benzothiazolinone hydrazone, and the labeled Amadori-PEs were analyzed with normal phase HPLC-UV (318 nm). The detection limit was 4.5 ng (5 pmol) for Glc-PE and 5.3 ng (5 pmol) for Lac-PE. Among the several food samples examined, infant formula and chocolate contained a high amount of both Glc-PE and Lac-PE over wide concentration ranges, such as 1.5-112 microg/g. Testing biological materials showed Amadori-PE (Glc-PE) was detectable in rat plasma. PMID:11893788

  11. Spectrophotometric, spectrofluorimetric, and densitometric methods for the determination of indapamide.

    PubMed

    Youssef, Nadia F

    2003-01-01

    Three sensitive spectrophotometric, spectrofluorimetric, and densitometric methods are described for the determination of indapamide. The first and second methods are based on the oxidative coupling reaction of indapamide with 3-methyl-2-benzothiazolinone hydrazone HCl (MBTH) in the presence of cerium(IV) ammonium sulfate in an acidic medium. The absorbance of the reaction product is measured at the lambdamax, 601 nm. With the same reaction, indapamide is determined by its quenching effect on the fluorescence of excess cerous ions at the emission lambdamax, 350 nm, and the excitation at lambdamax, 300 nm. The reaction conditions were optimized, and Beer's law was obeyed for indapamide at 1.2-9.6 microg/mL with mean recoveries of 99.92 +/- 0.83 and 99.97 +/- 1.11%, respectively. The third method, a stability-indicating densitometric assay, was developed for the determination of indapamide, using toluene-ethyl acetate-glacial acetic acid (69 + 30 + 1, v/v/v) as the developing system and scanning at the lambdamax, 242 nm, in the presence of the degradation product and related substance; for the indapamide concentration range of 0.6-6 microg/spot, the mean recovery was 99.73 +/- 0.71%. The proposed methods were successfully applied to the determination of indapamide in bulk powder and commercial tablets, and the results of the analysis agreed statistically with those obtained with the official method. Furthermore, the methods were validated according to the guidelines of the U.S. Pharmacopeia and also assessed by applying the standard additions technique. PMID:14632394

  12. 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

  13. Ligational, analytical and biological applications on oxalyl bis(3,4-dihydroxybenzylidene) hydrazone

    NASA Astrophysics Data System (ADS)

    El-Asmy, Ahmed A.; El-Gammal, O. A.; Radwan, H. A.; Ghazy, S. E.

    2010-09-01

    The molecular modeling and parameters have been calculated to confirm the geometry of oxalyl bis(3,4-dihydroxybenzylidene) hydrazone, H 6L. The metal complexes of Cr 3+, VO 2+, ZrO 2+, HfO 2+, UO 22+ and MoO 22+ with H 6L have been prepared and characterized by partial elemental analysis, spectral studies (electronic; IR), thermal analysis and magnetic measurements. The data suggest the formation of polymer complexes with a unit [Cr(H 4L)(H 2O) 3Cl]H 2O, [VO(H 4L)(H 2O) 2], [Hf(H 4L)(H 2O)]H 2O [UO 2(H 4L)(H 2O) 2]2H 2O [MoO 2(H 4L)] and [(ZrO) 2(H 2L)-(C 2H 5OH) 2]. The ligand behaves as a dibasic bidentate in all complexes except ZrO 2+ which acts as a tetrabasic tetradentate with the two ZrO 2+ ions. An octahedral geometry was proposed for the Cr 3+, HfO 2+, MoO 22+and UO 22+ complexes and square pyramid for VO 2+. The Cr 3+ is necessary to degrade the DNA of eukaryotic subject completely; the other complexes have little effect. H 6L was found suitable as a new reagent for the separation and preconcentration of ZrO 2+ ions from different water samples using flotation technique with satisfactory results.

  14. 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

  15. Mononuclear and three-dimensional metal complexes based on a multidentate hydrazone ligand.

    PubMed

    Liu, Yan-Fei; Liu, Ya-Ping; Zhang, Ke-Ke; Ren, Qing-Ling; Qin, Jie

    2015-02-01

    A potentially pentadentate hydrazone ligand, N'-[1-(pyrazin-2-yl)ethylidene]nicotinohydrazide (HL), was prepared from the condensation reaction of nicotinohydrazide and acetylpyrazine. Reactions of HL with MnCl2, Mn(CH3COO)2 and Cd(CH3COO)2 afforded three metal complexes, namely dichlorido{N'-[1-(pyrazin-2-yl-κN(1))ethylidene]nicotinohydrazide-κ(2)N',O}manganese(II), [MnCl2(C12H11N5O)], (I), bis{N'-[1-(pyrazin-2-yl-κN(1))ethylidene]nicotinohydrazidato-κ(2)N',O]manganese(II), [Mn(C12H10N5O)2], (II), and poly[[(acetato-κ(2)O,O'){μ3-N'-[1-(pyrazin-2-yl-κ(2)N(1):N(4))ethylidene]nicotinohydrazidato-κ(3)N',O:N(1)}cadmium(II)] chloroform disolvate], {[Cd(C12H10N5O)(CH3COO)]·2CHCl3}n, (III), respectively. Complex (I) has a mononuclear structure, the Mn(II) centre adopting a distorted square-pyramidal coordination. Complex (II) also has a mononuclear structure, with the Mn(II) centre occupying a special position (C2 symmetry) and adopting a distorted octahedral coordination environment, which is defined by two O atoms and four N atoms from two N'-[1-(pyrazin-2-yl)ethylidene]nicotinohydrazidate (L(-)) ligands related via a crystallographic twofold axis. Complex (III) features a unique three-dimensional network with rectangular channels, and the L(-) ligand also serves as a counter-anion. The coordination geometry of the Cd(II) centre is pentagonal bipyramidal. This study demonstrates that HL, which can act as either a neutral or a mono-anionic ligand, is useful in the construction of interesting metal-organic compounds. PMID:25652278

  16. 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 photoexcitation.

  17. 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

  18. Ticlopidine hydrochloride use and threatened stroke.

    PubMed Central

    Rothrock, J F; Hart, R G

    1994-01-01

    Ticlopidine hydrochloride is an antiplatelet agent of proven antithrombotic efficacy that in December 1991 became available for general clinical use in the United States. The relative value of ticlopidine compared with aspirin, also an effective antiplatelet agent, has become a key clinical issue. Whereas ticlopidine is somewhat more effective than aspirin for preventing stroke in certain populations, it is also more expensive and potentially toxic. We recommend its use for patients with threatened stroke who are intolerant of aspirin and for patients who have cerebral ischemic symptoms despite aspirin therapy. Patients surviving major ischemic stroke make up a third group for whom ticlopidine use may be recommended in preference to aspirin. The use of ticlopidine rather than aspirin in patients with other cerebrovascular conditions is not strongly supported by existing data. The risk-benefit-cost equation involving ticlopidine versus other antithrombotic therapies is complex, rendering a wide range of acceptable management practices. If reliable laboratory monitoring for neutropenia during the first 3 months of therapy is not feasible, ticlopidine should not be used. PMID:8128701

  19. Stability of cefozopran hydrochloride in aqueous solutions.

    PubMed

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

    2016-04-01

    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

  20. Immobilization of polar bears (Ursus maritimus Phipps) with a mixture of tiletamine hydrochloride and zolazepam hydrochloride.

    PubMed

    Haigh, J C; Stirling, I; Broughton, E

    1985-01-01

    A 1:1 mixture of tiletamine hydrochloride and zolazepam hydrochloride was tested on 39 polar bears in and near Churchill, Manitoba, Canada during October 1983. The mean dose for satisfactory immobilization with a single injection was 5.1 mg/kg. Bears showed signs of ataxia from 1-3 min following injection and were usually sitting within 4 min. The mean induction time, taken as the adoption of sternal recumbency, was 5.1 min. Maximum relaxation was usually seen by about 20 min post-injection. The duration of immobilization appeared to be related to the dose of drug received. In bears that received a dose near the mean, recumbency lasted about 2 hr. Cubs of the year recovered more quickly than adults. Preliminary results indicated that the bears did not suffer respiratory depression and were able to thermoregulate while immobilized. Bears could be handled safely while under the effects of the drug and workers could readily evaluate the state of their sedation by their reactions. The drug did not appear to provide good analgesia at the doses tested. PMID:3981743

  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. 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.

  3. Synthesis and Screening of Human Monoamine Oxidase-A Inhibitor Effect of New 2-Pyrazoline and Hydrazone Derivatives.

    PubMed

    Evranos-Aksöz, Begüm; Baysal, İpek; Yabanoğlu-Çiftçi, Samiye; Djikic, Teodora; Yelekçi, Kemal; Uçar, Gülberk; Ertan, Rahmiye

    2015-10-01

    A group of 3,5-diaryl-2-pyrazoline and hydrazone derivatives was prepared via the reaction of various chalcones with hydrazide compounds in ethanol. Twenty original compounds were synthesized. Ten of these original compounds have a pyrazoline structure, nine of these original compounds have a hydrazone structure, and one of these original compounds has a chalcone structure. Structural elucidation of the compounds was performed by IR, (1)H NMR, (13)C NMR, mass spectral data, and elemental analyses. These compounds were tested for their inhibitory activities toward the A and B isoforms of human monoamine oxidase (MAO). Except for 3k and 6c, all compounds were found to be competitive, reversible, and selective inhibitors for either one of the isoforms (hMAO-A or MAO-B). Compounds 3k and 6c were found to be competitive, reversible, but non-selective MAO inhibitors. Compound 6h showed hMAO-B inhibitory activity whereas the others potently inhibited hMAO-A. Compound 5c showed higher selectivity than the standard drug moclobemide. According to the experimental K(i) values, compounds 6i, 6d, and 6a exhibited the highest inhibitory activity toward hMAO-A. The AutoDock 4.2 program was employed to perform automated molecular docking. The calculated results obtained computationally were in good agreement with the experimental values. PMID:26293971

  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. 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.

  6. 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

  7. 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

  8. 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

  9. 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...

  10. I2-Catalyzed Oxidative Coupling Reactions of Hydrazones and Amines and the Application in the Synthesis of 1,3,5-Trisubstituted 1,2,4-Triazoles.

    PubMed

    Chen, Zhengkai; Li, Hongli; Dong, Weipeng; Miao, Maozhong; Ren, Hongjun

    2016-03-18

    A general and expeditious approach for the metal-free mediated synthesis of 1,3,5-trisubstituted 1,2,4-triazoles from hydrazones and aliphatic amines has been achieved under aerobic oxidative conditions. The reaction proceeds through a cascade C-H functionalization, double C-N bonds formation, and oxidative aromatization sequence. PMID:26914527

  11. 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...

  12. Measurement of pseudoephedrine hydrochloride dissolution using chloride-ion electrode.

    PubMed

    Chen, S T; Thompson, R C; Poust, R I

    1981-11-01

    Experiments were performed to determine the suitability of using a chloride-ion electrode for the measurement of pseudoephedrine hydrochloride dissolution from commercially available compressed tablets. Dissolution experiments were carried out in 500 ml of distilled water using the USP paddle method at 100 rpm. Both chloride ion and pseudoephedrine (UV spectrophotometry) were measured at six different sampling times. Percent dissolved versus time values were linearized on a log-normal probability basis. The slopes of individual lines obtained from the chloride and pseudoephedrine measurements were compared using a Student t test and did not differ significantly (t = 0.415, df = 5, p greater than 0.05). In addition to providing an efficient, inexpensive, and simple method for measuring pseudoephedrine hydrochloride dissolution rates, the chloride-ion electrode could be used in the measurement of dissolution rates for a wide variety of drugs available as hydrochloride salts. PMID:7299681

  13. 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.

  14. 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

  15. Stability and compatibility of topotecan hydrochloride with selected drugs.

    PubMed

    Mayron, D; Gennaro, A R

    1999-05-01

    The physical and chemical compatibility of topotecan 56 microg/mL (as the hydrochloride) with 18 other drugs during simulated Y-site injection was studied. A vial of topotecan hydrochloride was reconstituted under aseptic conditions with sterile water for injection to yield a solution containing 1 mg of topotecan base per milliliter and further mixed with 0.9% sodium chloride injection or 5% dextrose injection. Equal volumes of topotecan solution and each secondary drug, also prepared in 0.9% sodium chloride injection or 5% dextrose injection, were mixed in sterile vials. All mixtures were stored at 20-23 degrees C under normal fluorescent light. Samples were taken initially and at four hours for analysis by high-performance liquid chromatography, visual inspection, and pH measurement. With a few exceptions, the drug combinations exhibited no visible change in color or clarity initially or after four hours, and the concentration of topotecan hydrochloride and of the secondary drugs was 95% or more of the initial concentration. The concentration of topotecan hydrochloride dropped to 88.7% of the initial concentration after four hours when the drug was mixed with ticarcillin disodium and with clavulanate potassium in 5% dextrose injection. An intense yellow color and a slight haze developed immediately after topotecan hydrochloride was mixed with dexamethasone sodium phosphate or with fluorouracil in 0.9% sodium chloride injection. The topotecan-mitomycin combination in both diluents became pale purple immediately and turned dark pink-lavender within four hours, after which analysis showed 15-20% degradation of mitomycin. During simulated Y-site injection, topotecan hydrochloride was physically and chemically compatible with 15 of 18 drug products. PMID:10344611

  16. 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

  17. 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

  18. [Effect of topical exhedrine hydrochloride on muco-ciliary transport].

    PubMed

    Grammatica, L; Fiorella, R

    1983-07-30

    The time of nasal M.C.T. (Mucus Ciliar Transport) was studied by the indirect objective method of bleu-sky in 30 healthy subjects before and after the application of efedrina hydrochloride in water solution associated with timolo, eucaliptolo, mentolo essence of canfora monobramata and clorbutamolo. The time of nasal M.C.T., regular in the 87% of the subjects during the first determination was found extended in almost all of the cases after the application of vasoconstrictor (85%). This experimental data may be caused both by a direct effect of efedrina hydrochloride and by the substances associated in the solution and their physical characteristics. PMID:6626327

  19. 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

  20. 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

  1. 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)

  2. 21 CFR 558.315 - Levamisole hydrochloride (equivalent).

    Code of Federal Regulations, 2010 CFR

    2010-04-01

    ... 21 Food and Drugs 6 2010-04-01 2010-04-01 false Levamisole hydrochloride (equivalent). 558.315 Section 558.315 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL DRUGS, FEEDS, AND RELATED PRODUCTS NEW ANIMAL DRUGS FOR USE IN ANIMAL FEEDS Specific New Animal Drugs for Use in Animal Feeds...

