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Sample records for 4 5 7

  1. 9. (5 X 7 enlargement from 4 X 5 negative) ...

    Library of Congress Historic Buildings Survey, Historic Engineering Record, Historic Landscapes Survey

    9. (5 X 7 enlargement from 4 X 5 negative) FIRST FLOOR, WINDOW MOLDING ON SOUTH WALL LOOKING SOUTH - Sites Homestead, Monongahela National Forest (Tract 390) East of Route 28, Seneca Rocks, Pendleton County, WV

  2. 7 CFR 773.4-773.5 - [Reserved

    Code of Federal Regulations, 2014 CFR

    2014-01-01

    ... 7 Agriculture 7 2014-01-01 2014-01-01 false 773.4-773.5 Section 773.4-773.5 Agriculture Regulations of the Department of Agriculture (Continued) FARM SERVICE AGENCY, DEPARTMENT OF AGRICULTURE SPECIAL PROGRAMS SPECIAL APPLE LOAN PROGRAM §§ 773.4-773.5...

  3. 7 CFR 773.4-773.5 - [Reserved

    Code of Federal Regulations, 2013 CFR

    2013-01-01

    ... 7 Agriculture 7 2013-01-01 2013-01-01 false 773.4-773.5 Section 773.4-773.5 Agriculture Regulations of the Department of Agriculture (Continued) FARM SERVICE AGENCY, DEPARTMENT OF AGRICULTURE SPECIAL PROGRAMS SPECIAL APPLE LOAN PROGRAM §§ 773.4-773.5...

  4. 7 CFR 773.4-773.5 - [Reserved

    Code of Federal Regulations, 2010 CFR

    2010-01-01

    ... 7 Agriculture 7 2010-01-01 2010-01-01 false 773.4-773.5 Section 773.4-773.5 Agriculture Regulations of the Department of Agriculture (Continued) FARM SERVICE AGENCY, DEPARTMENT OF AGRICULTURE SPECIAL PROGRAMS SPECIAL APPLE LOAN PROGRAM §§ 773.4-773.5...

  5. 7 CFR 773.4-773.5 - [Reserved

    Code of Federal Regulations, 2011 CFR

    2011-01-01

    ... 7 Agriculture 7 2011-01-01 2011-01-01 false 773.4-773.5 Section 773.4-773.5 Agriculture Regulations of the Department of Agriculture (Continued) FARM SERVICE AGENCY, DEPARTMENT OF AGRICULTURE SPECIAL PROGRAMS SPECIAL APPLE LOAN PROGRAM §§ 773.4-773.5...

  6. 7 CFR 773.4-773.5 - [Reserved

    Code of Federal Regulations, 2012 CFR

    2012-01-01

    ... 7 Agriculture 7 2012-01-01 2012-01-01 false 773.4-773.5 Section 773.4-773.5 Agriculture Regulations of the Department of Agriculture (Continued) FARM SERVICE AGENCY, DEPARTMENT OF AGRICULTURE SPECIAL PROGRAMS SPECIAL APPLE LOAN PROGRAM §§ 773.4-773.5...

  7. Crystal structure of 2-amino-7,7-dimethyl-5-oxo-4-(pyridin-4-yl)-5,6,7,8-tetrahydro-4 H-chromene-3-carbonitrile hemihydrate

    NASA Astrophysics Data System (ADS)

    Sharma, N.; Banerjee, B.; Brahmachari, G.; Kant, R.; Gupta, V. K.

    2015-12-01

    The title compound, 2-amino-7,7-dimethyl-5-oxo-4-(pyridin-4-yl)-5,6,7,8-tetrahydro-4 Hchromene-3-carbonitrile was synthesized by multicomponent reaction at room temperature using commercially available urea as inexpensive and environmentally benign organo-catalyst. Its structure was determined by X-ray structure analysis. The crystals are monoclinic, sp. gr. C2/ c, a = 22.010(6), b = 11.0364(10), c = 17.147(4) Å, β = 130.37(4)°, Z = 8, R = 0.0433 for 2377 observed reflections.

  8. 7. Photographic copy (reduced to 4 x 5 from 8 ...

    Library of Congress Historic Buildings Survey, Historic Engineering Record, Historic Landscapes Survey

    7. Photographic copy (reduced to 4 x 5 from 8 X 10 black and white paper reproduction in 1941 appraisal by E.E. Malloy at the Engineering Office, Oakland Army Base, California). Photograph taken between June 1940 and January 1941 by unknown photographer. PARTIAL SOUTH ELEVATION OF VEHICLE MAINTENANCE SHOP (BLDG. 99). - Oakland Army Base, Vehicle Maintenance Shop, Attu Street & Corregidor Avenue, Oakland, Alameda County, CA

  9. 7. Photographic copy of photograph (from original 4 x 5 ...

    Library of Congress Historic Buildings Survey, Historic Engineering Record, Historic Landscapes Survey

    7. Photographic copy of photograph (from original 4 x 5 black and white print in the Army Port Contractors' 'Completion Report' at the Engineering Office, Oakland Army Base, California). Photograph taken January 28, 1942 by unknown photographer. AT CENTER RIGHT, SOUTH AND EAST SIDES OBLIQUE VIEW OF POST HEADQUARTERS BUILDING (ADMINISTRATION BUILDING, BLDG. 1) TAKEN FROM EAST SIDE OF MARITIME STREET. - Oakland Army Base, Maritime Street at West Grand Avenue, Oakland, Alameda County, CA

  10. 40 CFR 721.5280 - 2,7-Naphthalenedisulfonic acid, 4-amino-5-hydroxy-, coupled with diazotized 4-butylbenzenamine...

    Code of Federal Regulations, 2014 CFR

    2014-07-01

    ... Specific Chemical Substances § 721.5280 2,7-Naphthalenedisulfonic acid, 4-amino-5-hydroxy-, coupled with... 2,7-naphthalenedisulfonic acid, 4-amino-5-hydroxy-, coupled with diazotized 4-butylbenzenamine... 40 Protection of Environment 31 2014-07-01 2014-07-01 false 2,7-Naphthalenedisulfonic acid,...

  11. 40 CFR 721.5280 - 2,7-Naphthalenedisulfonic acid, 4-amino-5-hydroxy-, coupled with diazotized 4-butylbenzenamine...

    Code of Federal Regulations, 2013 CFR

    2013-07-01

    ... Specific Chemical Substances § 721.5280 2,7-Naphthalenedisulfonic acid, 4-amino-5-hydroxy-, coupled with... 2,7-naphthalenedisulfonic acid, 4-amino-5-hydroxy-, coupled with diazotized 4-butylbenzenamine... 40 Protection of Environment 32 2013-07-01 2013-07-01 false 2,7-Naphthalenedisulfonic acid,...

  12. 40 CFR 721.5280 - 2,7-Naphthalenedisulfonic acid, 4-amino-5-hydroxy-, coupled with diazotized 4-butylbenzenamine...

    Code of Federal Regulations, 2012 CFR

    2012-07-01

    ... Specific Chemical Substances § 721.5280 2,7-Naphthalenedisulfonic acid, 4-amino-5-hydroxy-, coupled with... 2,7-naphthalenedisulfonic acid, 4-amino-5-hydroxy-, coupled with diazotized 4-butylbenzenamine... 40 Protection of Environment 32 2012-07-01 2012-07-01 false 2,7-Naphthalenedisulfonic acid,...

  13. 40 CFR 721.5280 - 2,7-Naphthalenedisulfonic acid, 4-amino-5-hydroxy-, coupled with diazotized 4-butylbenzenamine...

    Code of Federal Regulations, 2010 CFR

    2010-07-01

    ... Specific Chemical Substances § 721.5280 2,7-Naphthalenedisulfonic acid, 4-amino-5-hydroxy-, coupled with... 2,7-naphthalenedisulfonic acid, 4-amino-5-hydroxy-, coupled with diazotized 4-butylbenzenamine... 40 Protection of Environment 30 2010-07-01 2010-07-01 false 2,7-Naphthalenedisulfonic acid,...

  14. 40 CFR 721.5280 - 2,7-Naphthalenedisulfonic acid, 4-amino-5-hydroxy-, coupled with diazotized 4-butylbenzenamine...

    Code of Federal Regulations, 2011 CFR

    2011-07-01

    ... Specific Chemical Substances § 721.5280 2,7-Naphthalenedisulfonic acid, 4-amino-5-hydroxy-, coupled with... 2,7-naphthalenedisulfonic acid, 4-amino-5-hydroxy-, coupled with diazotized 4-butylbenzenamine... 40 Protection of Environment 31 2011-07-01 2011-07-01 false 2,7-Naphthalenedisulfonic acid,...

  15. 40 CFR 721.5262 - 2,7-Naphthalenedisulfonic acid, 5-[[4-chloro-6-[substituted] amino]-1,3,5-triazin-2-yl]amino]-4...

    Code of Federal Regulations, 2010 CFR

    2010-07-01

    ...,7-Naphthalenedisulfonic acid, 5- amino]-1,3,5-triazin-2-yl]amino]-4-hydroxy-3- -, trisodium salt... identified generically as 2,7-Naphthalenedisulfonic acid, 5- amino]-1,3,5-triazin-2-yl]amino]-4-hydroxy-3... 40 Protection of Environment 30 2010-07-01 2010-07-01 false 2,7-Naphthalenedisulfonic acid,...

  16. 40 CFR 721.5262 - 2,7-Naphthalenedisulfonic acid, 5-[[4-chloro-6-[substituted] amino]-1,3,5-triazin-2-yl]amino]-4...

    Code of Federal Regulations, 2013 CFR

    2013-07-01

    ...,7-Naphthalenedisulfonic acid, 5- amino]-1,3,5-triazin-2-yl]amino]-4-hydroxy-3- -, trisodium salt... identified generically as 2,7-Naphthalenedisulfonic acid, 5- amino]-1,3,5-triazin-2-yl]amino]-4-hydroxy-3... 40 Protection of Environment 32 2013-07-01 2013-07-01 false 2,7-Naphthalenedisulfonic acid,...

  17. 40 CFR 721.5262 - 2,7-Naphthalenedisulfonic acid, 5-[[4-chloro-6-[substituted] amino]-1,3,5-triazin-2-yl]amino]-4...

    Code of Federal Regulations, 2012 CFR

    2012-07-01

    ...,7-Naphthalenedisulfonic acid, 5- amino]-1,3,5-triazin-2-yl]amino]-4-hydroxy-3- -, trisodium salt... identified generically as 2,7-Naphthalenedisulfonic acid, 5- amino]-1,3,5-triazin-2-yl]amino]-4-hydroxy-3... 40 Protection of Environment 32 2012-07-01 2012-07-01 false 2,7-Naphthalenedisulfonic acid,...

  18. 40 CFR 721.5262 - 2,7-Naphthalenedisulfonic acid, 5-[[4-chloro-6-[substituted] amino]-1,3,5-triazin-2-yl]amino]-4...

    Code of Federal Regulations, 2011 CFR

    2011-07-01

    ...,7-Naphthalenedisulfonic acid, 5- amino]-1,3,5-triazin-2-yl]amino]-4-hydroxy-3- -, trisodium salt... identified generically as 2,7-Naphthalenedisulfonic acid, 5- amino]-1,3,5-triazin-2-yl]amino]-4-hydroxy-3... 40 Protection of Environment 31 2011-07-01 2011-07-01 false 2,7-Naphthalenedisulfonic acid,...

  19. 4 CFR 7.5 - Adverse actions: Suspensions for 14 days or less.

    Code of Federal Regulations, 2010 CFR

    2010-01-01

    ... therefor, and any order effecting the suspension, together with any supporting material, shall be... 4 Accounts 1 2010-01-01 2010-01-01 false Adverse actions: Suspensions for 14 days or less. 7.5 Section 7.5 Accounts GOVERNMENT ACCOUNTABILITY OFFICE PERSONNEL SYSTEM PERSONNEL RELATIONS AND...