  3. Stability of propranolol hydrochloride in SyrSpend SF.

    PubMed

    Geiger, Christine M; Voudrie, Mark A; Sorenson, Bridget

    2012-01-01

    Propranolol hydrochloride is a beta blocker used to treat high blood pressure, abnormal heart rhythms, heart disease, pheochromocytoma, and certain types of tremors. Propranolol is marketed by Wyeth (now a part of Pfizer) and AstraZeneca under the brand names Inderal, Inderal LA, Avlocardyl, Deralin, Dociton, Inderalici, InnoPran XL, Sumial, Anaprilium, Bedranol SR (Sandoz). It is also available generically from several manufacturers. Propranolol hydrochloride is available as tablet, capsule, and oral liquid dosage forms in several strengths. Some patients are unable to tolerate oral tablets and capsules, challenging compounding pharmacies to seek alternative dosing options; namely oral solutions and suspensions. The objective of this study was to determine the stability of propranolol hydrochloride in SyrSpend SF. The drug was compounded into a 1-mg/mL suspension using SyrSpend SF and subsequently stored in a low-actinic plastic prescription bottle at room temperature conditions. Six samples were assayed at each specific time point extending to 90 days by a stability-indicating high-performance liquid chromatography method. The method was validated for its specificity through forced-degradation studies. Based on the data collected, when protected from light at room temperature, the beyond-use date of propranolol hydrochloride in SyrSpend SF was shown to be at least 90 days. PMID:23259369

  4. 21 CFR 520.1242e - Levamisole hydrochloride effervescent tablets.

    Code of Federal Regulations, 2013 CFR

    2013-04-01

    ... thoroughly. Allow 1 gallon of medicated water for each 100 pounds body weight of pigs to be treated. No other....1242e Section 520.1242e Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN...: (1) Amount. The equivalent of 8 milligrams of levamisole hydrochloride per kilogram of body...

  5. 21 CFR 520.1242e - Levamisole hydrochloride effervescent tablets.

    Code of Federal Regulations, 2012 CFR

    2012-04-01

    ... thoroughly. Allow 1 gallon of medicated water for each 100 pounds body weight of pigs to be treated. No other....1242e Section 520.1242e Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN...: (1) Amount. The equivalent of 8 milligrams of levamisole hydrochloride per kilogram of body...

  6. 21 CFR 520.2345a - Tetracycline hydrochloride capsules.

    Code of Federal Regulations, 2010 CFR

    2010-04-01

    ... 21 Food and Drugs 6 2010-04-01 2010-04-01 false Tetracycline hydrochloride capsules. 520.2345a Section 520.2345a Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES... this drug to use by or on the order of a licensed veterinarian....

  7. 21 CFR 520.2345a - Tetracycline hydrochloride capsules.

    Code of Federal Regulations, 2011 CFR

    2011-04-01

    ... 21 Food and Drugs 6 2011-04-01 2011-04-01 false Tetracycline hydrochloride capsules. 520.2345a Section 520.2345a Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES... this drug to use by or on the order of a licensed veterinarian....

  8. 21 CFR 520.2345a - Tetracycline hydrochloride capsules.

    Code of Federal Regulations, 2014 CFR

    2014-04-01

    ... 21 Food and Drugs 6 2014-04-01 2014-04-01 false Tetracycline hydrochloride capsules. 520.2345a Section 520.2345a Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES... this drug to use by or on the order of a licensed veterinarian....

  9. 21 CFR 520.2345a - Tetracycline hydrochloride capsules.

    Code of Federal Regulations, 2013 CFR

    2013-04-01

    ... 21 Food and Drugs 6 2013-04-01 2013-04-01 false Tetracycline hydrochloride capsules. 520.2345a Section 520.2345a Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES... this drug to use by or on the order of a licensed veterinarian....

  10. 21 CFR 520.2345a - Tetracycline hydrochloride capsules.

    Code of Federal Regulations, 2012 CFR

    2012-04-01

    ... 21 Food and Drugs 6 2012-04-01 2012-04-01 false Tetracycline hydrochloride capsules. 520.2345a Section 520.2345a Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES... this drug to use by or on the order of a licensed veterinarian....

  11. EVALUATION OF THE POTENTIAL CARCINOGENICITY OF O-TOLUIDINE HYDROCHLORIDE

    EPA Science Inventory

    o-Toluidine hydrochloride is a potential human carcinogen, classified as weight-of-evidence Group B2 under the EPA Guidelines for Carcinogen Risk Assessment (U.S. EPA, 1986a). vidence on potential carcinogenicity from animal studies is "Sufficient," and the evidence from human st...

  12. 40 CFR 180.276 - Formetanate hydrochloride; tolerances for residues.

    Code of Federal Regulations, 2012 CFR

    2012-07-01

    ... hydrochloride) in or on raw agricultural commodities as follows: Commodity Parts per million Apple 0.50 Apple, wet pomace 1.5 Grapefruit 1.5 Lemon 0.60 Lime 0.03 Nectarine 0.40 Orange 1.5 Peach 0.40 Pear...

  13. 40 CFR 180.276 - Formetanate hydrochloride; tolerances for residues.

    Code of Federal Regulations, 2010 CFR

    2010-07-01

    ... hydrochloride) in or on raw agricultural commodities as follows: Commodity Parts per million Apple 0.50 Apple, wet pomace 1.5 Grapefruit 1.5 Lemon 0.60 Lime 0.03 Nectarine 0.40 Orange 1.5 Peach 0.40 Pear...

  14. 40 CFR 180.276 - Formetanate hydrochloride; tolerances for residues.

    Code of Federal Regulations, 2011 CFR

    2011-07-01

    ... hydrochloride) in or on raw agricultural commodities as follows: Commodity Parts per million Apple 0.50 Apple, wet pomace 1.5 Grapefruit 1.5 Lemon 0.60 Lime 0.03 Nectarine 0.40 Orange 1.5 Peach 0.40 Pear...

  15. 21 CFR 522.536 - Detomidine hydrochloride injection.

    Code of Federal Regulations, 2010 CFR

    2010-04-01

    ... 21 Food and Drugs 6 2010-04-01 2010-04-01 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...

  16. 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...

  17. 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 SERVICES (CONTINUED) ANIMAL DRUGS, FEEDS, AND RELATED PRODUCTS IMPLANTATION OR INJECTABLE DOSAGE FORM...

  18. 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 FOR HUMAN CONSUMPTION (CONTINUED) SUBSTANCES GENERALLY RECOGNIZED AS SAFE Multiple Purpose...

  19. 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 FOR HUMAN CONSUMPTION (CONTINUED) SUBSTANCES GENERALLY RECOGNIZED AS SAFE Multiple Purpose...

  20. 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 FOR HUMAN CONSUMPTION (CONTINUED) SUBSTANCES GENERALLY RECOGNIZED AS SAFE Multiple Purpose...

  1. 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 FOR HUMAN CONSUMPTION (CONTINUED) SUBSTANCES GENERALLY RECOGNIZED AS SAFE Multiple Purpose...

  2. 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 182.1047 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) SUBSTANCES GENERALLY RECOGNIZED AS SAFE Multiple Purpose GRAS Food Substances § 182.1047 Glutamic...

  3. Anticancer phytochemical analogs 37: synthesis, characterization, molecular docking and cytotoxicity of novel plumbagin hydrazones against breast cancer cells.

    PubMed

    Dandawate, Prasad; Ahmad, Aamir; Deshpande, Jyoti; Swamy, K Venkateswara; Khan, Ejazuddin M; Khetmalas, Madhukar; Padhye, Subhash; Sarkar, Fazlul

    2014-07-01

    We have synthesized, structurally characterized and examined cytotoxicity of novel plumbagin hydrazones against estrogen and progesterone receptor positive (ER+/PR+) MCF-7 and triple negative MDA-MB-231 breast cancer cell lines in order to evaluate the potential of these novel phytochemical analogs. Compounds were docked into the protein cavity of p50-subunit of NF-?B protein revealing better fit and better binding energies than the parent plumbagin compound. This was also reflected in their superior cytotoxicities which were found to be mediated by inhibition of NF-?B expression. These compounds can provide a starting point for the development of novel drug molecules against triple negative breast cancers. PMID:24835626

  4. Stereoselective Alkylations of Chiral Nitro Imine and Nitro Hydrazone Dianions. Synthesis of Enantiomerically Enriched 3-Substituted 1-Nitrocyclohexenes†

    PubMed Central

    Denmark, Scott E.; Ares, Jeffrey J.

    2011-01-01

    Dianions of chiral nitro imines (generated by a combination of LDA and s-BuLi) underwent diastereoselective alkylation with methyl, butyl, isopropyl, allyl and methallyl iodides. In contrast to the behavior of simple metalloenamines, the most selective auxiliary contained no coordinating groups, but did possess a large steric difference between the two substituents. The yield and selectivity of the alkylations were improved by the addition of HMPA or DMPU. The use of (S)-1-naphthylethylamine as the auxiliary afforded the R absolute configuration of the alkylation products. This stereochemical outcome could be rationalized by simple steric approach controlled alkylation in a conformationally fixed, internally coordinated dianion. A SAMP nitro hydrazone gave poorer yields and selectivities. PMID:18855478

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

    PubMed Central

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

    2015-01-01

    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 = 10 μM in an assay with COS7-cell lysate overexpressing murine ATGL. PMID:25778769

  6. Stability of labetalol hydrochloride, metoprolol tartrate, verapamil hydrochloride, and spironolactone with hydrochlorothiazide in extemporaneously compounded oral liquids.

    PubMed

    Allen, L V; Erickson, M A

    1996-10-01

    The stability of drugs commonly prescribed for use in oral liquid dosage forms but not commercially available as such was studied. Labetalol hydrochloride 40 mg/mL, metoprolol tartrate 10 mg/mL, verapamil hydrochloride 50 mg/mL, and spironolactone 5 mg/mL plus hydrochlorothiazide 5 mg/ mL were prepared in a 1:1 mixture of Ora-Sweet and Ora-Plus (Paddock Laboratories), a 1:1 mixture of Ora-Sweet SF and Ora-Plus (Paddock Laboratories), and cherry syrup and placed in polyethylene terephthalate bottles. The sources of the drugs were tablets. Six bottles were prepared per liquid; three were stored at 5 degrees C and three at 25 degrees C, all in the dark. A sample was removed from each bottle initially and at intervals up to 60 days and analyzed for drug concentration by stability-indicating high-performance liquid chromatography. At least 91% of the initial drug concentration was retained in all the oral liquids for up to 60 days. There were no substantial changes in the appearance or odor of the liquids, or in the pH. Labetalol hydrochloride 40 mg/mL, metoprolol tartrate 10 mg/mL, verapamil hydrochloride 50 mg/mL, plus hydrochlorothiazide 5 mg/ mL in three oral liquids compounded extemporaneously from sweetened vehicles and tablets were stable for up to 60 days when stored without light at 5 and 25 degrees C. PMID:8893069

  7. 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

  8. 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···OC hydrogen bond occurring between the carbonyl (-CO) and the hydrazone -CN-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 C2O1 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

  9. 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

  10. 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.

  11. Effects of zilpaterol hydrochloride and zilpaterol hydrochloride withdrawal time on beef carcass cutability, composition, and tenderness.

    PubMed

    Shook, J N; VanOverbeke, D L; Kinman, L A; Krehbiel, C R; Holland, B P; Streeter, M N; Yates, D A; Hilton, G G

    2009-11-01

    The impact of zilpaterol hydrochloride (ZH) on carcass yield, composition, and tenderness was evaluated using 384 beef steers in a randomized complete block design. Main effects were the addition of 0 or 8.3 mg/kg of ZH for the final 20 d of feeding and each inclusion level was paired with withdrawal periods of 3, 10, 17, or 24 d. The 2 animals with BW closest to the pen average were selected for carcass fabrication to determine carcass yield, composition, and tenderness. The carcasses from animals fed ZH had greater (P = 0.008) individual side weights. Carcass fat determinations were unchanged (P = 0.70) by ZH. Weights of the strip loin (P = 0.01), peeled tenderloin (P = 0.02), and top sirloin butt (P < 0.001) were all improved with ZH. When expressed as a proportion of carcass weight, ZH increased percentage of carcass in the top sirloin butt (P = 0.006), bottom sirloin tri-tip (P = 0.02), top inside round (P = 0.002), bottom round flat (P = 0.001), and flank steak (P = 0.02). A longer withdrawal time (WT) increased (P < 0.001) carcass weights. Shoulder clod weights were greatest (P < 0.001) with 17-d WT from ZH, whereas chuck roll weights were greatest (P = 0.02) at 17 and 24 d of WT. Peeled tenderloins, top sirloin butts, and eye of rounds responded to WT, with increased (P < 0.001) weights seen at 10 d of WT as compared with all other WT. Shear force values were greater at each of the 3 aging times, 7 d (P < 0.001), 14 d (P < 0.001), and 21 d (P = 0.003), in steaks from ZH-fed steers compared with control steers. Protein percentages were greater in ZH steaks (P = 0.03) and ZH ground beef trim (P < 0.001). Percent moisture was increased (P < 0.001) in strip loin steaks at 3 and 10 d WT. Ground beef trim had an increase (P = 0.04) in percent moisture and a decrease (P = 0.01) in percent fat at 10 d WT. Carcass weights and yields were improved with ZH feeding and may continue to improve even up to 10 d after withdrawal of the supplement. Tenderness was slightly reduced with ZH supplementation but was unaffected by WT. Zilpaterol hydrochloride can be a valuable supplement to finishing beef steers to improve carcass lean yields and composition. PMID:19684279

  12. 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.

  13. 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.

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

    PubMed

    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. PMID:25594208

  15. 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

  16. Structural and vibrational study of 8-hydroxyquinoline-2-carboxaldehyde isonicotinoyl hydrazone - A potential metal-protein attenuating compound (MPAC) for the treatment of Alzheimer's disease

    NASA Astrophysics Data System (ADS)

    de Freitas, Leonardo Viana; da Silva, Cecilia C. P.; Ellena, Javier; Costa, Luiz Antônio Sodré; Rey, Nicolás A.

    2013-12-01

    A comprehensive structural and vibrational study of the potential metal-protein attenuating compound 8-hydroxyquinoline-2-carboxaldehyde isonicotinoyl hydrazone is reported. X-ray diffraction data, as well as FT-IR and Raman frequencies, were compared with the respective theoretical values obtained from DFT calculations. Theory agrees well with experiment. In this context, an attempt of total assignment concerning the FT-IR and Raman spectra of the title compound was performed, shedding new light on previous partial assignments published elsewhere.

  17. 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

  18. [Molecular imprinting-flow injection chemiluminescence method for determination of doxycycline hydrochloride].

    PubMed

    Zhou, Yan-Mei; Zhang, Cheng-Li; Lei, Jian-Du; Ma, Tong-Sen; Ma, Guang-Hui; Su, Zhi-Guo; Chao, Yang

    2009-07-01

    Doxycycline hydrochloride can enhance the chemiluminescence of potassium ferricyanide and luminol in alkaline medium. So a molecular imprinting-flow-injection chemiluminescence method for the determination of doxycycline hydrochloride was established by using doxycycline hydrochloride-imprinted polymers as recognition material and potassium ferricyanide and luminol as detection system. Doxycycline hydrochloride-imprinted polymer was synthesized using methacrylic acid as functional monomer and ethylene glycol dimethacrylate as cross-linker. The linear range is 9.0 x 10(-7)-6.0 x 10(-5) g x mL(-1) and the detection limit is 3.2 x 10(-7) g x mL(-1). The relative standard deviation for 6.0 X 10(-6) g x mL(-1) of doxycycline hydrochloride was 3.5% (n = 9). This method has been successfully applied to the determination of doxycycline hydrochloride in tablets and in urine samples. PMID:19798931

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

    PubMed

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

    2012-04-28

    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 T(g). 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 T(g). 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 between the Johari-Goldstein β-relaxation and the structural α-relaxation in non-ionic glass-forming systems. The novel features of the ionic conductivity relaxation are brought out by presenting the measurements in terms of the electric modulus or permittivity. If presented in terms of conductivity, the novel features are lost. This warns against insisting that a log-log plot of conductivity vs. frequency is optimal to reveal and interpret the dynamics of ionic conductors. PMID:22559496

  20. Olopatadine hydrochloride inhibits capsaicin-induced flare response in humans.

    PubMed

    Shindo, Masahisa; Yoshida, Yuichi; Yamamoto, Osamu

    2011-01-01

    Capsaicin, a vanilloid, has the potential for releasing substance P (SP) from sensory nerves. Topical application of capsaicin induces a flare response in the skin. However, it has not been clarified whether the release of SP is involved in the process of flare response or not. A potent antihistamine drug, olopatadine hydrochloride, is known to have inhibitory action against the release of SP. We examined the effects of olopatadine (at a dose of 5 mg) on skin reaction induced by topical application of capsaicin in 10 healthy subjects. The scores of capsaicin-induced flare responses after olopatadine administration were significantly lower at 30 min than at baseline. Our findings suggest that olopatadine hydrochloride could inhibit capsaicin-induced flare responses. PMID:21346393

  1. Visual colorimetric detection of berberine hydrochloride with silver nanoparticles.

    PubMed

    Ling, Jian; Sang, You; Huang, Cheng Zhi

    2008-08-01

    A visual colorimetric method for the detection of berberine hydrochloride was proposed in this contribution based on the color change caused by the aggregation of silver nanoparticles (AgNps). It was found that citrate-capped AgNps dispersed in water owing to the electrostatic repulsion from each other by the negative charged surface, presenting a bright yellow color. However, the presence of positively charged berberine could induce the aggregation of citrate-capped AgNps, resulting in color change from yellow to green and even to blue depending on the concentration of berberine. Under the optimum condition investigated with UV-vis absorption and light scattering technique, berberine hydrochloride from 0.05 micromol l(-1) to 0.4 micromol l(-1) could be visually detected based on the color alteration of the AgNps suspension. PMID:18513909

  2. 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

  3. Tumorigenic effect of 1-hydrazinophthalazine hydrochloride in mice.

    PubMed

    Toth, B

    1978-11-01

    A solution of 0.125% 1-hydrazinophthalazine hydrochloride, an antihypertensive drug widely used in humans, was given continuously in drinking water for the life-spans of randomly bred Swiss mice. Consumption of the chemical significantly increased the lung tumor incidence from 36 to 60% in females and from 26 to 46% in males, compared to controls. Histopathologically, the tumors were classified as adenomas and adenocarcinomas of the lungs. PMID:280718

  4. Stability of sotalol hydrochloride in extemporaneously prepared oral suspension formulations.

    PubMed

    Sidhom, Madiha B; Rivera, Nadya; Almoazen, Hassan; Taft, David R; Kirschenbaum, Harold L

    2005-01-01

    The physical, chemical, and microbial stabilities of extemporaneously compounded oral liquid formulations of sotalol hydrochloride were studied. Sotalol hydrochloride oral liquid suspensions (5mg/mL) were prepared from commercially available tablets (Betapace) in a 1:1 mixture of Ora-Plus: Ora-Sweet, a 1:1 mixture of Ora-Plus:Ora-Sweet SF, and a 1:2.4 mixture of simple syrup:methylcellulose vehicle. Six batches of each formulation were prepared; three were stored at refrigerated temperature (2 deg to 8 deg C) and three at room temperature (20 deg to 25 deg C). Samples were collected from each batch weekly for 6 weeks, and again at 12 weeks. Samples were analyzed by means of a high-performance liquid chromatographic method, and the concentrations obtained were compared to the theoretical time zero value. Samples were examined for pH, odor, color, and consistency changes. The suspensions also were evaluated for their microbial stability. Sotalol hydrochloride oral liquid suspensions (5mg/mL) were chemically stable for 12 weeks regardless of storage conditions (room temperature or refrigerated). Bacterial growth was not supported by any of the formulations. Suspensions stored at refrigerated temperature retained better physical quality (e.g., odor, color, and consistency) than suspensions stored at room temperature. Overall, this study demonstrates that oral formulations of sotalol hydrochloride can be readily prepared with commercially available vehicles. The method of preparation is relatively simple, the materials are relatively inexpensive, and the products have a shelf-life of at least 12 weeks. PMID:23925139

  5. Neuroleptic malignant syndrome possibly caused by molindone hydrochloride.

    PubMed

    Gradon, J D

    1991-10-01

    The case of a patient who developed neuroleptic malignant syndrome (NMS) on three separate occasions is presented. Her third bout of this syndrome possibly was caused by molindone hydrochloride. This medication has been reported only once previously to cause NMS. The pharmacology of molindone is reviewed and a complicating factor in this case--the recent onset of hypothyroidism--is discussed together with its implication in the development of the clinical manifestations of this syndrome. PMID:1803792

  6. 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 4at 100?M and 250?M concentration respectively. Tetracycline hydrochloride has also protected bovine serum albumin (BSA) from radiation induced degradation. The exvivo 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 9Gy. This study demonstrates the radioprotective potential of the drug by providing some insight into exvivo and invivo efficacy. PMID:26763761

  7. 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).

  8. Psychosedation with dexmedetomidine hydrochloride during minor oral surgery.

    PubMed

    Taniyama, Kiichi; Oda, Hideki; Okawa, Kazuko; Himeno, Katsuhito; Shikanai, Koki; Shibutani, Tohru

    2009-01-01

    We performed intravenous sedation with dexmedetomidine hydrochloride during minor oral surgery and compared this agent with propofol. Patients were randomly divided into 2 groups: dexmedetomidine hydrochloride (D) and propofol (P) groups. In Group D, systolic blood pressure (SBP) increased immediately after the start of initial loading, although no significant differences were noted. Both SBP and diastolic blood pressure (DBP) gradually decreased during maintenance administration and were significantly lower than pretreatment values. The heart rate decreased immediately after the start of administration and was significantly lower during both initial loading and maintenance administration; the heart rate was also significantly lower than that in Group P. In Group D, arterial blood oxygen saturation (SpO2) significantly decreased after the sedation level reached an optimum level until the end of administration. The bispectral index (BIS) value gradually decreased during initial loading. At the optimal sedation level, it decreased to 80 to 85. During maintenance administration, marked changes were observed in this parameter. No marked differences in amnestic effects and comfort were noted between the 2 groups. If the sedation level can be evaluated accurately via another objective method, intravenous sedation with dexmedetomidine hydrochloride may be useful in dental treatment. PMID:19769420

  9. 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. PMID:25097652

  10. The Cytotoxicity of Benzaldehyde Nitrogen Mustard-2-Pyridine Carboxylic Acid Hydrazone Being Involved in Topoisomerase II? 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??M , HCT-116: 57.5 5.3??M, K562: 48.2 4.0??M, and PC-12: 19.4 2.2??M) 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 II?. Those revealed that the cytotoxic mechanism of the BNMPH could stem from both the topoisomerase II inhibition, ROS generation and DNA alkylation. PMID:24995306

  11. 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

  12. 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.

  13. 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.

  14. 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

  15. New acyclic 1,2,4-triazole-based Schiff base hydrazone: Synthesis, characterization, spectrophotometric and computational studies

    NASA Astrophysics Data System (ADS)

    Khanmohammadi, Hamid; Erfantalab, Malihe; Azimi, Golamhassan

    2013-03-01

    A new 1,2,4-triazole-based Schiff base hydrazone with N, O, S donor set of atoms, H4L, has been prepared by condensation reaction of N,N'-bis(3-formyl-5-methylsalicylidene)ethane-1,2-diamine, H2L, with 4-amino-3-(4-pyridyl)-5-mercapto-1,2,4-triazole. The structure of H4L was characterized by using FT-IR, UV-Vis and 1H NMR spectroscopic methods as well as elemental analysis data. The formation constants of copper(II), cadmium(II), mercury(II) and silver(I) complexes of H4L in DMSO were calculated using a hard model chemometrics method applying the spectrophotometric data. The protonation constants of H4L were also measured in DMSO-water (1:10) mixture. Furthermore, 1H chemical shifts of H4L were studied by the gauge independent atomic orbital (GIAO) and continuous set of gauge transformations (CSGTs) methods at the level of density functional theory using B3LYP/6-311++G* basis sets in gas phase. The computed chemical shifts are in reasonably good agreement with the experimental data.

  16. 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.

  17. 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

  18. New acyclic 1,2,4-triazole-based Schiff base hydrazone: synthesis, characterization, spectrophotometric and computational studies.

    PubMed

    Khanmohammadi, Hamid; Erfantalab, Malihe; Azimi, Golamhassan

    2013-03-15

    A new 1,2,4-triazole-based Schiff base hydrazone with N, O, S donor set of atoms, H(4)L, has been prepared by condensation reaction of N,N'-bis(3-formyl-5-methylsalicylidene)ethane-1,2-diamine, H(2)L, with 4-amino-3-(4-pyridyl)-5-mercapto-1,2,4-triazole. The structure of H(4)L was characterized by using FT-IR, UV-Vis and (1)H NMR spectroscopic methods as well as elemental analysis data. The formation constants of copper(II), cadmium(II), mercury(II) and silver(I) complexes of H(4)L in DMSO were calculated using a hard model chemometrics method applying the spectrophotometric data. The protonation constants of H(4)L were also measured in DMSO-water (1:10) mixture. Furthermore, (1)H chemical shifts of H(4)L were studied by the gauge independent atomic orbital (GIAO) and continuous set of gauge transformations (CSGTs) methods at the level of density functional theory using B3LYP/6-311++G(*) basis sets in gas phase. The computed chemical shifts are in reasonably good agreement with the experimental data. PMID:23321219

  19. [Characterization of collagen of canine intervertebral disks using the N-methyl-benzothiazol-2-on-hydrazone reaction].

    PubMed

    Silva, N; Farias, G; Torres, J M

    1991-06-01

    Collagen types were studied in the lumbar intervertebral discs of non-chondrodystrophic dogs, 1 to 3 years old. Parts of intervertebral discs were frozen and sections were subjected to the 3-methyl-benzothiazol-2-on-hydrazone (MBTH) method, which permits differentiation of genetic types and maturation stages of collagen. The annulus fibrosus showed a blue (collagen I) and a violet colour (collagen II) at the external zone. The internal zone was more homogeneous and contained a mixture of both colours (collagen I and II). The nucleus pulposus showed only the violet colour, indicative of collagen II. Discs were also dissected at three different zones and submitted to an extraction technique to obtain collagen, then subjected to SDS-polyacrylamide gel electrophoresis and determination of spectrophotometric reactions of MBTH. Both studies demonstrated type I and type II collagens in the external and internal zones of the annulus fibrosus, but only type II in the nucleus pulposus. Collagen characterization, using this technique, would allow for evaluation in pathologic events of the intervertebral discs as well as for establishing the degree of alteration. PMID:1716811

  20. 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.

  1. 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

  2. 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 ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL DRUGS, FEEDS, AND RELATED PRODUCTS..., tetracaine hydrochloride ear ointment. (a) Specifications. The product contains 5 milligrams of...

  3. 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 ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL DRUGS, FEEDS, AND RELATED PRODUCTS..., tetracaine hydrochloride ear ointment. (a) Specifications. The product contains 5 milligrams of...

  4. 76 FR 53907 - Determination That TALWIN COMPOUND (Aspirin; Pentazocine Hydrochloride) Tablets, 325 Milligrams...

    Federal Register 2010, 2011, 2012, 2013, 2014

    2011-08-30

    ... Hydrochloride) Tablets, 325 Milligrams; Equivalent to 12.5 Milligram Base, Were Not Withdrawn From Sale for... hydrochloride (HCl)) tablets, 325 milligrams (mg); equivalent to (EQ) 12.5 mg base, were not withdrawn from sale.... The 1984 amendments include what is now section 505(j)(7) of the Federal Food, Drug, and Cosmetic...

  5. 21 CFR 520.1263 - Lincomycin hydrochloride monohydrate oral dosage forms.

    Code of Federal Regulations, 2011 CFR

    2011-04-01

    ... 21 Food and Drugs 6 2011-04-01 2011-04-01 false Lincomycin hydrochloride monohydrate oral dosage forms. 520.1263 Section 520.1263 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND... § 520.1263 Lincomycin hydrochloride monohydrate oral dosage forms....

  6. 21 CFR 520.1263 - Lincomycin hydrochloride monohydrate oral dosage forms.

    Code of Federal Regulations, 2010 CFR

    2010-04-01

    ... 21 Food and Drugs 6 2010-04-01 2010-04-01 false Lincomycin hydrochloride monohydrate oral dosage forms. 520.1263 Section 520.1263 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND... § 520.1263 Lincomycin hydrochloride monohydrate oral dosage forms....

  7. 21 CFR 520.1263 - Lincomycin hydrochloride monohydrate oral dosage forms.

    Code of Federal Regulations, 2012 CFR

    2012-04-01

    ... 21 Food and Drugs 6 2012-04-01 2012-04-01 false Lincomycin hydrochloride monohydrate oral dosage forms. 520.1263 Section 520.1263 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND... § 520.1263 Lincomycin hydrochloride monohydrate oral dosage forms....

  8. 21 CFR 522.1662 - Oxytetracycline hydrochloride implantation or injectable dosage forms.

    Code of Federal Regulations, 2013 CFR

    2013-04-01

    ... 21 Food and Drugs 6 2013-04-01 2013-04-01 false Oxytetracycline hydrochloride implantation or... HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL DRUGS, FEEDS, AND RELATED PRODUCTS IMPLANTATION OR INJECTABLE DOSAGE FORM NEW ANIMAL DRUGS § 522.1662 Oxytetracycline hydrochloride implantation or...

  9. 21 CFR 522.1662 - Oxytetracycline hydrochloride implantation or injectable dosage forms.

    Code of Federal Regulations, 2012 CFR

    2012-04-01

    ... 21 Food and Drugs 6 2012-04-01 2012-04-01 false Oxytetracycline hydrochloride implantation or... HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL DRUGS, FEEDS, AND RELATED PRODUCTS IMPLANTATION OR INJECTABLE DOSAGE FORM NEW ANIMAL DRUGS § 522.1662 Oxytetracycline hydrochloride implantation or...

  10. 21 CFR 522.1662 - Oxytetracycline hydrochloride implantation or injectable dosage forms.

    Code of Federal Regulations, 2014 CFR

    2014-04-01

    ... 21 Food and Drugs 6 2014-04-01 2014-04-01 false Oxytetracycline hydrochloride implantation or... HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL DRUGS, FEEDS, AND RELATED PRODUCTS IMPLANTATION OR INJECTABLE DOSAGE FORM NEW ANIMAL DRUGS § 522.1662 Oxytetracycline hydrochloride implantation or...

  11. 21 CFR 522.1662 - Oxytetracycline hydrochloride implantation or injectable dosage forms.