  20. 4 CFR 7.5 - Adverse actions: Suspensions for 14 days or less.

    Code of Federal Regulations, 2012 CFR

    2012-01-01

    ... 4 Accounts 1 2012-01-01 2012-01-01 false Adverse actions: Suspensions for 14 days or less. 7.5... § 7.5 Adverse actions: Suspensions for 14 days or less. (a) Policy. A GAO employee may be suspended for 14 days or less for such cause as will promote the efficiency of GAO (including...

  1. 8 CFR 1236.4 - Removal of S-5, S-6, and S-7 nonimmigrants.

    Code of Federal Regulations, 2011 CFR

    2011-01-01

    ... 8 Aliens and Nationality 1 2011-01-01 2011-01-01 false Removal of S-5, S-6, and S-7 nonimmigrants... OF ALIENS ORDERED REMOVED Detention of Aliens Prior to Order of Removal § 1236.4 Removal of S-5, S-6, and S-7 nonimmigrants. (a) Condition of classification. As a condition of classification and...

  2. 4 CFR 7.5 - Adverse actions: Suspensions for 14 days or less.

    Code of Federal Regulations, 2014 CFR

    2014-01-01

    ... 4 Accounts 1 2014-01-01 2013-01-01 true Adverse actions: Suspensions for 14 days or less. 7.5... § 7.5 Adverse actions: Suspensions for 14 days or less. (a) Policy. A GAO employee may be suspended for 14 days or less for such cause as will promote the efficiency of GAO (including...

  3. 40 CFR 721.5262 - 2,7-Naphthalenedisulfonic acid, 5-[[4-chloro-6-[substituted] amino]-1,3,5-triazin-2-yl]amino]-4...

    Code of Federal Regulations, 2014 CFR

    2014-07-01

    ...,7-Naphthalenedisulfonic acid, 5- amino]-1,3,5-triazin-2-yl]amino]-4-hydroxy-3- -, trisodium salt...-Naphthalenedisulfonic acid, 5- amino]-1,3,5-triazin-2-yl]amino]-4-hydroxy-3- -, trisodium salt (PMN P-00-0803) is...-naphthalenedisulfonic acid, 5- ethyl]amino]-1,3,5-triazin-2-yl]amino]-4-hydroxy-3- -, sodium salt (1:3) (PMN......

  4. 8 CFR 236.4 - Removal of S-5, S-6, and S-7 nonimmigrants.

    Code of Federal Regulations, 2011 CFR

    2011-01-01

    ... 8 Aliens and Nationality 1 2011-01-01 2011-01-01 false Removal of S-5, S-6, and S-7 nonimmigrants... of Aliens Prior to Order of Removal § 236.4 Removal of S-5, S-6, and S-7 nonimmigrants. (a) Condition... section 101(a)(15)(S) of the Act, nonimmigrants in S classification must have executed Form I-854, Part...

  5. Interacting composite fermions: Nature of the 4/5, 5/7, 6/7, and 6/17 fractional quantum Hall states

    NASA Astrophysics Data System (ADS)

    Balram, Ajit C.

    2016-10-01

    Numerical studies by Wójs, Yi, and Quinn have suggested that an unconventional fractional quantum Hall effect is plausible at filling factors ν =1 /3 and 1/5, provided the interparticle interaction has an unusual form for which the energy of two fermions in the relative angular momentum three channel dominates. The interaction between composite fermions in the second Λ level (composite fermion analog of the electronic Landau level) satisfies this property, and recent studies have supported unconventional fractional quantum Hall effect of composite fermions at ν*=4 /3 and 5 /3 , which manifests as fractional quantum Hall effect of electrons at ν =4 /11 , 4/13, 5/13, and 5/17. I investigate in this article the nature of the fractional quantum Hall states at ν =4 /5 , 5/7, 6/17, and 6/7, which correspond to composite fermions at ν*=4 /3 , 5/3, and 6/5, and find that all these fractional quantum Hall states are conventional. The underlying reason is that the interaction between composite fermions depends substantially on both the number and the direction of the vortices attached to the electrons. I also study in detail the states with different spin polarizations at 6/17 and 6/7 and predict the critical Zeeman energies for the spin phase transitions between them. I calculate the excitation gaps at 4/5, 5/7, 6/7, and 6/17 and compare them against recent experiments.

  6. Human 5–HT4 and 5–HT7 Receptor Splice Variants: Are they Important?

    PubMed Central

    Coupar, Ian M; Desmond, Paul V; Irving, Helen R

    2007-01-01

    G-protein-coupled receptors (GPCRs), which are encoded by >300 genes in the human genome, are by far the largest class of targets for modern drugs. These macromolecules display inherent adaptability of function, which is partly due to the production of different forms of the receptor protein. These are commonly called ‘isoforms’ or ‘splice variants’ denoting the molecular process of their production/assembly. Not all GPCRs are expressed as splice variants, but certain subclasses of 5–HT receptors are for example, the 5–HT4 and 5–HT7 receptors. There are at least 11 human 5–HT4 and three h5–HT7 receptor splice variants. This review describestheir discoveries, nomenclature and structures. The discovery that particular splice variants are tissue specific (or prominent) has highlighted their potential as future drug targets. In particular, this review examines the functional relevance of different 5–HT4 and 5–HT7 receptor splice variants. Examples are given to illustrate that splice variants have differential modulatory influences on signalling processes. Differences in agonist potency and efficacies and also differences in desensitisation rates to 5–HT occur with both 5–HT4 and 5–HT7 receptor splice variants. The known and candidate signalling systems that allow for splice variant specific responses include GPCR interacting proteins (GIPs) and GPCR receptor kinases (GRKs) which are examined.Finally, the relevance of 5–HT receptor splice variants to clinical medicine and to the pharmaceutical industry is discussed. PMID:19305739

  7. Aminobenzoic acid diuretics. 7. 3-Substituted 4-phenyl-, 4-arylcarbonyl-, and 4-arylmethyl-5-sulfamoylbenzoic acids and related compounds.

    PubMed

    Nielsen, O B; Bruun, H; Bretting, C; Feit, P W

    1975-01-01

    Various 4-substituted 3-alkylamino-, 3-alkoxy-, 3-alkylthio-, and 3-alkyl-5-sulfamoylbenzoic acids related to known aminobenzoic acid diuretics were synthesized and screened for their diuretic properties in dogs. The tabulated results from a 3-hr test period revealed that generally the diuretic profile and potency could be retained when 3-alkoxy, 3-alkylthio, and 3-phenethyl were substituted for the 3-alkylamino moiety. The high potency of several 3-alkoxy-, 3-alkylthio-, and 3-phenethyl-4-benzoyl-5-sulfamoylbenzoic acids confirmed previous suggestions that the apparent diuretic effect of 4- and 5-alkylamino-6-carboxy-3-phenyl-1,2-benzisothiazole 1,1-dioxides originates from the corresponding 4-benzoyl-5-sulfamoylbenzoic acid derivatives due to an existing equilibrium in plasma. 4-Benzoyl-5-sulfamoyl-3-(3-thenyloxy) benzoic acid (118) is among the most potent benzoic acid diuretics hitherto synthesized and shows significant diuretic activity in dogs at 1 mug/kg. The results obtained with different 3-substituted 4-phenyl-5-sulfamoylbenzoic acids supported the earlier concept regarding the steric influence of the 4-substituent on the diuretic potency of sulfamoylbenzoic acid diuretics.

  8. A toxicological study of 5,6,7,8 tetrafluoro- 1,4-benzodioxin

    SciTech Connect

    London, J.E.

    1988-05-01

    The acute oral LD/sub 50/ values for 5,6,7,8 tetrafluro-1,4 benzodioxin for mice and rats are less than 5 gkg. According to classical guidelines, the material is considered slightly toxic in both species. The sensitization study in the guinea pig did not show the material to have potential sensitizing properties. Skin application studies on the rabbit demonstrated that it was cutaneously mildly irritating. This material was very mildly irritating in the rabbit eye application studies. 4 refs., 2 tabs.

  9. Airborne spectrophotometry of Eta Carinae from 4.5 to 7.5 microns and a model for source morphology

    NASA Technical Reports Server (NTRS)

    Russell, Ray W.; Lynch, David K.; Hackwell, John A.; Rudy, Richard J.; Rossano, George S.; Castelaz, M. W.

    1987-01-01

    Spectrophotometric observations of Eta Car between 4.5 and 7.5 microns show a featureless thermal-like spectrum with no fine-structure lines or broad emission or absorption features. The color temperature of the spectrum is approximately 375 K. High spatial resolution maps at 3.5, 4.8, and 10 microns obtained from the ground are used to discuss the dust distribution and temperature structure, and to present a model for general source morphology. The upper limit to the brightness of the forbidden Ar II fine-structure emission line at 6.98 microns is less than 7 x 10 to the -16th W/sq cm, which still allows for a significant overabundance of argon and is consistent with the evolved nature of the source.

  10. Synthesis and characterization of Ni(II) complex with 5,5,7,12,12,14-hexamethyl-1,4,8,11-tetraazacyclotetradeca-7,14-dienium bromide

    SciTech Connect

    Yusoff, Latifah M.; Yusoff, Siti Fairus M.; Ismail, Wafiuddin; Yamin, Bohari M.

    2014-09-03

    Nickel(II) complex have been synthesized by treating a 14-membered ring tetraaza macrocyclic compound, 5,5,7,12,12,14-hexamethyl-1,4,8,11-tetraazacyclotetradeca-7,14-dienium, bromide (Me{sub 6}N{sub 4}H{sub 4})Br{sub 2} with nickel acetate in metanol. The complex was characterized using elemental analysis, Fourier Transform Infrared (FTIR), Ultraviolet-Visible (UV-Vis), and single crystal diffraction (X-ray). The nickel atom coordinates through four nitrogen atoms in the ligand. Square planar geometry has been proposed for this complex.

  11. A novel one-pot pseudo-five-component synthesis of 4,5,6,7-tetrahydro-1H-1,4-diazepine-5-carboxamide derivatives.

    PubMed

    Shaabani, Ahmad; Maleki, Ali; Mofakham, Hamid; Moghimi-Rad, Jafar

    2008-05-16

    A novel one-pot pseudo-five-component synthesis of 4,5,6,7-tetrahydro-1 H-1,4-diazepine-5-carboxamide derivatives starting from simple and readily available inputs including 2,3-diaminomaleonitrile, a cyclic or acyclic ketone, an isocyanide, and water in the presence of a catalytic amount of p-toluenesulfonic acid in aqueous medium at ambient temperature in high yields is described.

  12. Results of postirradiation examination of the in-pile blockage experiments MOL-7C/4 and MOL-7C/5

    SciTech Connect

    Weimar, P.; Schleisiek, K. )

    1991-10-01

    The Mol-7C in-pile local blockage experiments are performed in the BR-2 reactor at Mol, Belgium as a joint project of Kernforchungszentrum Karlsruhe (KfK) and Studiecentrum voor Kernenergie/Centre d'Etude de l'Energie Nuclearire-Mol. The main objective is to investigate the consequences of local cooling disturbances in liquid-metal-cooled reactor (LMR) fuel subassemblies. In the tests Mol-7C/4 and MOL-7C/5, fuel pins from KNK II are used with a burnup of 5 and 1.7%, respectively. An active central porous blockage is used to simulate the cooling disturbance. During irradiation, the blockage causes significant local damage, including melting of cladding and fuel. Extensive postirradiation examinations (PIE) are performed to investigate the extent of damage. In this paper a description and interpretation of results of the destructive PIE performed at the Hot Cells Laboratory at KfK is given, along with some conclusions related to LMR safety.

  13. The in vitro and in vivo antimalarial activity of some Mannich bases derived from 4-(7'-trifluoromethyl-1',5'-naphthyridin-4'-ylamino)phenol, 2-(7'-trifluoromethyl-quinolin-4'-ylamino)phenol, and 4'-chloro-5-(7''-trifluoromethylquinolin-4''-ylamino)biphenyl -2-ols.