    Code of Federal Regulations, 2011 CFR

    2011-04-01

    ... 21 Food and Drugs 6 2011-04-01 2011-04-01 false Oxytetracycline hydrochloride implantation or... HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL DRUGS, FEEDS, AND RELATED PRODUCTS IMPLANTATION OR INJECTABLE DOSAGE FORM NEW ANIMAL DRUGS § 522.1662 Oxytetracycline hydrochloride implantation or...

  12. 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...; penicillin G potassium, USP; and tetracycline hydrochloride soluble powders administered in drinking water... ANADA 200-347 for Penicillin G Potassium, USP, all soluble powders administered in drinking water to...

  13. 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

  14. 21 CFR 524.1662a - Oxytetracycline hydrochloride and hydrocortisone spray.

    Code of Federal Regulations, 2010 CFR

    2010-04-01

    ... spray. 524.1662a Section 524.1662a Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND... NEW ANIMAL DRUGS § 524.1662a Oxytetracycline hydrochloride and hydrocortisone spray. (a) Specifications. Each 3-ounce unit of oxytetracycline hydrochloride and hydrocortisone spray contains...

  15. 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...

  16. 21 CFR 524.1662 - Oxytetracycline hydrochloride ophthalmic and topical dosage forms.

    Code of Federal Regulations, 2011 CFR

    2011-04-01

    ... 21 Food and Drugs 6 2011-04-01 2011-04-01 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....

  17. 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....

  18. 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

    ... 40 Protection of Environment 11 2011-07-01 2011-07-01 false Free Formaldehyde Analysis of Insulation Resins by Hydroxylamine Hydrochloride B Appendix B to Subpart NNN of Part 63 Protection of...—Free Formaldehyde Analysis of Insulation Resins by Hydroxylamine Hydrochloride 1. Scope This method...

  19. 78 FR 16685 - Impax Laboratories, Inc.; Withdrawal of Approval of Bupropion Hydrochloride Extended-Release...

    Federal Register 2010, 2011, 2012, 2013, 2014

    2013-03-18

    ... Bupropion Hydrochloride Extended-Release Tablets, 300 Milligrams AGENCY: Food and Drug Administration, HHS... Hydrochloride (HCl) Extended-Release Tablets, 300 Milligrams (mg) (Bupropion HCl Extended-Release Tablets 300 mg... Extended-Release Tablets 300 mg (marketed under the name BUDEPRION XL) on December 15, 2006 pursuant...

  20. 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... HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL DRUGS, FEEDS, AND RELATED PRODUCTS IMPLANTATION OR INJECTABLE DOSAGE FORM NEW ANIMAL DRUGS § 522.1662 Oxytetracycline hydrochloride implantation or...

  1. 40 CFR 721.1075 - Benzenamine, 4-(1-methyl-bu-toxy)-, hydrochloride.

    Code of Federal Regulations, 2011 CFR

    2011-07-01

    ... 40 Protection of Environment 31 2011-07-01 2011-07-01 false Benzenamine, 4-(1-methyl-bu-toxy)-, hydrochloride. 721.1075 Section 721.1075 Protection of Environment ENVIRONMENTAL PROTECTION AGENCY (CONTINUED... Specific Chemical Substances § 721.1075 Benzenamine, 4-(1-methyl-bu-toxy)-, hydrochloride. (a)...

  2. 40 CFR 721.1075 - Benzenamine, 4-(1-methyl-bu-toxy)-, hydrochloride.

    Code of Federal Regulations, 2010 CFR

    2010-07-01

    ... 40 Protection of Environment 30 2010-07-01 2010-07-01 false Benzenamine, 4-(1-methyl-bu-toxy)-, hydrochloride. 721.1075 Section 721.1075 Protection of Environment ENVIRONMENTAL PROTECTION AGENCY (CONTINUED... Specific Chemical Substances § 721.1075 Benzenamine, 4-(1-methyl-bu-toxy)-, hydrochloride. (a)...

  3. 78 FR 27971 - Determination That REV-EYES (Dapiprazole Hydrochloride Ophthalmic Solution), 0.5%, Was Not...

    Federal Register 2010, 2011, 2012, 2013, 2014

    2013-05-13

    ... HUMAN SERVICES Food and Drug Administration Determination That REV-EYES (Dapiprazole Hydrochloride... determined that REV-EYES (dapiprazole hydrochloride ophthalmic solution), 0.5%, was not withdrawn from sale... refer to a listed drug. REV-EYES (dapiprazole hydrochloride ophthalmic solution), 0.5%, is the...

  4. 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

  5. Colorimetric determination of tetracycline hydrochloride in pharmaceutical preparations.

    PubMed

    Saha, U

    1987-01-01

    A simple, sensitive, and rapid colorimetric method is presented for the estimation of tetracycline hydrochloride as the pure drug and in formulations. The proposed method is based on the reaction of tetracycline HCl with cupric chloride in an alkaline medium to give a yellowish green solution whose absorbance is measured at 400 nm against a reagent blank. The color obeys Beer's law in the concentration range of 0-20 micrograms/mL. Molar absorptivity and Sandell's sensitivity of the yellowish-green copper complexes of tetracycline HCl are 1.99 X 10(4) L X mol-1 X cm-1 and 0.0241 ppm, respectively. PMID:3624177

  6. Sustaining pattern of phenformin hydrochloride using various polymers and waxes.

    PubMed

    Pandey, V P; Kannappan, N; Manavalan, R; Subburaj, T

    2002-01-01

    The present study was carried out to formulate matrix tablets of phenformin hydrochloride. Granules of phenformin HCl were prepared by using ethyl cellulose, eudragit RS 100, gum acacia, carnauba wax, stearyl alcohol, glyceryl monostearate and triethanol amine. Thus the granules were compressed and fourteen tablets formulations were prepared. All the physical parameters of granules and matrix tablets were studied including compatibility study. One commercial timed disintegration capsule was also included for study and comparison. The results of in vitro studies showed that sustained release matrix tablet might be prepared using carnauba wax, stearyl alcohol, triethanol amine and magnesium stearate. PMID:12481378

  7. 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.

  8. 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

  9. The antitumor mechanism of di-2-pyridylketone 2-pyridine carboxylic acid hydrazone and its copper complex in ROS generation and topoisomerase inhibition, and hydrazone involvement in oxygen-catalytic iron mobilization.

    PubMed

    Huang, Tengfei; Li, Cuiping; Sun, Xingzhi; Zhu, Zhenfu; Fu, Yun; Liu, Youxun; Yuan, Yanbin; Li, Shaoshan; Li, Changzheng

    2015-11-01

    Iron depletion and stimulation of iron-dependent free radical damage is a rapidly developing field for chelation therapy, but the iron mobilization from ferritin by chelators has received less attention. In this study, the di-2-pyridylketone 2-pyridine carboxylic acid hydrazone (DPPCAH) and its copper complex was prepared and characterized by NMR and MS spectra. The proliferation inhibition assay showed that both DPPCAH and its copper complex exhibited selectively proliferation inhibition for HepG2 (IC50, 4.6 ± 0.2 µM for DPPACH and 1.3 ± 0.2 µM for its copper complex), but less inhibition for HCT-116 cell line (IC50, >100 µM for DPPACH and 7.8 ± 0.4 µM for its copper complex). The mechanistic studies revealed that DPPACH could remove iron from ferritin in a oxygen-catalytic manner, and contributed to redox activity of labile iron pool (LIP), that is less reported for the chelators that possess significant biological activity. The reactive oxygen species (ROS) generation and DNA cleavage assay in vitro and in vivo showed that both DPPACH-Fe(II) and DPPACH-Cu were redox-active species, indicating that ROS may mediate their antitumor activity. Further study revealed that both DPPACH and its copper complex displayed certain degree of inhibition of type II topoisomerase (Top) which contributed to their antitumor activity. Thus, the mechanism that iron mobilization by DPPACH from ferritin contributed to LIP was proposed, and both DPPACH and its copper complex were involved in ROS generation and Top II inhibition for their antitumor activities. PMID:26398524

  10. 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

  11. Formulation and evaluation of effervescent floating tablets of tizanidine hydrochloride.

    PubMed

    Someshwar, Komuravelly; Chithaluru, Kalyani; Ramarao, Tadikonda; Kumar, K K Kalyan

    2011-06-01

    Tizanidine hydrochloride is an orally administered prokinetic agent that facilitates or restores motility through-out the length of the gastrointestinal tract. The objective of the present investigation was to develop effervescent floating matrix tablets of tizanidine hydrochloride for prolongation of gastric residence time in order to overcome its low bioavailability (34-40 %) and short biological half life (4.2 h). Tablets were prepared by the direct compression method, using different viscosity grades of hydroxypropyl methylcellulose (HPMC K4M, K15M and K100M). Tablets were evaluated for various physical parameters and floating properties. Further, tablets were studied for in vitro drug release characteristics in 12 hours. Drug release from effervescent floating matrix tablets was sustained over 12 h with buoyant properties. DSC study revealed that there is no drug excipient interaction. Based on the release kinetics, all formulations best fitted the Higuchi, first-order model and non-Fickian as the mechanism of drug release. Optimized formulation (F9) was selected based on the similarity factor (f2) (74.2), dissolution efficiency at 2, 6 and 8 h, and t50 (5.4 h) and was used in radiographic studies by incorporating BaSO4. In vivo X-ray studies in human volunteers showed that the mean gastric residence time was 6.2 ± 0.2 h. PMID:21684848

  12. Transepithelial transport of biperiden hydrochloride in Caco-2 cell monolayers.

    PubMed

    Abalos, Ivana S; Rodríguez, Yanina I; Lozano, Verónica; Cereseto, Marina; Mussini, Maria V; Spinetto, Marta E; Chiale, Carlos; Pesce, Guido

    2012-09-01

    The aim of this research has been to determine the biperiden hydrochloride permeability in Caco-2 model, in order to classify it based on the Biopharmaceutics Classification System (BCS). The World Health Organization (WHO) as well as many other authors have provisionally assigned the drug as BCS class I (high solubility-high permeability) or III (high solubility-low permeability), based on different methods. We determined biperiden BCS class by comparing its permeability to 5 pre-defined compounds: atenolol and ranitidine hydrochloride (low permeability group) and metoprolol tartrate, sodium naproxen and theophylline (high permeability group). Since biperiden permeability was higher than those obtained for high permeability drugs, we classified it as a BCS class I compound. On the other hand, as no differences were obtained for permeability values when apical to basolateral and basolateral to apical fluxes were studied, this drug cannot act as a substrate of efflux transporters. As a consequence of our results, we suggest that the widely used antiparkinsonian drug, biperiden, should be candidate for a waiver of in vivo bioequivalence studies. PMID:22554863

  13. [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

  14. 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

  15. 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

  16. Effect of tolazoline hydrochloride on sputum viscosity in cystic fibrosis

    PubMed Central

    Feather, Elizabeth A.; Russell, George

    1970-01-01

    Comparisons have been made between the effects of autonomic dysfunction and the pathophysiological changes in the exocrine secretions from patients with cystic fibrosis (Roberts, 1959). Cotton (1966) found that administration of tolazoline hydrochloride (an alpha-adrenergic blocker) to patients with cor pulmonale in the terminal stages of cystic fibrosis was associated with an improvement in the results of their lung function tests. This effect might have been due to an alteration of the abnormal viscosity of the bronchial mucus mediated via the autonomic nervous system, thus permitting easier expectoration. Measurement, by means of a Ferranti-Shirely cone and plate viscometer, of several different aspects of sputum viscosity is described. Tolazoline hydrochloride, administered to five patients with cystic fibrosis, was shown not to differ significantly from a placebo in its effect on sputum viscosity and dynamic lung volumes. We could not relate the improved lung function seen in Cotton's series to an autonomic effect of the drug on the physical properties of bronchial mucus in this condition. PMID:5494682

  17. 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

  18. Formulation and Evaluation of Tramadol hydrochloride Rectal Suppositories.

    PubMed

    Saleem, M A; Taher, M; Sanaullah, S; Najmuddin, M; Ali, Javed; Humaira, S; Roshan, S

    2008-09-01

    Rectal suppositories of tramadol hydrochloride were prepared using different bases and polymers like PEG, cocoa butter, agar and the effect of different additives on in vitro release of tramadol hydrochloride was studied. The agar-based suppositories were non-disintegrating/non-dissolving, whereas PEGs were disintegrating/dissolving and cocoa butter were melting suppositories. All the prepared suppositories were evaluated for various physical parameters like weight variation, drug content and hardness. The PEG and cocoa butter suppositories were evaluated for macromelting range, disintegration and liquefaction time. In vitro release study was performed by USP type I apparatus. The prepared suppositories were within the permissible range of all physical parameters. In vitro drug release was in the order of PEG>Agar>cocoa butter. Addition of PVP, HPMC in agar suppositories retards the release. The mechanism of drug release was diffusion controlled and follows first order kinetics. The results suggested that blends of PEG of low molecular weight (1000) with high molecular weight (4000 and 6000) in different percentage and agar in 10% w/w as base used to formulate rapid release suppositories. The sustained release suppositories can be prepared by addition of PVP, HPMC in agar-based suppositories and by use of cocoa butter as base. PMID:21394263

  19. Pyridine-Hydrazones as N,N'-Ligands in Asymmetric Catalysis: Pd(II)-Catalyzed Addition of Boronic Acids to Cyclic Sulfonylketimines.

    PubMed

    lvarez-Casao, Yolanda; Monge, David; lvarez, Eleuterio; Fernndez, Rosario; Lassaletta, Jos M

    2015-10-16

    The design, synthesis, and coordination features of a novel class of chiral pyridine-hydrazone ligands are described. As a first application, L/Pd(TFA)2 complexes served as catalysts in the 1,2-addition of arylboronic acids to saccharin-derived cyclic ketimines, affording products in high yields and enantioselectivities. The method was also applied to more challenging 3,4-disubstituted 1,2,5-thiadiazole 1,1-dioxides, affording again high yields and enantioselectivities along with high regioselectivities for unsymmetrically substituted derivatives. PMID:26425892

  20. 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.

  1. Synthesis, antioxidant, anticancer and antiviral activities of novel quinoxaline hydrazone derivatives and their acyclic C-nucleosides.