    PubMed

    Barlin, G B; Jiravinyu, C; Butcher, G A; Kotecka, B; Rieckmann, K

    1992-08-01

    A series of di-Mannich base derivatives (4 and 5) from 4-(7'-trifluoromethyl-1',5'-naphthyridin-4'-ylamino)phenol and 2-(7'-trifluoromethylquinolin-4'-ylamino)phenol, respectively, and mono-Mannich base derivatives (6) from 4'-chloro-5-(7''-trifluoromethylquinolin-4''- ylamino)biphenyl-2-ol were assayed for activity against the chloroquine-sensitive (FCQ-27) isolate of cultured Plasmodium falciparum using the inhibition of uptake of radiolabelled hypoxanthine. All seven di-Mannich base derivatives (5) revealed a higher activity than chloroquine, whereas the di-Mannich base derivatives (4) were slightly less active (with some derivatives more active and some less active than chloroquine). The mono-Mannich base derivatives (6) were less active than chloroquine. Comparative tests of selected compounds of (4 and 5) using a morphological assay revealed no significant differences in activity between the chloroquine-sensitive (FCQ-27) and chloroquine-resistant (K-1) isolates. Selected di-Mannich bases (4 and 5) and the mono-Mannich bases 5-7''-bromo (and 7-trifluoromethyl)-1'',5''-naphthyridin-4''-ylamino)-3-(t- butylaminomethyl)-4'-chlorobiphenyl-2-ols (7, X = Br, CF3) markedly suppressed parasitaemia in Plasmodium vinckei vinckei infected mice when administered (i.p.) in a single dose of 200 mg kg-1.

  14. Microstructure, thermal, and mechanical properties of nanostructured Cu-9.5Ni-4.0Sn-7.5P

    NASA Astrophysics Data System (ADS)

    Li, J.; Wang, T. M.

    1995-04-01

    Nanostructured Cu-9.5Ni-4.0Sn-7.5P samples represent a polycrystal microstructure of nanometer-sized α-Cu and Cu3P crystallites for crystallite sizes less than 20 nm and of nanometer-sized α-Cu, Cu3P, and Ni2P crystallites for crystallite sizes greater than 20 nm. The specific heat values between 300 K and 400 K for the nanostructured sample with crystallite size of 10 nm are about 20% higher than for the amorphous sample and about 40% higher than for the coarse-grained sample. The hardness of the nanostructured sample with crystallite size of 10 nm is 30% higher than that of the amorphous sample and 110% higher than that of the coarse-grained sample. The variation in hardness with the crystallite size for the nanostructured samples follows the Hall-Petch relationship.

  15. Comparison of laser ablation and sputter desorption of clusters from Au7Cu5Al4

    NASA Astrophysics Data System (ADS)

    King, B. V.; Moore, J. F.; Cui, Y.; Veryovkin, I. V.; Tripa, C. E.

    2014-12-01

    Ionized and neutral clusters were desorbed from spangold, a polycrystalline ternary alloy with composition Au7Cu5Al4, using both a femtosecond laser beam and an energetic ion beam and the resulting time of flight mass spectra compared. Neutral clusters containing up to 7 atoms were ejected by the 15 keV Ar+ beam whereas only smaller positively and negatively charged clusters were observed from the laser ablated spangold surface. Laser ionization mass spectrometry (LIMS) positive ion spectra were dominated by Al containing cluster ions whereas Au containing ions dominated the negative LIMS spectrum. An odd-even variation in LIMS cluster yield was observed, consistent with previous results and due to fragmentation of photoionized clusters. The laser sputtered neutral mass spectrometry (laser SNMS) spectrum showed that larger desorbed clusters were gold rich. The cluster signals also followed a power law dependence with cluster size with the exponent value of 6-7.6 for sputtered mixed clusters being greater than that found from sputtering of pure elements, similar to the result found previously in the Cu-Au system.

  16. Synthesis, structures, electrochemical studies and antioxidant activity of 5-aryl-4-oxo-3,4,5,8-tetrahydropyrido[2,3-d]pyrimidine-7-carboxylic acids

    NASA Astrophysics Data System (ADS)

    Quiroga, Jairo; Romo, Pablo E.; Ortiz, Alejandro; Isaza, José Hipólito; Insuasty, Braulio; Abonia, Rodrigo; Nogueras, Manuel; Cobo, Justo

    2016-09-01

    The synthesis of 5-aryl-4-oxo-3,4,5,8-tetrahydropyrido[2,3-d]pyrimidine-7-carboxylic acids 3 from the reaction of 6-aminopyrimidines 1 with arylidene derivatives of pyruvic acid 2 under microwave and ultrasound irradiation is described. The orientation of cyclization process was determined by NMR measurements. The methodology provides advantages such as high yields and friendly to the environment without the use of solvents. The antioxidant properties, DPPH free radical scavenging, ORAC, and anodic potential oxidation of the new pyridopyrimidines were studied.

  17. New composite spectra of Mars, 0.4-5.7 μm

    USGS Publications Warehouse

    Erard, Stephane; Calvin, Wendy M.

    1997-01-01

    About 15 areas were observed in the equatorial regions of Mars by the infrared spectrometers IRS (Mariner 6 and 7) and ISM (Phobos-2). The comparison between the spectra shows a remarkable consistency between two data sets acquired 20 years apart and calibrated independently. This similarity demonstrates the accuracy of ISM calibration above 2 μm, except for a possible stray light contribution above 2.6 μm, on the order of ∼1–2% of the solar flux at 2.7 μm. Most differences in spectral shapes are related to differences in spectral/spatial resolution and viewing geometries. No important variation in surface properties is detected, except for a spot in southern Arabia Terra which has a much deeper hydration feature in IRS spectra; differences in viewing geometries and spatial resolutions do not seem to account for this difference that could result from shifting or dehydration of surface materials. Composite spectra of several types of bright and dark materials are computed by modeling the thermal emission and are completed with telescopic spectra in the visible range. Modeled reflectance in the 3.0–5.7 μm range is consistent with basalts and palagonites. The bright regions and analog palagonite spectra are different from hematite in this range, but resemble several phyllosilicates. We infer that (1) although hematite dominates the spectra in the 0.4- to 2.5-μm range, the silicate-clay host is spectrally active beyond 3 μm and can be identified from this domain; (2) phyllosilicates such as montmorillonite or smectite may be abundant components of the martian soils, although the domain below 3 μm lacks the characteristic features of the most usual terrestrial clay minerals.

  18. (3-Methyl-3a,4,7,7a-tetra­hydro-5H-4,7-methano­isoxazolo[4,5-d][1,2]oxazin-5-yl)(phen­yl)methanone

    PubMed Central

    Lough, Alan J.; Nagireddy, Jaipal R.; Tam, William

    2014-01-01

    The title compound, C14H14N2O3, is the exo isomer with a syn arrangement of two O atoms in the isoxazole and oxazine rings. The dihedral angle between the isoxazole and phenyl rings is 60.38 (4)°. In the crystal, weak C—H⋯O hydrogen bonds link the mol­ecules, forming a three-dimensional network. The isoxazole O atom is an acceptor for three of these hydrogen bonds. PMID:24860351

  19. Synthesis, characterization, and crystal structure of 2-amino-7-methyl-5-oxo-4-phenyl-4,5-dihydropyrano[3,2-c] pyran-3-carbonitrile

    SciTech Connect

    Sharma, S.; Banerjee, B.; Brahmachari, G.; Kant, Rajni; Gupta, V. K.

    2015-12-15

    2-Amino-7-methyl-5-oxo-4-phenyl-4,5-dihydropyrano[3,2-c] pyran-3-carbonitrile, C{sub 16}H{sub 12}N{sub 2}O{sub 3} is synthesized via one-pot multi-component reaction at room temperature using commercially available urea as inexpensive and environmentally benign organo-catalyst. Its structure is determined by single-crystal X-ray diffraction technique The crystals are monoclinic, a = 10.7357(12), b = 8.7774(8), c = 15.0759(16) Å, β = 103.575(11)°, Z = 4, sp. gr. P2{sub 1}/n, R = 0.0551 for 1696 observed reflections. The crystal structure is stabilized by N–H···N, C–H···O, and C–H···π interactions.

  20. Synthesis, characterization, and crystal structure of 2-amino-7-methyl-5-oxo-4-phenyl-4,5-dihydropyrano[3,2- c]pyran-3-carbonitrile

    NASA Astrophysics Data System (ADS)

    Sharma, S.; Banerjee, B.; Brahmachari, G.; Kant, Rajni; Gupta, V. K.

    2015-12-01

    2-Amino-7-methyl-5-oxo-4-phenyl-4,5-dihydropyrano[3,2- c]pyran-3-carbonitrile, C16H12N2O3 is synthesized via one-pot multi-component reaction at room temperature using commercially available urea as inexpensive and environmentally benign organo-catalyst. Its structure is determined by single-crystal X-ray diffraction technique The crystals are monoclinic, a = 10.7357(12), b = 8.7774(8), c = 15.0759(16) Å, β = 103.575(11)°, Z = 4, sp. gr. P21/ n, R = 0.0551 for 1696 observed reflections. The crystal structure is stabilized by N-H···N, C-H···O, and C-H···π interactions.

  1. Synthesis of 3-amino-6-methyl-5-ethoxycarbonyl-4,7-dihydrothieno(2,3-b)pyridine derivatives

    SciTech Connect

    Krauze, A.A.; Liepin'sh, E.E.; Pelcher, Yu.E.; Dubur, G.Ya.

    1987-07-01

    The alkylation of piperidinium salts of substituted 1,4-dihydropyridine-2-thiols with chloroacetonitrile or iodoacetamide gave 2-cyanomethylthio- and 2-carbamoylmethylthio-substituted 6-methyl-4-acryl(pyridyl)-5-ethoxycarbonyl-3-cyano-1,4-dihydropyridines, which undergo intramolecular cyclization in basic media to give 3-amino-6-methyl-4-aryl(pyridyl)-5-ethoxycarbonyl-2-cyano(carbamoyl)-4,7-dihydrothieno(2,3-b)pyridines.

  2. Complete Genome Sequences of Krokinobacter sp. 4H-3-7-5 and Lacinutrix sp. 5H-3-7-4, polysaccharide-degrading members of the family Flavobacteriaceae

    SciTech Connect

    Klippel, Dr Barbara; Bruce, David; Davenport, Karen W.; Detter, J C; Goodwin, Lynne A.; Han, James; Han, Shunsheng; Land, Miriam L; Nolan, Matt; Ovchinnikova, Galina; Pennacchio, Len; Pitluck, Sam; Tapia, Roxanne; Walston Davenport, Karen; Woyke, Tanja; Wiebusch, Sigrid; Basner, Alexander; Abe, Fumiyoshi; Horikoshi, Koki; Antranikian, Garabed

    2011-01-01

    Two members of the family Flavobacteriaceae were isolated from deep sea sediments in Japan using artificial seawater and cellulose, xylan and chitin as sole carbon and energy source. Here, we present the finished genome sequence of Krokinobacter sp. 4H-3-7-5 and Lacinutrix sp. 5H-3-7-4 which both encode for putatively novel enzymes involved in cellulose, hemicellulose and chitin degradation.

  3. Complete Genome Sequences of Krokinobactersp. Strain 4H-3-7-5 and Lacinutrixsp. Strain 5H-3-7-4, Polysaccharide-Degrading Members of the Family Flavobacteriaceae▿

    PubMed Central

    Klippel, Barbara; Lochner, Adriane; Bruce, David C.; Walston Davenport, Karen; Detter, Chris; Goodwin, Lynne A.; Han, James; Han, Shunsheng; Hauser, Loren; Land, Miriam L.; Nolan, Matt; Ovchinnikova, Galina; Pennacchio, Len; Pitluck, Sam; Tapia, Roxanne; Woyke, Tanja; Wiebusch, Sigrid; Basner, Alexander; Abe, Fumiyoshi; Horikoshi, Koki; Keller, Martin; Antranikian, Garabed

    2011-01-01

    Two members of the family Flavobacteriaceaewere isolated from subseafloor sediments using artificial seawater with cellulose, xylan, and chitin as the sole carbon and energy sources. Here, we present the complete genome sequences of Krokinobactersp. strain 4H-3-7-5 and Lacinutrixsp. strain 5H-3-7-4, which both encode putatively novel enzymes involved in cellulose, hemicellulose, and chitin metabolism. PMID:21725025

  4. Complete genome sequences of Krokinobacter sp. strain 4H-3-7-5 and Lacinutrix sp. strain 5H-3-7-4, polysaccharide-degrading members of the family Flavobacteriaceae.

    PubMed

    Klippel, Barbara; Lochner, Adriane; Bruce, David C; Davenport, Karen Walston; Detter, Chris; Goodwin, Lynne A; Han, James; Han, Shunsheng; Hauser, Loren; Land, Miriam L; Nolan, Matt; Ovchinnikova, Galina; Pennacchio, Len; Pitluck, Sam; Tapia, Roxanne; Woyke, Tanja; Wiebusch, Sigrid; Basner, Alexander; Abe, Fumiyoshi; Horikoshi, Koki; Keller, Martin; Antranikian, Garabed

    2011-09-01

    Two members of the family Flavobacteriaceae were isolated from subseafloor sediments using artificial seawater with cellulose, xylan, and chitin as the sole carbon and energy sources. Here, we present the complete genome sequences of Krokinobacter sp. strain 4H-3-7-5 and Lacinutrix sp. strain 5H-3-7-4, which both encode putatively novel enzymes involved in cellulose, hemicellulose, and chitin metabolism.

  5. 3-Amino-2-carbamoyl-4,6-diphenyl-4,5- and -4,7-dihydrothieno-(2,3-b)pyridines

    SciTech Connect

    Krauze, A.A.; Liepin'sh, E.E.; Dubur, G.Ya.

    1987-10-01

    The treatment of piperidinium salts of 3-cyano-1,4-dihydropyridine-2-thiols with alkyl halides leads to 2-alkylthio-3-cyano-1,4-dihydropyridines. The authors have shown that alkylation of the piperidinium salt of 4,6-diphenyl-3-cyano-1,4-dihydropyridine-2-thiol with iodoacetamide gives carbamoylmethylthio derivative II, which, by the action of an equimolar amount of a base with heating to 50-60/sup 0/C, gives a mixture of 3-amino-2-carbamoyl-4,6-diphenyl-4,7-dihydrothieno(2,3-b)pyridine and 3-amino-2-carbamoyl-4,6-diphenyl-4,5-dihydrothieno(2,3-b)-pyridine in a ratio of 1:1. In the presence of excess base the principal product is IV. It was established by PMR spectroscopy that dihydropyridine II initially undergoes cyclization to 4,7-dihydrothienopyridine III, which then undergoes isomerization to 4,5-dihydrothienopyridine IV. Acidification of a solution of IV in d/sub 6/-DMSO gives rise to reverse isomerization.

  6. Synthesis of [3 alpha-3H]7-dehydrocholesterol via stable tritiated 4-phenyl-1,2,4-triazoline-3,5-dione derivative.

    PubMed

    Batta, A K; Salen, G; Tint, G S; Honda, A; Shefer, S

    1997-11-01

    Synthesis of [3 alpha-3H]7-dehydrocholesterol is described via protection of the 5,7-diene system in 7-dehydrocholesterol as the Diels-Alder adduct with 4-phenyl-1,2,4-triazoline-3,5-dione followed by oxidation of the hydroxyl group to give the 3-oxo adduct. Reduction of the keto adduct with [3H]sodium borohydride produced the adduct of [3 alpha-3H]7-dehydrocholesterol from which the radiolabeled sterol was obtained via treatment with lithium aluminum hydride. The advantage of the method is that highly labeled [3 alpha-3H]7-dehydrocholesterol can be prepared. Further, unlike 7-dehydrocholesterol, its adduct with 4-phenyl-1,2,4-triazoline-3,5-dione is stable and can be stored. This allows the preparation of small batches of [3 alpha-3H]7-dehydrocholesterol for immediate use in biological experiments, and losses due to decomposition of excess radiolabeled 7-dehydrocholesterol are minimized.

  7. Anti-platelet activity of erythro-(7S,8R)-7-acetoxy-3,4,3',5'-tetramethoxy-8-O-4'-neolignan from Myristica fragrans.

    PubMed

    Kang, Jung Won; Min, Byung-Sun; Lee, Jeong-Hyung

    2013-11-01

    Platelets play a critical role in pathogenesis of cardiovascular disorders and strokes. The inhibition of platelet function is beneficial for the treatment and prevention of these diseases. In this study, we investigated the anti-platelet activity of erythro-(7S,8R)-7-acetoxy-3,4,3',5'-tetramethoxy-8-O-4'-neolignan (EATN), a neolignan isolated from Myristica fragrans, using human platelets. EATN preferentially inhibited thrombin- and platelet-activating factor (PAF)-induced platelet aggregation without affecting platelet damage in a concentration-dependent manner with IC50 values of 3.2 ± 0.4 and 3.4 ± 0.3 μM, respectively. However, much higher concentrations of EATN were required to inhibit platelet aggregation induced by arachidonic acid. EATN also inhibited thrombin-induced serotonin and ATP release, and thromboxane B2 formation in human platelets. Moreover, EATN caused an increase in cyclic AMP (cAMP) levels and attenuated intracellular Ca(2+) mobilization in thrombin-activated human platelets. Therefore, we conclude that the inhibitory mechanism of EATN on platelet aggregation may increase cAMP levels and subsequently inhibit intracellular Ca(2+) mobilization by interfering with a common signaling pathway rather than by directly inhibiting the binding of thrombin or PAF to their receptors. This is the first report of the anti-platelet activity of EATN isolated from M. fragrans.

  8. Metabolism of 4-Hydroxy-7-oxo-5-heptenoic Acid (HOHA) Lactone by Retinal Pigmented Epithelial Cells.

    PubMed

    Wang, Hua; Linetsky, Mikhail; Guo, Junhong; Yu, Annabelle O; Salomon, Robert G

    2016-07-18

    4-Hydroxy-7-oxo-5-heptenic acid (HOHA)-lactone is a biologically active oxidative truncation product released (t1/2 = 30 min at 37 °C) by nonenzymatic transesterification/deacylation from docosahexaenoate lipids. We now report that HOHA-lactone readily diffuses into retinal pigmented epithelial (RPE) cells where it is metabolized. A reduced glutathione (GSH) Michael adduct of HOHA-lactone is the most prominent metabolite detected by LC-MS in both the extracellular medium and cell lysates. This molecule appeared inside of ARPE-19 cells within seconds after exposure to HOHA-lactone. The intracellular level reached a maximum concentration at 30 min and then decreased with concomitant increases in its level in the extracellular medium, thus revealing a unidirectional export of the reduced GSH-HOHA-lactone adduct from the cytosol to extracellular medium. This metabolism is likely to modulate the involvement of HOHA-lactone in the pathogenesis of human diseases. HOHA-lactone is biologically active, e.g., low concentrations (0.1-1 μM) induce secretion of vascular endothelial growth factor (VEGF) from ARPE-19 cells. HOHA-lactone is also a precursor of 2-(ω-carboxyethyl)pyrrole (CEP) derivatives of primary amino groups in proteins and ethanolamine phospholipids that have significant pathological and physiological relevance to age-related macular degeneration (AMD), cancer, and wound healing. Both HOHA-lactone and the derived CEP can contribute to the angiogenesis that defines the neovascular "wet" form of AMD and that promotes the growth of tumors. While GSH depletion can increase the lethality of radiotherapy, because it will impair the metabolism of HOHA-lactone, the present study suggests that GSH depletion will also increase levels of HOHA-lactone and CEP that may promote recurrence of tumor growth.

  9. 4-Hydroxy-7-oxo-5-heptenoic Acid Lactone Induces Angiogenesis through Several Different Molecular Pathways.

    PubMed

    Guo, Junhong; Linetsky, Mikhail; Yu, Annabelle O; Zhang, Liang; Howell, Scott J; Folkwein, Heather J; Wang, Hua; Salomon, Robert G

    2016-12-19

    Oxidative stress and angiogenesis have been implicated not only in normal phenomena such as tissue healing and remodeling but also in many pathological processes. However, the relationships between oxidative stress and angiogenesis still remain unclear, although oxidative stress has been convincingly demonstrated to influence the progression of angiogenesis under physiological and pathological conditions. The retina is particularly susceptible to oxidative stress because of its intensive oxygenation and high abundance of polyunsaturated fatty acyls. In particular, it has high levels of docosahexanoates, whose oxidative fragmentation produces 4-hydroxy-7-oxo-5-heptenoic acid lactone (HOHA-lactone). Previously, we found that HOHA-lactone is a major precursor of 2-(ω-carboxyethyl)pyrrole (CEP) derivatives, which are tightly linked to age-related macular degeneration (AMD). CEPs promote the pathological angiogenesis of late-stage AMD. We now report additional mechanisms by which HOHA-lactone promotes angiogenesis. Using cultured ARPE-19 cells, we observed that HOHA-lactone induces secretion of vascular endothelial growth factor (VEGF), which is correlated to increases in reactive oxygen species and decreases in intracellular glutathione (GSH). Wound healing and tube formation assays provided, for the first time, in vitro evidence that HOHA-lactone induces the release of VEGF from ARPE-19 cells, which promotes angiogenesis by human umbilical vein endothelial cells (HUVEC) in culture. Thus, HOHA-lactone can stimulate vascular growth through a VEGF-dependent pathway. In addition, results from MTT and wound healing assays as well as tube formation experiments showed that GSH-conjugated metabolites of HOHA-lactone stimulate HUVEC proliferation and promote angiogenesis in vitro. Previous studies demonstrated that HOHA-lactone, through its CEP derivatives, promotes angiogenesis in a novel Toll-like receptor 2-dependent manner that is independent of the VEGF receptor or VEGF

  10. Antimalarial activity of Mannich bases derived from 4-(7'-bromo-1',5'-naphthyridin-4'-ylamino)phenol and 4-(7'-trifluoromethylquinolin-4'-ylamino)phenol against Plasmodium falciparum in vitro.

    PubMed

    Scott, H V; Tan, W L; Barlin, G B

    1987-04-01

    Mono- and di-Mannich bases derived from 4-(7'-bromo-1',5'-naphthyridin-4'-ylamino)phenol and 4-(7'-trifluoromethylquinolin-4'-ylamino)phenol were assayed for antimalarial activity (using an in vitro radioisotopic technique) against two isolates of Plasmodium falciparum. Many from these two series of compounds had an IC50 value (concentration of compound causing 50% inhibition of 3H-hypoxanthine incorporation) comparable to or better than those of mefloquine and amodiaquine, for both a chloroquine-sensitive isolate (FCQ-27) and the chloroquine-resistant isolate (K1). At least one compound, 2,6-bis (piperidin-1''-ylmethyl)-4-(7'-trifluoromethylquinolin -4'-ylamino)phenol (TN112), showed significant superior activity to the three antimalarials chloroquine, mefloquine and amodiaquine against both isolates. (Statistically superior activity compared to these three antimalarials was found for TN112, except that against the K1 isolate its activity was just outside the range of significance relative to mefloquine.) Some of the 7-bromo-1,5-naphthyridine Mannich bases were appreciably less toxic in mice than amodiaquine.

  11. Synergistic effect of 2,2',4,4',5,5'-hexachlorobiphenyl and 2,3,7,8-tetrachlorodibenzo-p-dioxin on hepatic porphyrin levels in the rat.