    PubMed

    El-Tombary, Alaa A; El-Hawash, Soad A M

    2014-01-01

    The present investigation describes the synthesis of a new series of aldehydo-sugar-N-(3-phenylquinoxalin-2- yl)hydrazones 3a-d and their acyclic C-nucleoside analogs, 1-(4-phenyl-[1,2,4]triazolo[4,3-a]quinoxalin-1-yl)alditols 7ad by using 2-hydrazino-3-phenylquinoxaline 1 as key intermediate. The synthesized compounds were screened for their antioxidant activities by 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) radical cation scavenging method. Compounds 3d and 7a, showed potent scavenging activities against ABTS(+) radicals and were found to be the most potent antioxidants described in this study. Out of the synthesized compounds, compounds 3d and 7a were selected by the National Cancer Institute for evaluation of their in vitro anticancer activity. Results revealed that compounds 3d and 7a exhibited non-selective broad spectrum activity against all cancer cell lines between 10(-6) to 10(-5) molar concentrations. Compound 3d showed the highest sensitivity against leukemia cell line HL-60 (TB) with GI50 of 5.15 µM, while compound 7a showed the highest sensitivity against ovarian cancer cell lines IGROV1 and OVCAR-4 with GI50 of 14.5 and 16.0 μM, respectively. In addition, compounds 3d and 7a showed TGI values of 72.2 and 96.3 µM, respectively against ovarian cancer cell line OVCAR-4. Furthermore, the target compounds were tested for antiviral activity against Herpes Simplex virus type-1 (HSV-1) using plaque reduction infectivity assay. The results indicated that compounds 3a-d and 7a exhibited very weak antiviral activity in comparison to Aphidicolin as a positive control. PMID:24151878

  2. Neuroprotective effect of penehyclidine hydrochloride on focal cerebral ischemia-reperfusion injury★

    PubMed Central

    Yu, Cuicui; Wang, Junke

    2013-01-01

    Penehyclidine hydrochloride can promote microcirculation and reduce vascular permeability. However, the role of penehyclidine hydrochloride in cerebral ischemia-reperfusion injury remains unclear. In this study, in vivo middle cerebral artery occlusion models were established in experimental rats, and penehyclidine hydrochloride pretreatment was given via intravenous injection prior to model establishment. Tetrazolium chloride, terminal deoxynucleotidyl transferase-mediated deoxyuridine triphosphate-biotin nick end labeling and immunohistochemical staining showed that, penehyclidine hydrochloride pretreatment markedly attenuated neuronal histopathological changes in the cortex, hippocampus and striatum, reduced infarction size, increased the expression level of Bcl-2, decreased the expression level of caspase-3, and inhibited neuronal apoptosis in rats with cerebral ischemia-reperfusion injury. Xanthine oxidase and thiobarbituric acid chromogenic results showed that penehyclidine hydrochloride upregulated the activity of superoxide dismutase and downregulated the concentration of malondialdehyde in the ischemic cerebral cortex and hippocampus, as well as reduced the concentration of extracellular excitatory amino acids in rats with cerebral ischemia-reperfusion injury. In addition, penehyclidine hydrochloride inhibited the expression level of the NR1 subunit in hippocampal nerve cells in vitro following oxygen-glucose deprivation, as detected by PCR. Experimental findings indicate that penehyclidine hydrochloride attenuates neuronal apoptosis and oxidative stress injury after focal cerebral ischemia-reperfusion, thus exerting a neuroprotective effect. PMID:25206707

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

    NASA Astrophysics Data System (ADS)

    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.

  4. 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

  5. [Pharmacological effects of nalfurafine hydrochloride, a kappa-opioid receptor agonist].

    PubMed

    Nakao, Kaoru; Hasebe, Ko; Yoshikawa, Satoru; Ikeda, Ken; Hirakata, Mikito; Miyamoto, Yohei; Mochizuki, Hidenori

    2010-11-01

    Nalfurafine hydrochloride, a kappa-opioid receptor agonist, was approved in January 2009 and released to the market on March 2009 for the indication of "Improvement of pruritus in hemodialysis patients (only for cases resistant to conventional treatments)" in Japan (Brand Name: REMITCH CAPSULES 2.5 microg, Marketing Authorization Holder: Toray Industries, Inc., Distributed by Torii Pharmaceutical Co., Ltd., Co-developed by Japan Tobacco Inc.). In addition to antipruritic effect, nalfurafine hydrochloride showed ameliorating effects on pain, neuropathic pain, drug dependence, schizophrenia and dyskinesia in non-clinical studies. Therefore, nalfurafine hydrochloride may become a useful therapeutic agent for their diseases. PMID:21226314

  6. 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

  7. 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

  8. 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

  9. Double emulsion templated monodisperse phospholipid liposomes incorporating Doxorubicin hydrochloride

    NASA Astrophysics Data System (ADS)

    Hai, Mingtan; Weitz, David

    2012-02-01

    We present a novel approach for fabricating monodisperse phospholipid liposomes incorporating water soluble anticancer drug Doxorubicin hydrochloride using controlled w/o/w double emulsions as templates. Glass-capillary microfluidics is used to generate monodisperse w/o/w double emulsion templates and double emulsion droplet size is from 20 to 100 um according to different flow rates. We show that the high uniformity in size and shape of the templates are maintained in the final phospholipid liposomes after a solvent removal step by Nikon eclipse microscopy. The lipid bilayers encapsulating anticancer drug inside is retained after the emulsion drops are converted to vesicles. The liposomes vesicles are promising water soluble anticancer drug delivery vehicles.

  10. [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

  11. 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.

  12. Molindone hydrochloride: a review of laboratory and clinical findings.

    PubMed

    Owen, R R; Cole, J O

    1989-08-01

    Molindone hydrochloride, a dihydroindolone neuroleptic, is structurally distinct from other classes of neuroleptics. Molindone exhibits many similarities to other neuroleptics, including dopamine receptor blockade, antipsychotic efficacy, and extrapyramidal side effects. Despite these similarities, molindone also has atypical properties and inhibits the enzyme monoamine oxidase in vitro and in vivo. Several studies have shown that molindone causes less dopamine receptor supersensitivity than other neuroleptics and thus may be less likely to cause tardive dyskinesia. It also appears to have a greater effect on mesolimbic and mesocortical dopamine neurons than on those in the nigrostriatal dopamine system. Clinically, molindone has a tendency to cause weight loss and may have less effect on seizure threshold than conventional antipsychotic agents. The authors review the laboratory and clinical data on molindone and discuss the relevance of atypical research findings to the clinical characteristics of this antipsychotic agent. PMID:2671060

  13. 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

  14. 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

  15. Instability of the hydrochloride salts of cathinone derivatives in air.

    PubMed

    Tsujikawa, Kenji; Yamamuro, Tadashi; Kuwayama, Kenji; Kanamori, Tatsuyuki; Iwata, Yuko T; Inoue, Hiroyuki

    2015-03-01

    We observed the decomposition of the hydrochloride salt of α-pyrrolidinoheptanophenone (α-PHPP-HCl), a newly distributed pyrrolidine-type cathinone derivative when 2.5ng of this substance was placed in glass test tubes and stored in a refrigerator for 3 days. To further investigate this phenomenon, we studied the (i) time course of the residual ratios of α-PHPP-HCl when a small amount (10μg) of α-PHPP-HCl was stored in glass vials in air at room temperature; (ii) identification of the decomposition products of α-PHPP-HCl; (iii) effect of air on the decomposition process; (iv) effect of the added amounts of α-PHPP-HCl on its decomposition; and (v) comparison of the stability between various cathinone derivatives and their decomposition products. The decomposition of α-PHPP-HCl occurred in air and increased with time. Two possible decomposition products, α-(2″-oxopyrrolidino)heptanophenone and α-PHPP-N-oxide, were identified. These products were formed by oxygen in air because the yield significantly decreased by storing them in a vacuum desiccator. With the decrease in the amount of α-PHPP-HCl, the residual ratios decreased and amount of the decomposition products increased. This indicates that the decomposition of α-PHPP-HCl occurred on the upper surface of the samples. The hydrochloride salts of other cathinone derivatives were also unstable in air, and the residual ratios observed were different depending on the compounds. The pyrrolidine-type cathinone derivatives afforded two types of decomposition products, which were presumed to be 2″-oxo and N-oxide derivatives, similar to α-PHPP-HCl. In contrast, secondary amine-type cathinone derivatives showed different decomposition patterns, possibly including the dealkylated derivative. These findings may be very useful for the future toxicological analysis of cathinone derivatives. PMID:25594691

  16. [Identification of the related substances in fasudil hydrochloride with hyphenated techniques].

    PubMed

    Chen, Yue-Qin; Song, Min; Hang, Tai-Jun

    2013-03-01

    The study aims to identify the related substances in fasudil hydrochloride by hyphenated techniques. A WondaSil C18 (250 mm x 4.6 mm, 5 microm) column was used for the separation of the related substances with a mixture of methanol and ammonium acetate buffer solution as the mobile phase by gradient elution. The structures of the related substances were speculated by electrospray positive ionization LC-TOF/MS accurate ion mass and MS/MS determination and elucidation, and verified further through synthesis and spectroscopic analysis. Fasudil hydrochloride and the related substances were separated under the established HPLC condition. Three related substances in fasudil hydrochloride were characterized by hyphenated techniques. The hyphenated LC-MS method is useful for the identification of related substances in fasudil hydrochloride and the results obtained are valuable for its manufacturing process and quality control. PMID:23724655

  17. 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

  18. Effect of tetracycline hydrochloride treatment on the critical thermal maximum of common shiners

    SciTech Connect

    Not Available

    1980-01-01

    The transfer of fish from field to laboratory facilities or their propagation in closed or restricted systems frequently results in bacterial infection and ultimately large-scale mortality. In attemps to alleviate this problem, we have added tetracycline hydrochloride to the water prophylactically (pretreating tanks before wild fish were added) and therapeutically (treating tanks after bacterial outbreaks were detected.) In the present study, we examined the effect of tetracyline hydrochloride on the critical thermal maximum (CTM) of the common shiner (Notropis cornutus).

  19. Effects of olopatadine hydrochloride, a histamine h(1) receptor antagonist, on histamine-induced skin responses.

    PubMed

    Hashimoto, Takashi; Ishii, Norito; Hamada, Takahiro; Dainichi, Teruki; Karashima, Tadashi; Nakama, Takekuni; Yasumoto, Shinichiro

    2010-01-01

    Effects of olopatadine hydrochloride, a histamine H(1) 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

  20. 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.

  1. Synthesis of imidazol-1-yl-acetic acid hydrochloride: a key intermediate for zoledronic acid.

    PubMed

    Singh, Santosh Kumar; Manne, Narendra; Ray, Purna Chandra; Pal, Manojit

    2008-01-01

    A convenient and practical synthesis of imidazol-1-yl-acetic acid hydrochloride was achieved via N-alkylation of imidazole using tert-butyl chloroacetate followed by a non-aqueous ester cleavage of the resulting imidazol-1-yl-acetic acid tert-butyl ester in the presence of titanium tetrachloride. The synthesized imidazol-1-yl-acetic acid hydrochloride was then utilized to prepare zoledronic acid. PMID:19104672

  2. 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

  3. 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

  4. RP-HPLC Estimation of Imipramine Hydrochloride and Diazepam in Tablets

    PubMed Central

    Srikantha, D.; Raju, R. R.

    2015-01-01

    A simple and rapid reversed phase-high performance liquid chromatographic method was developed for simultaneous determination of imipramine hydrochloride and diazepam in pharmaceutical formulations. The elution was done in isocratic mode utilizing a mobile phase consisting of methanol:water:0.1M sodium acetate (30:50:20 v/v/v) on Chromosil C18 column with a flow rate of 1.0 ml/min and with detection at 243 nm. The measured retention time was 3.33±0.02 min for imipramine hydrochloride and 4.64±0.02 min for diazepam. Linearity was measured in the range 25-150 μg/ml for imipramine hydrochloride (r2=0.999) and in the range 5-30 μg/ml for diazepam (r2=0.9994), respectively. The limits of detection and quantitation were 0.03 and 0.1 μg/ml for imipramine hydrochloride and 0.02 and 0.07 μg/ml for diazepam. Satisfactory validation was also obtained from recovery (100.95-101.52% for imipramine hydrochloride and 99.47-100.33% for diazepam) studies, intraday and interday precision (<2%) and robustness results. The reported method was the first study of these drugs in combination and could be employed for routine quantitative determination of imipramine hydrochloride and diazepam in tablets. PMID:26180281

  5. 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

  6. Comparative effects of ractopamine hydrochloride and zilpaterol hydrochloride on growth performance, carcass traits, and longissimus tenderness of finishing steers.

    PubMed

    Scramlin, S M; Platter, W J; Gomez, R A; Choat, W T; McKeith, F K; Killefer, J

    2010-05-01

    Ractopamine hydrochloride (RAC) and zilpaterol hydrochloride (ZH) are beta-adrenergic agonists that improve growth performance and affect carcass characteristics. The objective of this study was to evaluate the comparative effects of RAC and ZH when fed to beef steers during the last 33 d of the finishing period. Three hundred crossbred beef steers (516 +/- 8 kg) were grouped by BW, BCS, and breed type and randomly assigned to 1 of 3 treatments (10 steers per pen; 10 pens per treatment). Treatments were control (no beta-agonists added), RAC (200 mg of ractopaminexhdx(-1)d(-1), for 33 d), or ZH (75 mg of zilpaterolxanimalx(-1)d(-1), for 30 d, removed 3 d for required withdrawal period). Steers were slaughtered, carcass characteristics were evaluated, and cut-out yields were determined. Both RAC and ZH increased final BW, ADG, feed efficiency (G:F), and HCW compared with controls (P < 0.05). Compared with RAC, ZH decreased ADG, ADFI, and final BW, but increased HCW and dressing percentage (P < 0.05). Carcass yield was not affected by RAC in this experiment, whereas ZH decreased adjusted fat thickness and KPH, increased ribeye area, improved yield grade, and increased cut-out yields, when compared with controls (P < 0.05). Marbling, lean maturity, and skeletal maturity were not different between treatments (P > 0.05). Steaks from RAC steers had greater (P < 0.05) Warner-Bratzler shear force (WBSF) values than steaks from control steers at 3 and 7 d of aging, but did not differ from controls after 14 d of aging. Steaks from ZH steers had greater WBSF values (P < 0.05) than steaks from controls and RAC steaks throughout the 21-d postmortem aging period. Although both beta-adrenergic agonists were effective at improving feedlot performance, RAC showed no negative effect on WBSF after 14 d, whereas WBSF values for ZH steaks were significantly greater than controls after 21 d. PMID:20042550

  7. Increased mortality in groups of cattle administered the β-adrenergic agonists ractopamine hydrochloride and zilpaterol hydrochloride.

    PubMed

    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

  8. 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 reaction have been studied. Linearity range is 50.00-600.00 microg/ml. The validity of the described procedures was assessed by applying the standard addition technique. Statistical analysis of the results has been carried out revealing high accuracy and good precision. The suggested procedures could be used for the determination of mequitazine, both in pure and dosage forms, as well as in the presence of its degradate. PMID:12062671

  9. 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 when stored in a freezer (≤-20 °C). PMID:27086098

  10. 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 the related impurities. PMID:20056035

  11. 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

  12. Human serum paraoxonase-1 (hPON1): in vitro inhibition effects of moxifloxacin hydrochloride, levofloxacin hemihidrate, cefepime hydrochloride, cefotaxime sodium and ceftizoxime sodium.