    PubMed Central

    van Birgelen, A P; Fase, K M; van der Kolk, J; Poiger, H; Brouwer, A; Seinen, W; van den Berg, M

    1996-01-01

    We studied the effect of polychlorinated biphenyls (PCBs) on hepatic porphyrin accumulation in female Sprague-Dawley rats by feeding them diets containing 2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD), 2,2',4,4',5,5'-hexachlorobiphenyl (PCB 153), 2,3,3',4,4',5-hexachlorobiphenyl (PCB 156), 3,3',4,4',5-pentachlorobiphenyl (PCB 126), or combinations of the single PCB congeners with TCDD for 13 weeks. A dose-dependent increase in hepatic porphyrin accumulation occurred after TCDD, PCB 126, or PCB 156 administration, reaching maximal levels of about twice control values. The lowest dose levels for which a significant increase in hepatic porphyrin accumulation was found were 0.7 microgram TCDD/kg diet, 50 micrograms PCB 126/kg diet, or 6 mg PCB 156/kg diet. These doses are equivalent to 47 ng TCDD/kg/day, 3.2 micrograms PCB 126/kg/day, and 365 micrograms PCB 156/kg/day. Relative potencies for hepatic porphyrin accumulation, using TCDD as a reference, ranged from 0.015 to 0.06 for PCB 126 and from 0.0001 to 0.0003 for PCB 156. CYP1A2 activities significantly correlated with hepatic porphyrin levels, with coefficients of 0.629, 0.483, or 0.808 for TCDD, PCB 126, or PCB 156, respectively. Administration of PCB 153 alone did not result in hepatic porphyrin accumulation. Co-administration of PCB 153 and TCDD revealed a strong synergistic effect on porphyrin accumulation (about 800 times control levels). This synergistic effect was significant in rats fed diets containing any combination of PCB 153 with TCDD. Uroporphyrin III and heptacarboxylic porphyrin were accumulated in porphyrinogenic livers. These results suggest that TCDD induction of CYP1A2 may be involved, leading to oxidation of uroporphyrinogen III to uroporphyrin III, in combination with an increase in delta-aminolevulinic acid synthetase induced by PCB 153. Under porphyrinogenic conditions, an inhibitor of CYP1A2 activity may also be formed. The interactive effects on porphyrin accumulation after co

  12. PLC-mediated PI(4,5)P2 hydrolysis regulates activation and inactivation of TRPC6/7 channels.

    PubMed

    Itsuki, Kyohei; Imai, Yuko; Hase, Hideharu; Okamura, Yasushi; Inoue, Ryuji; Mori, Masayuki X

    2014-02-01

    Transient receptor potential classical (or canonical) (TRPC)3, TRPC6, and TRPC7 are a subfamily of TRPC channels activated by diacylglycerol (DAG) produced through the hydrolysis of phosphatidylinositol 4,5-bisphosphate (PI(4,5)P2) by phospholipase C (PLC). PI(4,5)P2 depletion by a heterologously expressed phosphatase inhibits TRPC3, TRPC6, and TRPC7 activity independently of DAG; however, the physiological role of PI(4,5)P2 reduction on channel activity remains unclear. We used Förster resonance energy transfer (FRET) to measure PI(4,5)P2 or DAG dynamics concurrently with TRPC6 or TRPC7 currents after agonist stimulation of receptors that couple to Gq and thereby activate PLC. Measurements made at different levels of receptor activation revealed a correlation between the kinetics of PI(4,5)P2 reduction and those of receptor-operated TRPC6 and TRPC7 current activation and inactivation. In contrast, DAG production correlated with channel activation but not inactivation; moreover, the time course of channel inactivation was unchanged in protein kinase C-insensitive mutants. These results suggest that inactivation of receptor-operated TRPC currents is primarily mediated by the dissociation of PI(4,5)P2. We determined the functional dissociation constant of PI(4,5)P2 to TRPC channels using FRET of the PLCδ Pleckstrin homology domain (PHd), which binds PI(4,5)P2, and used this constant to fit our experimental data to a model in which channel gating is controlled by PI(4,5)P2 and DAG. This model predicted similar FRET dynamics of the PHd to measured FRET in either human embryonic kidney cells or smooth muscle cells, whereas a model lacking PI(4,5)P2 regulation failed to reproduce the experimental data, confirming the inhibitory role of PI(4,5)P2 depletion on TRPC currents. Our model also explains various PLC-dependent characteristics of channel activity, including limitation of maximum open probability, shortening of the peak time, and the bell-shaped response of total

  13. Process for manufacturing bis(2-methoxyethyl)-2,3,6,7-tetracyano-1,4,5,8,9,10-hexazaanthracene

    DOEpatents

    Rasmussen, Paul George; Lawton, Richard Graham

    2014-06-03

    A process to manufacture substituted tetracyano-hexaazatricyclics with the substitutions occurring at the 9 and 10 hydrogens. The process begins with 2,3-dichloro-5,6-dicyanopyrazine, which is reacted to form the desired tetracyano-hexaazatricyclic. Different process embodiments enable different reaction paths to the desired tetracyano-hexaazatricyclic. Different tetracyano-hexaazatricyclic embodiments include bis(2-methoxyethyl)-2,3,6,7-tetracyano-1,4,5,8,9,10-hexazaanthracene and bis(2-methoxyethoxyethyl)-2,3,6,7-tetracyano-1,4,5,8,9,10-hexazaanthracen- e.

  14. (Eco)toxicological effects of 2,4,7,9-tetramethyl-5-decyne-4,7-diol (TMDD) in zebrafish (Danio rerio) and permanent fish cell cultures.

    PubMed

    Vincze, Krisztina; Gehring, Martin; Braunbeck, Thomas

    2014-01-01

    2,4,7,9-tetramethyl-5-decyne-4,7-diol (TMDD) is a high-production volume chemical used in paper, ink, pesticide, and adhesive industries as a wetting and anti-foaming agent. The physicochemical properties and slow biodegradation rate of TMDD indicate a low bioaccumulation potential but a high prevalence in the environment. As a consequence, TMDD has been detected in several European rivers in the nanogram per liter and lower microgram per liter range; however, its environmental risk to aquatic organisms is considered low. Recent studies almost exclusively focused on acute effects by TMDD, little is known about cytotoxic and genotoxic effects, reproduction and developmental toxicity, endocrine disruption, and any kind of long-term toxicity and carcinogenicity so far. The present study aims to provide more specific baseline information on the ecotoxicological effects of TMDD in fish. For this end, cyto- and genotoxicity assays were carried out in vitro with the permanent fish cell line RTL-W1; in addition, in vivo studies were conducted with the early life stages of zebrafish (Danio rerio) in order to fill the data gaps in developmental toxicity and endocrine disruption. TMDD showed a cytotoxic and slight genotoxic potential in fish cell lines; moreover, various sublethal and lethal effects could be detected in developing zebrafish embryos. There was no evidence of endocrine-disrupting effects by TMDD; however, mortality following prolonged exposure to TMDD during fish sexual development test was clearly higher than mortality in the fish embryo test after 96-h exposure. Our results thus confirmed previous findings of laboratory screening tests, suggesting short-term toxic effects of TMDD in the intermediate, and long-term effects in the lower milligram per liter range.

  15. Two new isoflavone 7-O-α-4″-anhydro-4″,5″-didehydroglucuronides from Streptomyces sp. LZ35ΔgdmAI.

    PubMed

    Deng, Jing-Jing; Lu, Chun-Hua

    2016-01-01

    Two isoflavone 7-O-α-4″-anhydro-4″,5″-didehydroglucuronides, namely daidzein 7-O-α-4″-anhydro-4″,5″-didehydroglucuronide (1) and genistein 7-O-α-4″-anhydro-4″,5″-didehydroglucuronide (2), were isolated and identified from the mutant strain of Streptomyces sp. LZ35ΔgdmAI. Their structures were elucidated by the analysis of their high resolution mass spectrometry (HR-MS) and 1D, 2D Nuclear magnetic Resonance (NMR) spectroscopic data. They are new natural products and maybe the transformed products of the soybean meal by Streptomyces sp. LZ35ΔgdmAI.

  16. 5,7-dihydroxy-2-(3-hydroxy-4, 5-dimethoxy-phenyl)-chromen-4-one-a flavone from Bruguiera gymnorrhiza displaying anti-inflammatory properties

    PubMed Central

    Barik, Rajib; Sarkar, Ratul; Biswas, Prova; Bera, Rammohan; Sharma, Soma; Nath, Suvadeep; Karmakar, Sanmoy; Sen, Tuhinadri

    2016-01-01

    Objective: Bruguiera gymnorrhiza (BRG) (L.) Lamk (Rhizophoraceae), a mangrove species, is widely distributed in the Pacific region, eastern Africa, Indian subcontinent, and subtropical Australia. The leaves of this plant are traditionally used for treating burns and inflammatory lesions. This study isolates the bioactive compound from the methanol extract of BRG leaves and evaluates the possible mechanisms of anti-inflammatory activity involved. Materials and Methods: Bioassay-guided fractionation of BRG was performed to identify the bioactive fraction (displaying inhibition of cyclooxygenase 2 [COX2] - 5-lipoxygenase (5-LOX) activities and tumor necrosis factor-alpha (TNF-α) production at the tested concentrations of 100 and 10 μg/ml). The fractionation was performed by solvent extraction and preparative high-performance liquid chromatography. The bioactive compound was characterized by ultraviolet–visible, liquid chromatography–mass spectrometry and nuclear magnetic resonance spectroscopy. The antioxidant potential was evaluated by electron spin resonance spectrum of 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical at 250 μM. The effect of the compound was also studied on TNF-α converting enzyme and nuclear factor kappa B (NF-κB) activities at the concentrations 100, 10 and 1 μg/ml. Results: Bioassay-guided purification of BRG revealed the presence of a flavone (5,7-dihydroxy-2- [3-hydroxy-4,5-dimethoxy-phenyl]-chromen-4-one) of molecular weight 330Da. It demonstrated more than 80% inhibition against COX2, 5-LOX activities and TNF-α production at 100 μg/ml. It also displayed 40% inhibition against DPPH radical at the tested concentration along with 23.1% inhibition of NF-κB activity at 100 μg/ml. Conclusions: The isolated methoxy-flavone may play a predominant role in the anti-inflammatory properties displayed by BRG leaves. Such activity may involve multiple mechanisms, namely (a) modulation of oxidative stress (b) inhibition of arachidonic acid

  17. Synthesis of 5-chloroformycin A, 5-chloro-2'-deoxyformycin A and certain related 5,7-disubstituted 3-beta-D-ribofuranosylpyrazolo[4,3-d] pyrimidines from formycin A.