    PubMed

    Türkeş, Cüneyt; Söyüt, Hakan; Beydemir, Şükrü

    2015-01-01

    In this study, we investigated the effects of antibacterial drugs (moxifloxacin hydrochloride, levofloxacin hemihidrate, cefepime hydrochloride, cefotaxime sodium and ceftizoxime sodium) on human serum paraoxonase-1 (hPON1) enzyme activity from human serum in vitro conditions. For this purpose, hPON1 enzyme was purified from human serum using simple chromatographic methods. The antibacterial drugs exhibited inhibitory effects on hPON1 at low concentrations. Ki constants were calculated to be 2.641 ± 0.040 mM, 5.525 ± 0.817 mM, 35.092 ± 1.093 mM, 252.762 ± 5.749 mM and 499.244 ± 10.149 mM, respectively. The inhibition mechanism of moxifloxacin hydrochloride was competitive, whereas levofloxacin hemihidrate, cefepime hydrochloride, cefotaxime sodium and ceftizoxime sodium were noncompetitive inhibitors. PMID:25519764

  13. 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…

  14. 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

  15. 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?M (colon), and these IC50 values were comparable to those of the doxorubicin standard (IC50=0.021, 0.074, 0.001, and 0.872?M, respectively). DPPH assay showed compounds 3f, 3i, and 3g had IC50 values of 0.60, 0.99, and 1.30?M, respectively, which were comparable to that of ascorbic acid (IC50=0.87?M). 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

  16. 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

  17. 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

  18. 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

  19. Amantadine hydrochloride for refractory generalized epilepsy in adults.

    PubMed

    Drake, M E; Pakalnis, A; Denio, L S; Phillips, B

    1991-01-01

    Amantadine hydrochloride has been shown in several open studies to benefit children with refractory generalized epilepsy. We used amantadine as adjunctive therapy in 10 adolescents and adults with generalized tonic-clonic, myoclonic, or absence seizures refractory to therapeutic levels of valproate, carbamazepine, phenytoin, and benzodiazepines. Seven patients were men and 3 were women aged 18-29 years, and 8 of 10 patients were mentally retarded. All patients had generalized epileptiform paroxysms on EEG, with generalized or absence seizure recorded in 9. Five patients had both absence and tonic-clonic seizures, and 2 had all three seizure types. Amantadine was added to the existing regimens in weekly increments to 400 mg/day. Two patients had greater than 90 per cent seizure reduction, both with vomiting and somnolence. Two patients had seizure reduction between 50 and 90 per cent, 1 with anorexia and sleepiness. Three patients had no change in seizures, and 3 had worse tonic-clonic seizures. Amantadine may have some antiepileptic efficacy of unknown mechanism, but it may worsen generalized tonic-clonic seizures and is likely to be of limited value in adults. PMID:1927254

  20. Development and evaluation of microporous osmotic tablets of diltiazem hydrochloride

    PubMed Central

    Bathool, Afifa; Gowda, D. V.; Khan, Mohammed S.; Ahmed, Ayaz; Vasudha, S. L.; Rohitash, K.

    2012-01-01

    Microporous osmotic tablet of diltiazem hydrochloride was developed for colon targeting. These prepared microporous osmotic pump tablet did not require laser drilling to deliver the drug to the specific site of action. The tablets were prepared by wet granulation method. The prepared tablets were coated with microporous semipermeable membrane and enteric polymer using conventional pan coating process. The incorporation of sodium lauryl sulfate (SLS), a leachable pore-forming agent, could form in situ delivery pores while coming in contact with gastrointestinal medium. The effect of formulation variables was studied by changing the amounts of sodium alginate and NaCMC in the tablet core, osmogen, and that of pore-forming agent (SLS) used in the semipermeable coating. As the amount of hydrophilic polymers increased, drug release rate prolonged. It was found that drug release was increased as the concentration of osmogen and pore-former was increased. Fourier transform infrared spectroscopy and Differential scanning calorimetry results showed that there was no interaction between drug and polymers. Scanning electron microscopic studies showed the formation of pores after predetermined time of coming in contact with dissolution medium. The formation of pores was dependent on the amount of pore former used in the semipermeable membrane. in vitro results showed acid-resistant, timed release at an almost zero order up to 24 hours. The developed osmotic tablets could be effectively used for prolonged delivery of Diltiazem HCl. PMID:22837961

  1. Hydrocolloid carriers with filler inclusion for diltiazem hydrochloride release.

    PubMed

    Gal, A; Nussinovitch, A

    2007-01-01

    Hydrocolloid beads based on agarose, alginate (both 3%, w/w), or gellan (2%, w/w) were produced to study their potential as drug carriers. The beads included various fillers: talc, kaolin, calcium carbonate, potato, or corn starch (10%, w/w). After gelation, the carriers were subjected to either freeze- or vacuum-drying. The dried carriers were spheroids. The diameters of freeze- and vacuum-dried carriers ranged from 2.4 to 4.1 mm and 1.5 to 2.8 mm, respectively. The porosity values of the freeze-dried carriers were significantly higher than those of their vacuum-dried counterparts. Scanning electron microscopy (SEM) revealed that all dried carriers included internal voids that were partially occupied by the filler particles. Upon their introduction into simulated gastric fluid (3 h), followed by 6 h in intestinal fluid, all carriers were stable and underwent swelling. Release profiles of diltiazem hydrochloride from different carriers were obtained during immersion in dissolution medium. Filler inclusion (but not the type of filler) contributed to the stability of the carriers and prolonged the time of drug release (6.5-8.5 h) relative to the faster drug release from carriers that contained no filler (3.5 h). In summary, alginate, agar, and gellan beads with filler inclusion may be useful for slow drug release. PMID:17031844

  2. Dielectric relaxation studies and dissolution behavior of amorphous verapamil hydrochloride.

    TOXLINE Toxicology Bibliographic Information

    Adrjanowicz K; Kaminski K; Paluch M; Wlodarczyk P; Grzybowska K; Wojnarowska Z; Hawelek L; Sawicki W; Lepek P; Lunio R

    2010-02-01

    Verapamil hydrochloride (VH) is a very popular calcium channel blocker. Solubility of its crystalline form in the blood reaches only 10-20%. Thus, it seems to be very important to improve its bioavailability. In this article, we show that the preparation of the amorphous form of VH enhance its dissolution rate. In addition we performed dielectric measurements to describe molecular dynamics of this active pharmaceutical ingredient (API). Since examined sample is typical ionically conducting material, to gain information about structural relaxation we employed the dielectric modulus formalism. The temperature dependence of the structural relaxation time can be described over the entire measured range by a single Vogel-Fulcher-Tamman (VFT) equation. From the VFT fits the glass transition temperature was estimated as T(g) = 320.1 K. Below glass transition temperature one clearly visible secondary relaxation, with activation energy E(a) = 37.8 kJ/mol, was reported. Deviations of experimental data from KWW fits on high-frequency flank of alpha-peak indicate the presence of an excess wing in tested sample. Based on Kia Ngai's coupling model we identified the excess wing as true Johari-Goldstein process.

  3. 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

  4. Properties of olopatadine hydrochloride, a new antiallergic/antihistaminic drug.

    PubMed

    Ohmori, Kenji; Hasegawa, Kazuhide; Tamura, Tadafumi; Miyake, Kiyomi; Matsubara, Masahiro; Masaki, Shigehiro; Karasawa, Akira; Urayama, Naoko; Horikoshi, Kaori; Kajita, Jiro; Hasegawa, Masanori; Taniguchi, Koji; Komada, Toshio; Kawamoto, Yuji

    2004-01-01

    Olopatadine hydrochloride (CAS 140462-76-6, KW-4679, AL-4943A; hereinafter referred to as olopatadine) is a novel antiallergic drug that is a selective histamine H1 receptor antagonist possessing inhibitory effects on the release of inflammatory lipid mediators such as leukotriene and thromboxane from human polymorphonuclear leukocytes and eosinophils. Olopatadine also inhibits the tachykininergic contractions in guinea pig bronchi by prejunctional inhibition of peripheral sensory nerves. Oral administration of olopatadine at doses of 0.03 mg/kg or higher reduces the symptoms of experimental allergic cutaneous responses and rhinoconjunctivitis in sensitized animals. Preclinical and clinical evaluations have demonstrated that olopatadine is a safe drug. After oral administration to healthy volunteers, olopatadine was rapidly and extensively absorbed. Unlike most other antiallergic drugs which are eliminated via hepatic metabolism, olopatadine is mainly excreted into urine. Olopatadine did not affect cytochrome P450 activities in human liver microsomes and consequently drug-drug metabolic interactions are unlikely. In double-masked clinical trials, olopatadine was shown to be effective at alleviating symptoms of allergic diseases. The drug (Allelock) was approved in Japan for the treatment of allergic rhinitis, chronic urticaria, eczema dermatitis, prurigo, cutaneous pruritus, psoriasis vulgaris and erythema exsudativum multiforme in December, 2000. An ophthalmic solution of olopatadine is also useful for the treatment of allergic conjunctivitis: this formulation (Patanol) was approved in the USA and the European Union for the treatment of seasonal and perennial allergic conjunctivitis in 1996 and 2002, respectively. PMID:15646365

  5. 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

  6. Properties of melarsamine hydrochloride (Cymelarsan) in aqueous solution.

    PubMed Central

    Berger, B J; Fairlamb, A H

    1994-01-01

    The antitrypanosomal drug melarsamine hydrochloride (MelCy) (trade name, Cymelarsan) is a melamino-phenylarsine made by conjugation of one equivalent of melarsen oxide and two equivalents of cysteamine. Immediately after it was dissolved in water, the compound was found to exist as an equilibrium mixture containing MelCy (43%), MelCy which had lost one cysteamine moiety (MelCy -1; 24%), melarsen oxide (33%), and free cysteamine. Small amounts (< 1%) of the oxidation products derived from the last two components were also formed (cystamine and sodium melarsen). On incubation at room temperature, the MelCy content decreased steadily, with an associated increase in the melarsen oxide and sodium melarsen contents. After 5 days in solution at room temperature, 27% of the arsenical agent was MelCy, 14% was MelCy -1, 42% was melarsen oxide, and 17% was sodium melarsen. Since H2O2 production was detectable in MelCy or cysteamine solutions and the addition of small amounts of exogenous H2O2 readily converted the trivalent melarsen oxide to the pentavalent sodium melarsen, it is hypothesized that the nonenzymatic conversion of cysteamine to cystamine produced H2O2, which then oxidized melarsen oxide to sodium melarsen. Similar time course experiments showed that melarsonyl potassium and melarsoprol were more stable in solution. PMID:8092828

  7. 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

  8. 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

  9. Solubility analysis of buspirone hydrochloride polymorphs: measurements and prediction.

    PubMed

    Sheikhzadeh, M; Rohani, S; Taffish, M; Murad, S

    2007-06-29

    In this paper, the solubility of two polymorphs of buspirone hydrochloride (BUS-HCl) in isopropanol, water and mixture of these two solvents has been investigated. The solubility of BUS-HCl Form 2 in water and isopropanol is higher than BUS-HCl Form 1. According to thermodynamic properties and Burger and Ramberger polymorphic rules (Bernstein, 2002), BUS-HCl Forms 1 and 2 are enantiotropes (Sheikhzadeh et al., 2007). Using the solubility data, transformation analysis has been done and the results confirm these two polymorphs are enantiotropes and Form 1 converts to Form 2 at 95 degrees C. The UNIQUAC binary adjustable parameters have been found and based on these parameters, the solubility of these molecules has been predicted and compared with the experimental solubility. The solubility prediction has been performed by using different UNIFAC equations for binary and ternary systems. The UNIQUAC and original UNIFAC showed better prediction capability. Different general solubility equations (GSE) have been used for estimation of solubility which works based on partial charge, hydrogen bond factors and partition coefficients. PMID:17317053

  10. 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

  11. 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

  12. [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

  13. 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.

  14. Bioavailability of oral and intramuscular molindone hydrochloride in schizophrenic patients.

    PubMed

    Zetin, M; Cramer, M; Garber, D; Plon, L; Paulshock, M; Hoffman, H E; Schary, W L

    1985-01-01

    This study was designed to assess the bioequivalence of intramuscular molindone hydrochloride and marketed oral molindone. Ten schizophrenic patients (mean age, 30.2 years) received oral molindone in single daily doses of 100 or 150 mg for four to eight days followed by intramuscular molindone in single daily doses of 50 or 75 mg for four days. On the last day each molindone formulation was given, plasma samples were collected at baseline and at 0.5, 1, 2, 4, 6, 8, and 12 hours after administration. The pharmacokinetic measures of area under the curve and maximum concentration show that intramuscular molindone is 1.49 to 1.67 times more bioavailable than oral molindone. This finding indicates that once a patient's acute psychotic episode has been stabilized with intramuscular molindone, therapy can continue without interruption by substituting 1.5 mg of oral molindone for every 1 mg of intramuscular molindone. The time to maximum concentration occurred significantly earlier (P = 0.05) with intramuscular molindone (0.6 hours) than with oral molindone (1.1 hours). Elimination half-life values were approximately two hours for both formulations. PMID:3986861

  15. Conformation and interactions of dopamine hydrochloride in solution

    NASA Astrophysics Data System (ADS)

    Callear, Samantha K.; Johnston, Andrew; McLain, Sylvia E.; Imberti, Silvia

    2015-01-01

    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.

  16. Spectrophotometric estimation of tamsulosin hydrochloride by acid-dye method

    PubMed Central

    Shrivastava, Alankar; Saxena, Prachi; Gupta, Vipin B.

    2011-01-01

    A new spectrophotometric method for the estimation of tamsulosin hydrochloride in pharmaceutical dosage forms has been developed and validated. The method is based on reaction between drug and bromophenol blue and complex was measured at 421 nm. The slope, intercept and correlation coefficient was found to be 0.054, -0.020 and 0.999, respectively. Method was validated in terms of specificity, linearity, range, precision and accuracy. The developed method can be used to determine drug in both tablet and capsule formulations. Reaction was optimized using three parameters i.e., concentration of the dye, pH of the buffer, volume of the buffer and shaking time. Maximum stability of the chromophore was achieved by using pH 2 and 2 ml volume of buffer. Shaking time kept was 2 min and concentration of the dye used was 2 ml of 0.05% w/v solution. Method was validated in terms of linearity, precision, range, accuracy, LOD and LOQ and stochiometry of the method was also established using Mole ratio and Job's method of continuous variation. The dye benzonoid form (blue color) of dye ionized into quinonoid form (purple color) in presence of buffer and reacts with protonated form of drug in 1:1 ratio and forms an ion-pair complex (yellow color). PMID:23781431

  17. Capillary electrophoresis method for fexofenadine hydrochloride in capsules.

    PubMed

    Breier, Ana R; Garcia, Sílvia S; Jablonski, André; Steppe, Martin; Schapoval, Elfrides E S

    2005-01-01

    A simple, accurate, and effective capillary electrophoresis method with ultraviolet absorbance detection was developed and validated for the quantitation of the antihistamine fexofenadine in capsules. The separation was performed with an uncoated fused-silica capillary (47 cm x 75 microm id) and was operated at 20 kV potential. Temperature was maintained at 25 degrees C. The run buffer was prepared with 20mM Na2B4O7 x 10 H2O. Software was used for system control, data acquisition, and analysis. Method validation was performed by evaluation of the analytical parameters linearity, precision, accuracy, limits of detection and quantitation, and specificity. The method was linear (r = 0.9999) at concentrations ranging from 20 to 100 microg/mL, precise (relative standard deviation intra-assay = 1.2, 1.6, and 1.8% and interassay = 1.5%); accurate (recovery = 98.1%); and specific. The limits of detection and quantitation were 0.69 and 2.09 microg/mL, respectively. The method was compared to the liquid chromatography method developed previously by the authors for the same drug, and no significant difference was found between the 2 methods in fexofenadine hydrochloride quantitation. PMID:16152920

  18. Effects of ractopamine hydrochloride and zilpaterol hydrochloride supplementation on carcass cutability of calf-fed Holstein steers.