    PubMed Central

    Upadhya, K G; Sanghvi, Y S; Robins, R K; Revankar, G R; Ugarkar, B G

    1986-01-01

    A facile synthesis of 7-amino-5-chloro-3-beta-D-ribofuranosylpyrazolo [4,3-d]pyrimidine (5-chloroformycin A, 6), 7-amino-5-chloro-3-(2-deoxy-beta-D-erythro-pentofuranosyl) pyrazolo [4,3-d]-pyrimidine (5-chloro-2'-deoxyformycin A, 13) and certain related 5,7-disubstituted pyrazolo[4,3-d]pyrimidine ribonucleosides is described starting with formycin A. Thiation of tri-O-acetyloxoformycin B (4b) with phosphorus pentasulfide, followed 3-beta-D-ribofuranosyl-7-thioxopyrazolo[4,3-d] pyrimidin-5(1H,4H,6H)-one (3b) in excellent yield. Chlorination of 4b with either phosphorus oxychloride or phenyl phosphonicdichloride furnished the key intermediate 5,7-dichloro-3-(2,3, 5-tri-O-acetyl-beta-D-ribofuranosyl)pyrazolo[4,3-d]pyrimidine (5a), which on deacetylation afforded 5,7-dichloro-3-beta-D-ribofuranosylpyrazolo [4,3-d]pyrimidine (5b). Ammonolysis of 5a with liquid ammonia gave 6, whereas with MeOH/NH3, a mixture of 6 and 7-methoxy-5-chloro-3-beta-D-ribofuranosylpyrazolo[4,3-d]pyrimidine (7) was obtained. Reaction of 6 with lithium azide and subsequent hydrogenation afforded 5-aminoformycin A (10). Treatment of 5a with thiourea gave 5-chloro-3-(2,3,5-tri-O-acetyl-beta-D-ribofuranosyl) pyrazolo[4,3-d]pyrimidine-7(1H,6H)-thione (8a), which on further reaction with sodium hydrosulfide furnished 3-beta-D-ribofuranosylpyrazolo [4,3-d]pyrimidine-5,7(1H,4H,6H)-dithione (11). The four-step deoxygenation procedure using phenoxythiocarbonylation of the 2'-hydroxy group of the 3', 5'-protected 6 gave 5-chloro-2'-deoxyformycin A (13). PMID:3951995

  18. An Efficient Solution-Phase Synthesis of 4,5,7-Trisubstituted Pyrrolo[3,2-d]pyrimidines

    PubMed Central

    Zhang, Weihe; Liu, Jing; Stashko, Michael A.; Wang, Xiaodong

    2013-01-01

    We have developed an efficient and robust route to synthesize 4,5,7-trisubstituted pyrrolo[3,2-d]pyrimidines as potent kinase inhibitors. This solution-phase synthesis features a SNAr substitution reaction, cross-coupling reaction, one-pot reduction/reductive amination and N-alkylation reaction. These reactions occur rapidly with high yields and have broad substrate scopes. A variety of groups can be selectively introduced into the N5 and C7 positions of 4,5,7-trisubstituted pyrrolopyrimidines at a late stage of the synthesis, thereby providing a highly efficient approach to explore the structure-activity relationships of pyrrolopyrimidine derivatives. Four synthetic analogs have been profiled against a panel of 48 kinases and a new and selective FLT3 inhibitor 9 is identified. PMID:23181516

  19. (Y0.5In0.5)Ba(Co,Zn)4O7 cathodes with superior high-temperature phase stability for solid oxide fuel cells

    SciTech Connect

    Young Nam, Kim; Kim, Jung-Hyun; Paranthaman, Mariappan Parans; Manthiram, Arumugam; Huq, Ashfia

    2012-01-01

    (Y0.5In0.5)BaCo4-xZnxO7 (1.0 x 2.0) oxides crystallizing in a trigonal P31c structure have been synthesized and explored as cathode materials for solid oxide fuel cells (SOFC). At a given Zn content, the (Y0.5In0.5)BaCo4-xZnxO7 sample with 50 % Y and 50 % In exhibits much improved phase stability at intermediate temperatures (600 - 800 oC) compared to the samples with 100 % Y or In. However, the substitution of Zn for Co in (Y0.5In0.5)Ba(Co4-xZnx)O7 (1.0 x 2.0) decreases the amount of oxygen loss on heating, total electrical conductivity, and cathode performance in SOFC while providing good long-term phase stability at high temperatures. Among the various chemical compositions investigated in the (Y0.5In0.5)Ba(Co4-xZnx)O7 system, the (Y0.5In0.5)BaCo3ZnO7 sample offers a combination of good electrochemical performance and low thermal expansion coefficient (TEC) while maintaining superior phase stability at 600 800 oC for 100 h. Fuel cell performances of the (Y0.5In0.5)Ba(Co3Zn)O7 + Ce0.8Gd0.2O1.9 (GDC) (50 : 50 wt. %) composite cathodes collected with anode-supported single cell reveal a maximum power density value of 521 mW cm-2 at 700 oC.

  20. Synthesis, in vitro antimycobacterial evaluation and docking studies of some new 5,6,7,8-tetrahydropyrido[4',3':4,5]thieno[2,3-d]pyrimidin-4(3H)-one schiff bases.

    PubMed

    Malothu, Narender; Bhandaru, Jaswanth S; Kulandaivelu, Umasankar; Jojula, Malathi; Adidala, Raghuram Reddy; K R, Umadevi; A V N, Dusthackeer; Kaki, Venkat Rao; Akkinepally, Raghuram R

    2016-02-01

    Development of multidrug resistant (MDR) and extensively drug resistant (XDR) tuberculosis (TB) has been considered as major health burden, globally. In order to develop novel, potential molecules against drug resistant TB, twenty two (22) new 3-substituted-7-benzyl-5,6,7,8-tetrahydropyrido[4',3':4,5]thieno[2,3-d]pyrimidin-4(3H)-one (6a-k) and 3-substituted-7-benzyl-2-methyl-5,6,7,8-tetrahydropyrido[4',3':4,5]thieno[2,3-d]pyrimidin-4(3H)-one (7a-k) derivatives were designed and synthesized by using appropriate synthetic protocols. Pantothenate synthetase (PS) was considered as the target for the molecular docking studies and evaluated the binding pattern at active site, as PS plays a significant role in the biosynthesis of pantothenate in Mycobacterium tuberculosis (MTB). The preliminary in vitro antibacterial screening of test compounds was carried out against two strains of Gram-positive (Bacillus subtilis and Staphylococcus aureus) and Gram-negative (Escherichia coli and Klebsiella pneumoniae) bacteria. The antimycobacterial screening was performed against MTB H37Rv and an isoniazid-resistant clinical isolate of MTB. The compounds 6b, 6c, 6d, 6k, 7b, 7c, 7d and 7k exhibited promising antibacterial activity MIC in the range of 15-73 μM against all bacterial strains used and compounds 6d and 7b showed antimycobacterial activity (IC50 <340 μM in LRP assay) and (MIC <9 μM in broth microdilution method).

  1. Extensive theoretical studies on two new members of the FOX-7 family: 5-(dinitromethylene)-1,4-dinitramino-tetrazole and 1,1'-dinitro-4,4'-diamino-5,5'-bitetrazole as energetic compounds.

    PubMed

    He, Piao; Zhang, Jian-Guo; Wang, Kun; Yin, Xin; Jin, Xin; Zhang, Tong-Lai

    2015-02-28

    Two novel compounds 5-(dinitromethylene)-1,4-dinitramino-tetrazole (DNAT) and 1,1'-dinitro-4,4'-diamino-5,5'-bitetrazole (DNABT) were suggested to be potential candidates of high energy density materials (HEDMs). The optimized geometry, NBO charges and electronic density, HOMO-LUMO, electrostatic potential on the surface of molecules, the IR spectrum and thermochemical parameters were calculated for inspecting the electronic structure properties at B3LYP/6-311++G** level of theory. Meanwhile, the solid states of DNAT and DNABT were studied using the crystal packing models by the plane-wave periodic local-density approximation density functional theory. Four stable polymorphous cells have been found including P212121, P21/c, P1̄ and Pbca, assigned to the orthorhombic, monoclinic and triclinic lattice systems. In addition, properties such as density, enthalpy of formation and detonation performance have also been predicted. As a result, the detonation velocity and pressure of two compounds are found to be very remarkable (DNAT: D = 9.17 km s(-1), P = 39.23 GPa; DNABT: D = 9.53 km s(-1), P = 40.92 GPa). Considering the tetrazole rings with energetic groups and the insensitive fragment of FOX-7, high positive heat of formation (583.50 kJ mol(-1) and 1081.39 kJ mol(-1)) and eminent performance render DNAT and DNABT to be very promising powerful energetically insensitive compounds. This work provides theoretical support for further experimental synthesis.

  2. Synthesis, spectroscopic characterization, X-ray structure and DFT studies on 4-(2-hydroxyphenyl)-4,5,6,7-tetrahydro-1H-imidazo[4,5-c]pyridin-5-ium chloride hydrate.

    PubMed

    Türkyılmaz, Murat; Özdemir, Namık; Baran, Yakup

    2011-11-01

    The title molecular salt, 4-(2-hydroxyphenyl)-4,5,6,7-tetrahydro-1H-imidazo[4,5-c]pyridin-5-ium chloride hydrate (C(12)H(14)N(3)O(+)·Cl-·H(2)O), was synthesized and characterized by IR-NMR spectroscopy and single-crystal X-ray diffraction. In addition to the molecular geometry from X-ray experiment, the molecular geometry, vibrational frequencies and gauge-independent atomic orbital (GIAO) (1)H and (13)C NMR chemical shift values of the title compound in the ground state have been calculated using the density functional theory (DFT/B3LYP) method with the 6-31++G(d,p) and 6-311++G(d,p) basis sets, and compared with the experimental data. Besides, molecular electrostatic potential (MEP) distribution and non-linear optical properties of the title compound were investigated by theoretical calculations at the B3LYP/6-311++G(d,p) level.

  3. Late Alk4/5/7 signaling is required for anterior skeletal patterning in sea urchin embryos.

    PubMed

    Piacentino, Michael L; Ramachandran, Janani; Bradham, Cynthia A

    2015-03-01

    Skeletal patterning in the sea urchin embryo requires a conversation between the skeletogenic primary mesenchyme cells (PMCs) and the overlying pattern-dictating ectoderm; however, our understanding of the molecular basis for this process remains incomplete. Here, we show that TGF-β-receptor signaling is required during gastrulation to pattern the anterior skeleton. To block TGF-β signaling, we used SB431542 (SB43), a specific inhibitor of the TGF-β type I receptor Alk4/5/7. Treatment with SB43 during gastrulation blocks anterior PMC positioning and the formation of the anterior skeleton, but does not perturb general ectoderm specification or development. This is the first example of a signaling event required for patterning of a specific part of the skeleton. Alk4/5/7 inhibition does not prevent the formation of a mouth, although SB43-treated plutei display reduced feeding ability, presumably due to the loss of the structural support for the mouth conferred by the anterior skeleton. Both Univin and Nodal are potential ligands for Alk4/5/7; however, Nodal is unilaterally expressed on only the right side, whereas Univin is bilaterally expressed in the ectoderm adjacent to the anterior skeleton during the relevant time period. Our results demonstrate that Univin is both necessary and sufficient for secondary skeletal development in a control background, consistent with the hypothesis that Univin is a relevant Alk4/5/7 ligand for anterior skeletal patterning. Taken together, our data demonstrate that Alk4/5/7 signaling during gastrulation is required to direct PMCs to the oral hood, and suggest that Univin is a relevant ligand for this signaling event.

  4. Skin tumor initiating ability of benzo(a)pyrene 4,5- 7,5- and 7,8-diol-9,10-epoxides and 7,8-diol.

    PubMed

    Slaga, T J; Viaje, A; Betty, D L; Brachen, W; Buty, S G; Scribner, J D

    1976-11-01

    The skin tumor initiating abilities of both K-region and non-K-region epoxides of benzo(a)pyrene(BP) were determined in mice using a two-stage system of tumorigenesis. BP-4,5-epoxide and BP-7,8-dihydrodiol-9,10-epoxide (anti) were found to be weak tumor initiators whereas BP-7,8-epoxide had about a third of the activity as the parent hydrocarbon, BP. However, the 7,8-dihydrodiol of BP was found to be approximately as potent as BP suggesting that it may be a proximate carcinogen.

  5. Thermal Infrared Radiometric Calibration of the Entire Landsat 4, 5, and 7 Archive (1982-2010)

    NASA Technical Reports Server (NTRS)

    Schott, John R.; Hook, Simon J.; Barsi, Julia A.; Markham, Brian L.; Miller, Jonathan; Padula, Francis P.; Raqueno, Nina G.

    2012-01-01

    Landsat's continuing record of the thermal state of the earth's surface represents the only long term (1982 to the present) global record with spatial scales appropriate for human scale studies (i.e., tens of meters). Temperature drives many of the physical and biological processes that impact the global and local environment. As our knowledge of, and interest in, the role of temperature on these processes have grown, the value of Landsat data to monitor trends and process has also grown. The value of the Landsat thermal data archive will continue to grow as we develop more effective ways to study the long term processes and trends affecting the planet. However, in order to take proper advantage of the thermal data, we need to be able to convert the data to surface temperatures. A critical step in this process is to have the entire archive completely and consistently calibrated into absolute radiance so that it can be atmospherically compensated to surface leaving radiance and then to surface radiometric temperature. This paper addresses the methods and procedures that have been used to perform the radiometric calibration of the earliest sizable thermal data set in the archive (Landsat 4 data). The completion of this effort along with the updated calibration of the earlier (1985 1999) Landsat 5 data, also reported here, concludes a comprehensive calibration of the Landsat thermal archive of data from 1982 to the present

  6. Ethyl 4-(5-bromo-2-hy-droxy-phen-yl)-2,7,7-trimethyl-5-oxo-1,4,5,6,7,8-hexa-hydro-quinoline-3-carboxyl-ate.

    PubMed

    Kurbanova, Malahat M; Huseynov, Elnur Z; Gurbanov, Atash V; Maharramov, Abel M; Kia, Reza

    2013-04-01

    In the title compound, C21H24BrNO4, the dihedral angle between the heterocyclic ring and the pendant aromatic ring is 80.20 (13)°. The hexahydroquinone [i.e. the one with the C=O group] ring adopts a sofa conformation. An intra-molecular O-H⋯O hydrogen bond generates an S(6) ring motif. The ethyl group is disordered over two sets of sites with a refined site occupancy ratio of 0.633 (10):0.366 (10). In the crystal, mol-ecules are linked by N-H⋯O inter-actions, forming chains parallel to [101]. There are no significant C-H⋯π or π-π inter-actions in the crystal structure.

  7. Solid-Supported Synthesis and 5-HT7 /5-HT1A Receptor Affinity of Arylpiperazinylbutyl Derivatives of 4,5-dihydro-1,2,4-triazine-6-(1H)-one.

    PubMed

    Grychowska, Katarzyna; Masurier, Nicolas; Verdié, Pascal; Satała, Grzegorz; Bojarski, Andrzej J; Martinez, Jean; Pawłowski, Maciej; Subra, Gilles; Zajdel, Paweł

    2015-10-01

    A series of arylpiperazinylbutyl derivatives of 4,5-dihydro-1,2,4-triazine-6(1H)-ones was designed and synthesized according to the new solid-supported methodology. In this approach, triazinone scaffold was constructed from the Fmoc-protected glycine. The library representatives showed different levels of affinity for 5-HT7 and 5-HT1A receptors; compounds 13, 14 and 18-20 were classified as dual 5-HT7 /5-HT1A receptors ligands. The structure-affinity relationship analysis revealed that the receptor affinity and selectivity of the tested compounds depended on the kind of substituent in position 3 of triazinone fragment as well as substitution pattern of the phenylpiperazine moiety.

  8. Synthesis and crystal structure of copper complex of 7,16-bis(2-hydroxy-5-methyl-3-nitrobenzyl)-1,4,10,13-tetraoxa-7,16-diazacyclooctadecane

    NASA Astrophysics Data System (ADS)

    Ma, Shu-lan; Zhu, Wen-xiang

    2002-12-01

    A lariat crown ether compound 7,16-bis(2-hydroxy-5-methylbenzyl)-1,4,10,13-tetraoxa-7,16-diazacyclooctadecane has been prepared via one-pot Mannich reaction. A copper(II) complex with the ligand 7,16-bis(2-hydroxy-5-methyl-3-nitrobenzyl)-1,4,10,13-tetraoxa-7,16-diazacyclooctadecane was unexpectedly synthesized and characterized by elemental analysis, IR and UV spectra. The crystal structure of the complex has been determined by X-ray diffraction. Both crystal structure analysis and spectroscopy study indicated that the side-arm phenols of lariat crown ether are nitrated while complexing with Cu(NO 3) 2. Structure shows that the copper(II) ion is coordinated to two nitrogen and four oxygen atoms, two from the crown ether and other two from the deprotonated phenolate groups. The coordination polyhedron is a distorted octahedron.

  9. Solid-State Synthesis and Structure of the Enigmatic Ammonium Octaborate: (NH4)2[B7O9(OH)5]·3/4B(OH)3·5/4H2O.

    PubMed

    Neiner, Doinita; Sevryugina, Yulia V; Schubert, David M

    2016-09-06

    The compound known since the 19th century as ammonium octaborate was structurally characterized revealing the ammonium salt of the ribbon isomer of the heptaborate anion, [B7O9(OH)5](2-), with boric acid and water molecules. Of composition (NH4)2B7.75O12.63·4.88H2O, it approximates the classical ammonium octaborate composition (NH4)2B8O13·6H2O and has the structural formula {(NH4)2[B7O9(OH)5]}4·3B(OH)3·5H2O. It spontaneously forms at room temperature in solid-state mixtures of ammonium tetraborate and ammonium pentaborate. It crystallizes in the monoclinic space group P21/c with a = 11.4137(2) Å, b = 11.8877(2) Å, c = 23.4459(3) Å, β = 90.092(1)°, V = 3181.19(8) Å(3), and Z = 2 and contains well-ordered ammonium cations and [B7O9(OH)5](2-) anions and disordered B(OH)3 and H2O molecules linked by extensive H bonding. Expeditious solid-state formation of the heptaborate anion under ambient conditions has important implications for development of practical syntheses of industrially useful borates.

  10. 8 CFR 1236.4 - Removal of S-5, S-6, and S-7 nonimmigrants.

    Code of Federal Regulations, 2013 CFR

    2013-01-01

    ..., and S-7 nonimmigrants. (a) Condition of classification. As a condition of classification and continued stay in classification pursuant to section 101(a)(15)(S) of the Act, nonimmigrants in S classification... after, or conduct or a condition not disclosed to the Service prior to, the alien's classification as...

  11. 8 CFR 1236.4 - Removal of S-5, S-6, and S-7 nonimmigrants.

    Code of Federal Regulations, 2012 CFR

    2012-01-01

    ..., and S-7 nonimmigrants. (a) Condition of classification. As a condition of classification and continued stay in classification pursuant to section 101(a)(15)(S) of the Act, nonimmigrants in S classification... after, or conduct or a condition not disclosed to the Service prior to, the alien's classification as...

  12. Cytotoxic, Antiproliferative and Pro-Apoptotic Effects of 5-Hydroxyl-6,7,3′,4′,5′-Pentamethoxyflavone Isolated from Lantana ukambensis

    PubMed Central

    Sawadogo, Wamtinga Richard; Cerella, Claudia; Al-Mourabit, Ali; Moriou, Céline; Teiten, Marie-Hélène; Guissou, Innocent Pierre; Dicato, Mario; Diederich, Marc

    2015-01-01

    Lantana ukambensis (Vatke) Verdc. is an African food and medicinal plant. Its red fruits are eaten and highly appreciated by the rural population. This plant was extensively used in African folk medicinal traditions to treat chronic wounds but also as anti-leishmanial or cytotoxic remedies, especially in Burkina Faso, Tanzania, Kenya, or Ethiopia. This study investigates the in vitro bioactivity of polymethoxyflavones extracted from a L. ukambensis as anti-proliferative and pro-apoptotic agents. We isolated two known polymethoxyflavones, 5,6,7,3′,4′,5′-hexamethoxyflavone (1) and 5-hydroxy-6,7,3′,4′,5′-pentamethoxyflavone (2) from the whole plant of L. ukambensis. Their chemical structures were determined by spectroscopic analysis and comparison with published data. These molecules were tested for the anti-proliferative, cytotoxic and pro-apoptotic effects on human cancer cells. Among them, 5-hydroxy-6,7,3′,4′,5′-pentamethoxyflavone (2) was selectively cytotoxic against monocytic lymphoma (U937), acute T cell leukemia (Jurkat), and chronic myelogenous leukemia (K562) cell lines, but not against peripheral blood mononuclear cells (PBMCs) from healthy donors, at all tested concentrations. Moreover, this compound exhibited significant anti-proliferative and pro-apoptotic effects against U937 acute myelogenous leukemia cells. This study highlights the anti-proliferative and pro-apoptotic effects of 5-hydroxy-6,7,3′,4′,5′-pentamethoxyflavone (2) and provides a scientific basis of traditional use of L. ukambensis. PMID:26690473

  13. Structure and Electronic Transitions of C7H4O2(+) and C7H5O2(+) Ions: Neon Matrix and Theoretical Studies.

    PubMed

    Fulara, Jan; Erattupuzha, Sonia; Garkusha, Iryna; Maier, John P

    2016-12-29

    C7H4O2(+) and C7H5O2(+) ions and the respective neutrals have been investigated by absorption spectroscopy in neon matrixes following mass selection of ions produced from salicylic acid. Three electronic transitions starting at 649.6, 431.0, and 372.0 nm are detected for C7H4O2(+) and assigned on the basis of CASPT2 energies and Franck-Condon simulations as the excitations from the X (2)A″ to the 1 (2)A″, 2 (2)A″, and 3 (2)A″ electronic states of 6-(oxomethylene)-2,4-cyclohexadien-1-one ion (A(+)). Absorptions commencing at 366.4 nm are observed for C7H5O2(+) and assigned to the 1 (2)A' ← X (2)A' electronic transition of (2-hydroxyphenyl)methanone ion (J(+)). Neutralization of J(+) leads to the appearance of four absorption systems attributed to the 4 (2)A″, 3 (2)A″, 2 (2)A″, and 1 (2)A″ ← X (2)A″ transitions of J with origin bands 291.3, 361.2, 393.8, and 461.2 nm.

  14. Interconfigurational 5d → 4f luminescence of Ce3+ and Pr3+ in Ca9Lu(PO4)7.

    PubMed

    Trevisani, M; Ivanovskikh, K V; Piccinelli, F; Speghini, A; Bettinelli, M

    2012-09-26

    Ca(9)Lu(PO(4))(7):Ce (3+) and Ca (9)Lu (PO (4))(7):Pr (3+) polycrystalline materials were synthesized by solid state reaction at high temperature. The materials were characterized by powder x-ray diffraction (XRPD). The luminescence spectroscopy and the excited state dynamics of these compounds were investigated upon excitation with UV/VUV synchrotron radiation. Both materials showed efficient and fast 5d-4f emission upon direct VUV excitation into the 5d levels but only Ca(9)Lu(PO(4))(7):Ce (3+) revealed luminescence upon excitation across the bandgap. The decay kinetics of the 5d-4f emission upon VUV intra-center excitation is characterized by a decay time of 29 ns for Ce (3+) and 17 ns for Pr (3+) with no significant build-up after the excitation pulse. For the both compounds, no significant temperature dependence of the 5d-4f emission lifetime was observed within the range 8-300 K.

  15. 40 CFR 721.8485 - 2-Propenoic acid, 2-methyl-, (octahydro-4,7-methano-1H- indene-5-diyl)bis(methylene) ester.

    Code of Federal Regulations, 2010 CFR

    2010-07-01

    ...-, (octahydro-4,7-methano-1H- indene-5-diyl)bis(methylene) ester. 721.8485 Section 721.8485 Protection of...-methyl-, (octahydro-4,7-methano-1H- indene-5-diyl)bis(methylene) ester. (a) Chemical substance and...-, (octahydro-4,7-methano- 1H- indene-5-diyl)bis(methylene) ester (PMN P-99-1075; CAS No. 43048-08-4) is...

  16. 40 CFR 721.8485 - 2-Propenoic acid, 2-methyl-, (octahydro-4,7-methano-1H- indene-5-diyl)bis(methylene) ester.

    Code of Federal Regulations, 2011 CFR

    2011-07-01

    ...-, (octahydro-4,7-methano-1H- indene-5-diyl)bis(methylene) ester. 721.8485 Section 721.8485 Protection of...-methyl-, (octahydro-4,7-methano-1H- indene-5-diyl)bis(methylene) ester. (a) Chemical substance and...-, (octahydro-4,7-methano- 1H- indene-5-diyl)bis(methylene) ester (PMN P-99-1075; CAS No. 43048-08-4) is...