    PubMed

    Howard, S T; Woerner, D R; Vote, D J; Scanga, J A; Acheson, R J; Chapman, P L; Bryant, T C; Tatum, J D; Belk, K E

    2014-01-01

    Effects of ractopamine hydrochloride (RH) and zilpaterol hydrochloride (ZH) on saleable yield of carcass sides from calf-fed Holstein steers were evaluated using steers implanted with a progesterone (100 mg) plus estradiol benzoate (10 mg) implant followed by a terminal trenbolone acetate (200 mg) plus estradiol (40 mg) implant. Steers were blocked by weight into pens (n = 32) randomly assigned to one of four treatments: control, RH fed at 300 mg•steer(-1)/d(-1) (RH 300) or RH fed at 400 mg•steer(-1)/d(-1) (RH 400) the final 31 d of finishing, and ZH fed at 60 to 90 mg•steer(-1)/d(-1) (7.56 g/ton on a 100% DM basis) for 21 d with a 5 d withdrawal before harvest. Eight to nine carcass sides were randomly selected from each pen; carcass sides with excessive hide pulls, fat pulls or bruises were avoided. Cutout data were collected within a commercial facility using plant personnel to fabricate sides at a rate of one every 3 to 4 min into items typically merchandised by the facility. All lean, fat and bone were weighed and summed back to total chilled side weight with a sensitivity of ± 2% to be included in the data set. Compared to controls, β-agonists increased saleable yield of whole-muscle cuts by 0.61%, 0.86% and 1.95% for RH 300, RH 400 and ZH, respectively (P < 0.05). Percent fat was less in carcasses from the ZH treatment compared to controls (P < 0.05); however, this difference was not observed between RH treatments and controls (P > 0.05). Percent bone was less in the ZH treatment due to increased muscle (P < 0.05). The percent of chilled side weight comprised of trimmings was unchanged between treatments, but on a 100% lean basis, RH 400 and ZH increased trim yields (P < 0.05). Analysis of saleable yield by primal showed a fundamental shift in growth and development. Beta-agonists caused a shift in proportion of saleable yield within individual primals, with a greater portion produced from the hindquarter relative to the forequarter, specifically in those muscles of the round (P < 0.05). Beta-agonists increased saleable yield, but these effects were not constant between all major primals. The cutout value gained by packers as a result of β-agonist use may be influenced more by reduced fatness and increased absolute weight if musculature is primarily increased in the lower priced cuts of the carcass. PMID:24243909

  19. Effects of ractopamine hydrochloride and zilpaterol hydrochloride supplementation on longissimus muscle shear force and sensory attributes of beef steers.

    PubMed

    Arp, T S; Howard, S T; Woerner, D R; Scanga, J A; McKenna, D R; Kolath, W H; Chapman, P L; Tatum, J D; Belk, K E

    2013-12-01

    Effect of ractopamine hydrochloride (RH) and zilpaterol hydrochloride (ZH) on LM shear force and sensory attributes was determined using pens (n = 40) British × Continental crossbred steers randomly allocated to one of the following treatments: control; RH fed at 200 (RH 200) or 300 mg • steer(-1) • d(-1) (RH 300), or 400 mg • steer(-1) • d(-1) (RH 400) top-dressed for the final 30 d of feeding; or ZH fed at 7.5 mg/kg, beginning 23 d before slaughter with a 3-d withdrawal. Two replicates (pens) per treatment were represented in four blocks. Eighteen carcasses per pen were randomly selected and one 5-cm LM sample was removed from both carcass sides to be used for shear force and sensory evaluation. Samples were aged for 14 d, frozen at -28.8 °C, and cut into 2.5-cm steaks. All steaks were cooked to an internal temperature of 71.1 °C before being evaluated for Warner-Bratzler shear force (WBSF), slice shear force (SSF), or being fed to trained sensory panelists. Increasing dose and potency of β-agonist increased WBSF by 4 to 17% and SSF by 5 to 24% (P < 0.05). Steaks from steers fed ZH had higher WBSF and SSF values compared with all other treatments (P < 0.05), whereas steaks from controls and steers fed RH 200 were not different (P > 0.05). Probability of steaks failing to meet shear force standards to be certified tender (WBSF <4.4 kg, SSF < 20 kg) was increased from an initial probability of <0.06 in steaks from steers in the control treatment to 0.10 to 0.20 in steers fed RH 400 or ZH (P < 0.05). No difference was detected in panel ratings for overall tenderness of steaks from steers fed RH 200 compared with controls (P > 0.05). Steaks from steers fed RH 300 and RH 400 were comparable for all sensory attributes; however, both RH 300 and RH 400 were rated lower for overall tenderness than controls (P < 0.05). Panelists failed to detect differences in overall tenderness of steaks from steers fed RH 400 and ZH (P < 0.05). Panelists detected no difference in flavor profile or juiciness among treatments (P > 0.05). Results from this study indicated β-agonists negatively affected beef tenderness and these effects may be more noticeable in steers supplemented with ZH and higher doses of RH. PMID:24166996

  20. Synthesis and antitumor mechanisms of a copper(II) complex of anthracene-9-imidazoline hydrazone (9-AIH).

    PubMed

    Qin, Qi-Pin; Liu, Yan-Cheng; Wang, Hai-Lu; Qin, Jiao-Lan; Cheng, Feng-Jie; Tang, Shang-Feng; Liang, Hong

    2015-07-01

    A new anthracycline derivative, anthracene-9-imidazoline hydrazone (9-AIH), was synthesized and selected as an antitumor ligand to afford a copper(II) complex of 9-AIH, cis-[Cu(II)Cl2(9-AIH)] (1). Complex 1 was structurally characterized by IR, elemental analysis, ESI-MS and single crystal X-ray diffraction analysis. By MTT assay, it was revealed that 1 showed overall a higher in vitro cytotoxicity than 9-AIH towards a panel of human tumour cell lines, with IC50 values from 0.94–3.68 μM, in which the BEL-7404 cell line was the most sensitive to 1. By spectral analyses and gel electrophoresis, the DNA binding affinity of 9-AIH and 1 was determined. 9-AIH was suggested to bind with DNA in an intercalative mode, with a quenching constant of 1.04 × 10(4) M(−1) on the EB–DNA complex. While for 1, both intercalative and covalent binding modes were suggested. By flow cytometry, 1 was found to block the cell cycle of BEL-7404 cells in a dose-dependent mode, in which it induced the G2/M phase arrest at 0.5 μM and induced the S phase arrest at higher concentrations of 1.0 or 2.0 μM. From the cellular morphological observations under different fluorescence probe staining, a dose-dependent manner of 1 to induce cell apoptosis in the late stage was suggested. Comparatively, equivalent apoptotic cells, respectively, in the early and late stages were found when incubated with 2.0 μM of 9-AIH. The mitochondrial membrane potential measured by JC-1 staining and the ROS generation in cells detected using a DCFH-DA probe suggested that the cell apoptosis induced by 1 might undergo the ROS-related mitochondrial pathway. Accordingly, the mutant p53 expression was found to be suppressed and the caspase cascade (caspase-9/3) was consequently activated by 1. This action mechanism for 1 in the BEL-7404 cells was unique and was not found in the presence of 9-AIH under the same conditions, indicating their different antitumor mechanism. Furthermore, the in vivo acute toxicity of 1 tested on mice indicated that 1 should be a high cytotoxic antitumor agent, with the LD50 value in the range of 32–45 mg kg(−1), which is much higher than that of 9-AIH. From the above results, the central Cu(II) of 1 in the coordinated mode with 9-AIH was believed to play a key role in exerting both the high cytotoxicity and the effective antitumor mechanism. PMID:25904543

  1. 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

  2. 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

  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. 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,...

  5. 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,...

  6. 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.

  7. 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

  8. Ornithine carbamoyltransferase unfolding states in the presence of urea and guanidine hydrochloride.

    PubMed

    Barreca, D; Laganà, G; Ficarra, S; Tellone, E; Leuzzi, U; Galtieri, A; Bellocco, E

    2014-01-01

    Ornithine carbamoyltransferase folding/unfolding is a complex and not completely understood process. Our experimental results suggest that ornithine carbamoyltransferase interacts in a completely different way with urea and guanidine hydrochloride. In fact, we noticed that, increasing concentration from 0.0 to 8.0 M of the two additives, the enzyme follows a simple one-step transition mechanism in the presence of guanidine hydrochloride, with two macroscopic states (the native and the denatured one) significantly populated, whereas in the presence of urea a lot of different protein states can be detected and analyzed. Circular dichroism and UV-visible spectroscopy reveal a similar mechanism of perturbation at high temperature, with opening of hydrophobic core and a significant loss in α-helix structure in the presence of guanidine hydrochloride that cannot be found in the presence of urea. PMID:24122710

  9. High-performance thin-layer chromatographic determination of diltiazem hydrochloride as bulk drug and in pharmaceutical preparations.

    PubMed

    Devarajan, P V; Dhavse, V V

    1998-03-20

    A simple, rapid, selective and precise high-performance thin-layer chromatographic method for the analysis of diltiazem hydrochloride both as a bulk drug and in pharmaceuticals is reported. The mobile phase composition was ethyl acetate-methanol-strong ammonia solution (80:10:10, v/v). Densitometric analysis of diltiazem hydrochloride was carried out at 238 nm. The calibration curve of diltiazem hydrochloride in distilled water was linear in the range 40-400 ng. The mean value of correlation coefficient, slope and intercept were 0.997+/-0.0008, 0.0617+/-0.0012 and 7.16+/-0.2562, respectively. The limits of detection and quantitation were 20 ng and 40 ng, respectively. The recovery of diltiazem hydrochloride was about 99.5%. The method was utilized to analyse diltiazem hydrochloride from conventional and sustained release tablets in the presence of commonly used excipients. PMID:9551826

  10. 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

  11. A novel lidocaine hydrochloride ophthalmic gel for topical ocular anesthesia

    PubMed Central

    Shah, HR; Reichel, E; Busbee, BG

    2010-01-01

    Topical anesthetics play an important role in the practice of ophthalmology, both for procedures in the office and in the operating room. The need for safe, long-acting topical ocular anesthetic agents is ongoing, and has been highlighted by the increase of intravitreal administration of pharmacologic agents. Current practices for ocular anesthesia include subconjunctival injection of 2% aqueous lidocaine, topical 2% lidocaine drops and topical 0.5% tetracaine. Tetracaine is not yet FDA approved, and is associated with corneal epithelial toxicity and delayed epithelial healing after multiple administrations. Lidocaine jelly (2%) preparations have been reported to be beneficial in several systemic procedures, including those of the upper airway, dental, urogenital, and gastrointestinal. It has been theorized, and recent studies support the idea, that gel formulations of lidocaine may enhance anesthetic effect, and therefore be superior to anesthetic solutions for topical cataract surgery. The viscous nature of gel formulations is thought to lengthen contact time, resulting in better anesthesia at lower drug concentrations. Furthermore, several studies suggest that lidocaine is bactericidal and bacteriostatic, and may have a supplementary role in preventing and treating surgical site infections. Akten™, lidocaine 3.5% gel (Akorn, Buffalo Grove, IIlinois) was FDA approved for all ophthalmic procedures in October 2008. This gel is a preservative-free, lidocaine-based anesthetic gel consisting of 35 mg/mL of lidocaine hydrochloride. We describe the properties, including chemical structure, indications, evidence of support, use, adverse effects, and precautions, which we believe enable Akten to provide superior anesthesia, while minimizing side effects. PMID:22915870

  12. A novel lidocaine hydrochloride ophthalmic gel for topical ocular anesthesia.

    PubMed

    Shah, Hr; Reichel, E; Busbee, Bg

    2010-01-01

    Topical anesthetics play an important role in the practice of ophthalmology, both for procedures in the office and in the operating room. The need for safe, long-acting topical ocular anesthetic agents is ongoing, and has been highlighted by the increase of intravitreal administration of pharmacologic agents. Current practices for ocular anesthesia include subconjunctival injection of 2% aqueous lidocaine, topical 2% lidocaine drops and topical 0.5% tetracaine. Tetracaine is not yet FDA approved, and is associated with corneal epithelial toxicity and delayed epithelial healing after multiple administrations. Lidocaine jelly (2%) preparations have been reported to be beneficial in several systemic procedures, including those of the upper airway, dental, urogenital, and gastrointestinal. It has been theorized, and recent studies support the idea, that gel formulations of lidocaine may enhance anesthetic effect, and therefore be superior to anesthetic solutions for topical cataract surgery. The viscous nature of gel formulations is thought to lengthen contact time, resulting in better anesthesia at lower drug concentrations. Furthermore, several studies suggest that lidocaine is bactericidal and bacteriostatic, and may have a supplementary role in preventing and treating surgical site infections. Akten™, lidocaine 3.5% gel (Akorn, Buffalo Grove, IIlinois) was FDA approved for all ophthalmic procedures in October 2008. This gel is a preservative-free, lidocaine-based anesthetic gel consisting of 35 mg/mL of lidocaine hydrochloride. We describe the properties, including chemical structure, indications, evidence of support, use, adverse effects, and precautions, which we believe enable Akten to provide superior anesthesia, while minimizing side effects. PMID:22915870

  13. Pharmacokinetics and tissue distribution of minocycline hydrochloride in horses.

    TOXLINE Toxicology Bibliographic Information

    Nagata S; Yamashita S; Kurosawa M; Kuwajima M; Hobo S; Katayama Y; Anzai T

    2010-09-01

    OBJECTIVE: To determine the pharmacokinetics and tissue distribution of minocycline in horses.ANIMALS: 5 healthy Thoroughbred mares for the pharmacokinetic experiment and 6 healthy Thoroughbred mares for the tissue distribution experiment.PROCEDURES: Each mare was given 2.2 mg of minocycline hydrochloride/kg, IV. Blood samples were collected once before minocycline administration (0 hours) and 10 times within 48 hours after administration in the pharmacokinetics study, and 24 tissue samples were obtained at 0.5 and 3 hours in the distribution study.RESULTS: No adverse effects were observed in any of the mares after minocycline administration. The mean+/-SD elimination half-life was 7.70+/-1.91 hours. The total body clearance was 0.16+/-0.04 L/h/kg, and the volume of distribution at steady state was 1.53+/-0.09 L/kg. The percentage of plasma protein binding was 68.1+/-2.6%. Plasma concentration of free minocycline was 0.12 microg/mL at 12 hours. Minocycline was not detected in brain tissue, CSF or aqueous humor at 0.5 hours; however, it was found in all tissues, except in the aqueous humor, at 3 hours.CONCLUSIONS AND CLINICAL RELEVANCE: Clearance of minocycline in healthy mares was greater than that reported for humans. For effective treatment of infections with common equine pathogens, it will be necessary to administer minocycline at a dosage of 2.2 mg/kg, IV, every 12 hours. This drug could be useful for infections in many tissues, including the CNS. The pharmacokinetic and tissue distribution data should aid in the appropriate use of minocycline in horses.

  14. [Simultaneous determination of five cold medicine ingredients in paracetamol triprolidine hydrochloride and pseudoephedrine hydrochloride tablets by pH/organic solvent double-gradient high performance liquid chromatography].

    PubMed

    Xuan, Xueyi; Huang, Lina; Pan, Xiaoling; Li, Ning

    2013-02-01

    A pH/organic solvent double-gradient mode in reversed-phase high performance liquid chromatography (HPLC) has been established as a new approach to the simultaneous determination of acetaminophen, caffeine, salicylamide, pseudoephedrine hydrochloride and triprolidine hydrochloride in paracetamol triprolidine hydrochloride and pseudoephedrine hydrochloride tablets. Through the optimization of the organic solvent gradient mode and pH/organic solvent double-gradient mode, the optimum double-gradient HPLC system of the five cold medicine ingredients has been built. The determination was carried out on a Diamonsiol C18 column (250 mm x 4.6 mm, 5 microm). The mobile phase consisted of methanol, 0.05 mol/L ammonium acetate solution and 0.08 mol/L acetic acid solution. The column temperature was set at 30 degrees C. The flow rate was 1.0 mL/min. The sample was measured at multiple wavelengths: 0-6 min, 280 nm; 6-7 min, 257 nm; 7-14 min, 280 nm; 14 min, 233 nm. The separation of the five cold medicine ingredients in the tablets was achieved in 25.5 min. The linear ranges of acetaminophen, pseudoephedrine hydrochloride, caffeine, salicylamide and triprolidine hydrochloride were 0.055 -0.998 g/L, 0.053-0.946 g/L, 0.007-0.129 g/L, 0.035-0.622 g/L and 0.002-0.039 g/L, respectively, with their correlation coefficients greater than 0.999 0. The detection limits (S/N = 3) were 0.09, 6, 0.02, 0.128 and 0.02 mg/L, respectively. Their mean recoveries were 97.9%-102.8%. The advantage of the method is the simultaneous determination of acidic, neutral and basic compounds. It also can improve the column efficiency of the analyte, compress the half-peak width and reduce the trailing. The optimized and validated method can be used for the simultaneous determination of the five cold medicine ingredients in the tablets. PMID:23697177

  15. Molecular interactions between selected sodium salts of bile acids and morphine hydrochloride.

    PubMed

    Poša, Mihalj; Csanádi, János; Kövér, Katalin E; Guzsvány, Valéria; Batta, Gyula

    2012-06-01

    The objective of this study was to understand the prolonged analgesic action of morphine hydrochloride observed in the presence of sodium 12-oxochenodeoxycholanate. Based on literature, this phenomenon may be due to the formation of aggregates in the cell between the molecules of bile acids and morphine. In addition to the sodium 12-oxochenodeoxycholanate, the present investigation also included salts of cholic and 7-oxodeoxycholic acids. Saturation transfer difference NMR experiments showed that morphine binds to the bile acid molecule close to the aromatic protons H1 and H2 provided that the concentration of the bile acid salt approaches the critical micellar concentration (CMC). The spin-lattice relaxation times (T(1)) of the affected protons decrease significantly in the presence of micellar solutions of the bile acid salts, and the most pronounced change in T(1) was observed for sodium 7-oxodeoxycholate. Diffusion-ordered NMR experiments suggested that morphine hydrochloride can interact only with sodium 7-oxochenodeoxycholate. It can be supposed that the molecular ratio of sodium 7-oxodeoxycholate and morphine hydrochloride in the mixed micelle is 2:1. The CMC values of mixed micelles do not differ from the CMC values of the micelle constituents, which suggests that the binding of morphine hydrochloride does not perturb the hydrophobic domain of the bile acid molecule. In the presence of bile acids, the transfer rate constant (k(12)) of morphine hydrochloride from the buffered aqueous solution to chloroform (model of the cell membrane) shows a decrease. A significant decrease of the k(12) was also observed in the presence of micellar solutions. Kinetic measurements indicated that, in addition to micellar interaction between morphine hydrochloride and sodium salts of bile acids, a complex may also be formed in chloroform via hydrogen bonds formed between the drug and bile acid molecules. PMID:22387018

  16. High performance thin layer chromatographic method for simultaneous estimation of Ibuprofen and pseudoephedrine hydrochloride.

    PubMed

    Chitlange, S S; Sakarkar, D M; Wankhede, S B; Wadodkar, S G

    2008-01-01

    High performance thin layer chromatographic method is developed for simultaneous estimation of ibuprofen and pseudoephedrine hydrochloride in tablets. Silica gel 60F(254) plates were used as stationary phase and t.butanol: ethyl acetate: glacial acetic acid: water (7:4:2:2 v/v) as mobile phase. Wavelength selected for analysis was 254 nm. Percent estimation of ibuprofen and pseudoephedrine hydrochloride was found to be 99.56% and 98.77%, respectively. Percent recovery for both the drugs was found in the range of 98.27% to 100.91%, respectively. PMID:20046759

  17. 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.

  18. 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 either β-agonist to calf-fed Holstein steers increased live performance through increased BW, BW gain, and ADG. Furthermore, supplementing calf-fed Holstein steers with ZH provides greater improvements in HCW, LM area, and yield grade components, with a slight decrease in quality grade when compared to calf-fed Holstein steers supplemented with RH. PMID:25006068

  19. 78 FR 40484 - Determination That METADATE ER (Methylphenidate Hydrochloride) Extended-Release Tablet, 10...

    Federal Register 2010, 2011, 2012, 2013, 2014

    2013-07-05

    ... Hydrochloride) Extended-Release Tablet, 10 Milligrams, Was Not Withdrawn From Sale for Reasons of Safety or... tablet, 10 milligrams (mg), was not withdrawn from sale for reasons of safety or effectiveness. This..., Drug, and Cosmetic Act (21 U.S.C. 355(j)(7)), which requires FDA to publish a list of all...

  20. 75 FR 14444 - Determination That DIDREX (Benzphetamine Hydrochloride) Tablets, 25 Milligrams, Were Not...

    Federal Register 2010, 2011, 2012, 2013, 2014

    2010-03-25

    ... FR 4280). Pfizer Inc. ceased manufacturing DIDREX (benzphetamine HCL) Tablets, 25 mg, prior to... (Benzphetamine Hydrochloride) Tablets, 25 Milligrams, Were Not Withdrawn From Sale for Reasons of Safety or...), were not withdrawn from sale for reasons of safety or effectiveness. This determination will allow...

  1. 77 FR 7583 - Determination That WILPO (phentermine hydrochloride) Tablets, 8 Milligrams, Was Not Withdrawn...

    Federal Register 2010, 2011, 2012, 2013, 2014

    2012-02-13

    ..., 8 Milligrams, Was Not Withdrawn From Sale for Reasons of Safety or Effectiveness AGENCY: Food and... determined that WILPO (phentermine hydrochloride) Tablets, 8 Milligrams (mg), was not withdrawn from sale for... amendments include what is now section 505(j)(7) of the Federal Food, Drug, and Cosmetic Act (21 U.S.C....

  2. 75 FR 64310 - Determination That BUSPAR (Buspirone Hydrochloride) Tablets, 10 Milligrams, 15 Milligrams, and 30...

    Federal Register 2010, 2011, 2012, 2013, 2014

    2010-10-19

    ...The Food and Drug Administration (FDA) has determined that BUSPAR (buspirone hydrochloride) Tablets, 10 milligrams (mg), 15 mg, and 30 mg, 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 this drug product, and it will allow FDA to......

  3. 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…

  4. 21 CFR 520.1242b - Levamisole hydrochloride tablet or oblet (bolus).

    Code of Federal Regulations, 2014 CFR

    2014-04-01

    ... 21 Food and Drugs 6 2014-04-01 2014-04-01 false Levamisole hydrochloride tablet or oblet (bolus). 520.1242b Section 520.1242b Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND... nonaqueous titration with 0.1 N potassium isopropoxide; 1 isomer minimum 95 percent pure by optical...

  5. 21 CFR 520.1242b - Levamisole hydrochloride tablet or oblet (bolus).

    Code of Federal Regulations, 2013 CFR

    2013-04-01

    ... 21 Food and Drugs 6 2013-04-01 2013-04-01 false Levamisole hydrochloride tablet or oblet (bolus). 520.1242b Section 520.1242b Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND... nonaqueous titration with 0.1 N potassium isopropoxide; 1 isomer minimum 95 percent pure by optical...

  6. 21 CFR 520.1242b - Levamisole hydrochloride tablet or oblet (bolus).

    Code of Federal Regulations, 2011 CFR

    2011-04-01

    ... 21 Food and Drugs 6 2011-04-01 2011-04-01 false Levamisole hydrochloride tablet or oblet (bolus). 520.1242b Section 520.1242b Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND... nonaqueous titration with 0.1 N potassium isopropoxide; 1 isomer minimum 95 percent pure by optical...

  7. 21 CFR 520.1242b - Levamisole hydrochloride tablet or oblet (bolus).

    Code of Federal Regulations, 2012 CFR

    2012-04-01

    ... 21 Food and Drugs 6 2012-04-01 2012-04-01 false Levamisole hydrochloride tablet or oblet (bolus). 520.1242b Section 520.1242b Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND... nonaqueous titration with 0.1 N potassium isopropoxide; 1 isomer minimum 95 percent pure by optical...

  8. Effect of magnesium stearate concentration on dissolution properties of ranitidine hydrochloride coated tablets.

    PubMed

    Uzunović, Alija; Vranić, Edina

    2007-08-01

    Most pharmaceutical formulations also include a certain amount of lubricant to improve their flowability and prevent their adhesion to the surfaces of processing equipment. Magnesium stearate is an additive that is most frequently used as a lubricant. Magnesium stearate is capable of forming films on other tablet excipients during prolonged mixing, leading to a prolonged drug liberation time, a decrease in hardness, and an increase in disintegration time. It is hydrophobic, and there are many reports in the literature concerning its adverse effect on dissolution rates. The objective of this study was to evaluate the effects of two different concentrations of magnesium stearate on dissolution properties of ranitidine hydrochloride coated tablet formulations labeled to contain 150 mg. The uniformity content was also checked. During the drug formulation development, several samples were designed for choice of the formulation. For this study, two formulations containing 0,77 and 1,1% of magnesium stearate added in the manufacture of cores were chosen. Fraction of ranitidine hydrochloride released in dissolution medium was calculated from calibration curves. The data were analyzed using pharmacopeial test for similarity of dissolution profiles ( f2 equation), previously proposed by Moore and Flanner. Application of f2 equation showed differences in time-course of ranitidine hydrochloride dissolution properties. The obtained values indicate differences in drug release from analyzed ranitidine hydrochloride formulations and could cause differences in therapeutic response. PMID:17848158

  9. 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

    ... 40 Protection of Environment 11 2010-07-01 2010-07-01 true Free Formaldehyde Analysis of...—Free Formaldehyde Analysis of Insulation Resins by Hydroxylamine Hydrochloride 1. Scope This method was... Accuracy Test values should conform to the following statistical precision: Variance = 0.005...

  10. 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.

  11. 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...

  12. 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...

  13. 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...

  14. 21 CFR 524.1484d - Neomycin sulfate, hydrocortisone acetate, tetracaine hydrochloride ear ointment.

    Code of Federal Regulations, 2013 CFR

    2013-04-01

    ... 21 Food and Drugs 6 2013-04-01 2013-04-01 false Neomycin sulfate, hydrocortisone acetate, tetracaine hydrochloride ear ointment. 524.1484d Section 524.1484d Food and Drugs FOOD AND DRUG... sensitize. Care should be taken to observe animals being treated for evidence of hypersensitivity or...

  15. 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... observe animals being treated for evidence of hypersensitivity or allergy to the drug. If such signs...

  16. 21 CFR 524.1484d - Neomycin sulfate, hydrocortisone acetate, tetracaine hydrochloride ear ointment.

    Code of Federal Regulations, 2012 CFR

    2012-04-01

    ... 21 Food and Drugs 6 2012-04-01 2012-04-01 false Neomycin sulfate, hydrocortisone acetate, tetracaine hydrochloride ear ointment. 524.1484d Section 524.1484d Food and Drugs FOOD AND DRUG... sensitize. Care should be taken to observe animals being treated for evidence of hypersensitivity or...

  17. 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...

  18. 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...

  19. 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…

  20. 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...

  1. 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...

  2. 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.

  3. EVALUATION OF THE POTENTIAL CARCINOGENICITY OF 4-CHLORO-O-TOLUIDINE HYDROCHLORIDE

    EPA Science Inventory

    4-Chloro-o-toluidine hydrochloride is a probable human carcinogen, classified as weight-of-evidence Group B2 under the EPA Guidelines for Carcinogen Risk Assessment (U.S. EPA, 1986a). vidence on potential carcinogenicity from animal studies is "Sufficient," and the evidence from ...

  4. 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...

  5. Stability profiles of nepenthesin in urea and guanidine hydrochloride: comparison with porcine pepsin A.

    PubMed

    Kubota, Keiko; Metoki, Yuya; Athauda, Senarath B P; Shibata, Chiaki; Takahashi, Kenji

    2010-01-01

    Nepenthesin, an aspartic endopeptidase from the pitcher fluid of Nepenthes, was found to be markedly less stable than porcine pepsin A when treated with urea or guanidine hydrochloride. This is in sharp contrast with its remarkably high pH/temperature stability as compared with porcine pepsin A. No protein with such a stability profile has been reported to date. PMID:21071863

  6. 21 CFR 524.1662 - Oxytetracycline hydrochloride ophthalmic and topical dosage forms.

    Code of Federal Regulations, 2013 CFR

    2013-04-01

    ... 21 Food and Drugs 6 2013-04-01 2013-04-01 false Oxytetracycline hydrochloride ophthalmic and topical dosage forms. 524.1662 Section 524.1662 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL DRUGS, FEEDS, AND RELATED PRODUCTS OPHTHALMIC AND...

  7. 21 CFR 524.1662 - Oxytetracycline hydrochloride ophthalmic and topical dosage forms.

    Code of Federal Regulations, 2012 CFR

    2012-04-01

    ... 21 Food and Drugs 6 2012-04-01 2012-04-01 false Oxytetracycline hydrochloride ophthalmic and topical dosage forms. 524.1662 Section 524.1662 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL DRUGS, FEEDS, AND RELATED PRODUCTS OPHTHALMIC AND...

  8. 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

  9. 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 ...

  10. 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...

  11. 21 CFR 524.1662b - Oxytetracycline hydrochloride, polymyxin B sulfate ophthalmic ointment.

    Code of Federal Regulations, 2010 CFR

    2010-04-01

    ... 21 Food and Drugs 6 2010-04-01 2010-04-01 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...

  12. 21 CFR 524.1662b - Oxytetracycline hydrochloride, polymyxin B sulfate ophthalmic ointment.

    Code of Federal Regulations, 2013 CFR

    2013-04-01

    ... 21 Food and Drugs 6 2013-04-01 2013-04-01 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...

  13. 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

    ... 40 Protection of Environment 12 2013-07-01 2013-07-01 false 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...

  14. 21 CFR 524.1662b - Oxytetracycline hydrochloride, polymyxin B sulfate ophthalmic ointment.

    Code of Federal Regulations, 2011 CFR

    2011-04-01

    ... 21 Food and Drugs 6 2011-04-01 2011-04-01 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...

  15. 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...

  16. 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,...

  17. 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,...

  18. 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,...

  19. 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,...

  20. 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,...