  17. Discovery of 7-aryl-substituted (1,5-naphthyridin-4-yl)ureas as aurora kinase inhibitors.

    PubMed

    Defaux, Julien; Antoine, Maud; Le Borgne, Marc; Schuster, Tilmann; Seipelt, Irene; Aicher, Babette; Teifel, Michael; Günther, Eckhard; Gerlach, Matthias; Marchand, Pascal

    2014-01-01

    As part of our research projects to identify new chemical entities of biological interest, we developed a synthetic approach and the biological evaluation of (7-aryl-1,5-naphthyridin-4-yl)ureas as a novel class of Aurora kinase inhibitors for the treatment of malignant diseases based on pathological cell proliferation. 1,5-Naphthyridine derivatives showed excellent inhibitory activities toward Aurora kinases A and B, and the most active compound, 1-cyclopropyl-3-[7-(1-methyl-1H-pyrazol-4-yl)-1,5-naphthyridin-4-yl]urea (49), displayed IC₅₀ values of 13 and 107 nM against Aurora kinases A and B, respectively. In addition, the selectivity toward a panel of seven cancer-related protein kinases was highlighted. In vitro ADME properties were also determined in order to rationalize the difficulties in correlating antiproliferative activity with Aurora kinase inhibition. Finally, the good safety profile of these compounds imparts promising potential for their further development as anticancer agents.

  18. 5,7-Di-2-pyridyl-2,3-dihydro-thieno[3,4-b][1,4]dioxine.

    PubMed

    Djukic, Brandon; Harrington, Laura E; Britten, James F; Lemaire, Martin T

    2008-01-16

    The title compound, C(16)H(12)N(2)O(2)S, was prepared by a Neigishi cross-coupling reaction to investigate the coordination chemistry of thio-phene-containing ligands. In the mol-ecule, the pyridine rings are twisted from the thio-phene ring by 20.6 (1) and 4.1 (2)°. The six-membered dihydro-dioxine ring is in a half-chair conformation.

  19. 1,5-Dichloro-3(2,7),7(2,7)-dinaphthal-ena-2,4,6,8-tetra-oxa-1(2,6),5(2,6)-di(1,3,5-triazina)octa-phane.

    PubMed

    Sang, Qiu-Guang; Yang, Jing-Kui

    2011-09-01

    In the macrocyclic title compound, C(26)H(12)Cl(2)N(6)O(4), an O-atom-bridged calix[2]naphthalene-[2]triazine synthesized using a one-pot approach from naphthalene-2,7-diol and cyanuric chloride, the two isolated naphthalene planes and the two triazine-2,6-di-oxy planes adopt a 1,3-alternate configuration, with a dihedral angle of 84.10 (8)° between the naphthalene rings and a dihedral angle of 39.02 (14)° between the triazine rings. In the crystal, weak inter-molecular π-π stacking inter-actions are found between face-to-face naphthalene rings [centroid-centroid distance = 3.662 (7) Å].

  20. Synthesis and photoluminescence control of Ca10.5-1.5xLax(PO4)7:Eu2+ phosphors by aliovalent cation substitution

    NASA Astrophysics Data System (ADS)

    Fan, Yanting; Tang, Miao; Qiu, Zhongxian; Zhang, Jilin; Yu, Liping; Li, Chengzhi; Lian, Shixun; Zhou, Wenli

    2017-02-01

    A range of Ca10.5-1.5xLax(PO4)7:Eu2+phosphors were synthesized by high temperature solid state method. Subsequently we studied the crystal structures and luminescent properties through X-ray diffraction, photoluminescence and photoluminescence excitation, diffuse reflection spectra, Raman spectra and decay curves systematically. Based on the special crystal structure ofβ-Ca3(PO4)2:Eu2+, its emission undergoes a variation from violet-blue to cyan through introducing La3+. The substitution of La3+ for Ca2+ could form some cation vacancies in Ca(4) sites according to the scheme 3Ca2+= 2La3++ □ due to the different ion valence, which compels Eu2+ to migrate from Ca(4) site to other sites. Additionally, the formation of the cation vacancies can further reduce the thermal stability of phosphors.

  1. Synthesis and oxidation behavior of 2,4,5,7,8-pentamethyl-4H-1,3-benzodioxin-6-ol, a multifunctional oxatocopherol-type antioxidant.

    PubMed

    Rosenau, Thomas; Potthast, Antje; Elder, Thomas; Lange, Thomas; Sixta, Herbert; Kosma, Paul

    2002-05-31

    2,4,5,7,8-Pentamethyl-4H-1,3-benzodioxin-6-ol (PBD, 1) is a novel 3-oxa-tocopherol-type stabilizer, which is obtained as a mixture of two diastereomers by condensation of trimethylhydroquinone with acetaldehyde in an acid-catalyzed reaction. The oxidation behavior of 1 is governed by the amount of water available. In aqueous media, 1 is oxidized by one oxidation equivalent to 2,5-dihydroxy-3,4,6-trimethylacetophenone (3) via 2-(1-hydroxyethyl)-3,5,6-trimethylbenzo-1,4-quinone (2). The acid-catalyzed conversion of 2 into 3 proceeds in solution with first-order kinetics with regard to 2 but works also in solid phase. Oxidation in the presence of just 1 equiv of water produces acetophenone 3 as well, but according to a different mechanism involving o-quinone methide 5 and styrene derivative 6, from which finally acetaldehyde is released. A [1,5]-sigmatropic proton shift from the C-4a methyl group to the exocyclic methylene group in 5 causes formation of 6, as demonstrated by labeling experiments. In addition, the presence of both intermediates was proven by hetero-Diels-Alder trapping reactions. In the absence of water, oxidation of 1 produces chromenone 10 via the intermediates 5 and 6 and chromanone 9, and oxidation of 9 to 10 is preferred to oxidation of starting material 1. When the formation of an exocyclic methylene group at C-4 is impossible as a result of structural prerequisites, as in the diphenyl derivative 12, the initially generated o-quinone methide 5 cannot form 6 but undergoes dimerization to spiro-compounds. The transformation of p-quinone 2 into acetophenone 3 might contribute to the chemistry of tocopherols oxidized at C-4, i.e., 4-hydroxy-alpha-tocopherol and 4-oxo-alpha-tocopherol, which have been proposed as precursors of natural vitamin E metabolites.

  2. (3aRS,7aSR)-7a-Meth­oxy-2-oxo-2,3,3a,4,5,6,7,7a-octa­hydro-1-benzofuran-4,4-dicarbonitrile

    PubMed Central

    González, María; Martínez, Andrea; Rivadulla, Marcos L.; Covelo, Berta

    2012-01-01

    The racemic title compound, C11H12N2O3, contains a [4.3.0]bicyclic unit in which the shared C—C bond adopts a cis configuration. The five- and six-membered rings are in twisted envelope (with the bridgehead C atom bearing the methoxy substituent as the flap) and distorted chair conformations, respectively. In the crystal, the mol­ecules are linked via weak C—H⋯O iteractions, forming ladder-like chains along [010]. PMID:23476303

  3. Effects of grilling on luteolin (3',4',5,7-tetrahydroxyflavone) content in sweet green bell pepper (Capsicum annuum).

    PubMed

    Durucasu, Inci; Tokuşoğlu, Ozlem

    2007-10-01

    The content of luteloin in green bell pepper (Capsicum annuum) produced in Turkey were determined by RP-HPLC with DAD detection. The luteloin (3',4',5,7-Tetrahydroxyflavone) content of green pepper samples were 46.00 +/- 0.76 mg kg(-1) f.w. (average). The alterations of luteloin concentrations with heating process (grilling, közleme) and the loss of luteloin amount were also determined. Luteolin contents of grilled peppers were found as 29.96 +/- 0.96 mg kg(-1) f.w. The method was objective and reproducible for accurate detection of luteloin in green pepper and other pepper varieties.

  4. Proceedings of the Biennial EO/EEO Research Symposium (4th) Held in Cocoa Beach, Florida on December 5-7, 2001

    DTIC Science & Technology

    2003-01-01

    PROCEEDINGS 4th Biennial EO/EEO Research Symposium December 5-7, 2001 Cocoa Beach, Florida Published January 2003 DEOMI Research Report 03-01...distribution unlimited 13. SUPPLEMENTARY NOTES Proceedings 4th Biennial EO/EEO Research Symposium, Held in Cocoa Beach, Florida on December 5-7...Prescribed by ANSI Std Z39-18 ii Proceedings 4th Biennial EO/EEO Research Symposium December 5-7, 2001 Cocoa Beach, Florida Sponsored

  5. Synthesis, antimicrobial activity and QSAR studies of new 2,3-disubstituted-3,3a,4,5,6,7-hexahydro-2H-indazoles.

    PubMed

    Minu, Maninder; Thangadurai, Ananda; Wakode, Sharad Ramesh; Agrawal, Shyam Sundar; Narasimhan, Balasubramanian

    2009-06-01

    Antimicrobial activity of synthesized 2,3-disubstituted-3,3a,4,5,6,7-hexahydro-2H-indazole derivatives indicated that 3-(4-chlorophenyl)-2-(4-nitrophenylsulfonyl)-3,3a,4,5,6,7-hexahydro-2H-indazole (6) and 3-(4-fluorophenyl)-2-(4-nitrophenylsulfonyl)-3,3a,4,5,6,7-hexahydro-2H-indazole (20) were the most active compounds. Further, the results of QSAR studies indicated the importance of topological parameters (2)chi and (2)chi(v) in defining the antimicrobial activity of hexahydroindazoles.

  6. Aggregation-Induced Emission of Organogels Based on Self-Assembled 5-(4-Nonylphenyl)-7-azaindoles.

    PubMed

    López, Daniel; García-Frutos, Eva M

    2015-08-11

    A new self-assembled organogel based on 5-(4-nonylphenyl)-7-azaindole (1), possessing an aggregation-induced emission phenomenon (AIE), is described. The incorporation of phenyl alkyl chains improves processability of the platform to form a new class of gelator. The fluorescence spectrum of 1 suffers changes in the gelation process, and an AIE phenomenon is observed during the phase transition from sol to gel state. The fluorescence is decreased slowly by heating the gel, and no emission is detected in concentrated solutions of 1. The AIE effect is due to the formation of the supramolecular organogel, where a self-association of the 7-azaindole moieties by dual hydrogen-bonded dimers is present. Regarding the solid-state emission properties, the xerogel 1 exhibits blue emission as well as in its organogel form. Therefore, it could be considered as a promising blue emitter in the solid state.

  7. Platinum(II) complexes with 5,7-disubstituted-1,2,4-triazolo [1,5-a]pyrimidines: Spectroscopical characterization and cytotoxic activity in vitro

    NASA Astrophysics Data System (ADS)

    Łakomska, Iwona; Fandzloch, Marzena; Popławska, Beata; Sitkowski, Jerzy

    2012-06-01

    Complexes of the types: cis-[PtI2(dptp)2] (1), cis-[PtI2(NH3)(dptp)] (2), trans-[PtI2(dptp)(dmso)] (3) and trans-[PtI2(dbtp)(dmso)] (4), where dptp = 5,7-diphenyl-1,2,4-triazolo[1,5-a]pyrimidine (dptp), dbtp = 5,7-ditertbutyl-1,2,4-triazolo[1,5-a]pyrimidine have been synthesized and characterized by infrared and multinuclear magnetic resonance spectroscopic techniques (1H, 13C, 15N, 195Pt). In 195Pt NMR, the cis-diiodo complexes were observed between -2601 ppm and -3261 ppm, while the trans coordination compounds were found at higher field (ca. -4389 ppm). In all cases significant 15N NMR shielding (92-95 ppm) were observed for N(3) atom indicating this nitrogen atom as a coordination site. The cis complexes have been assayed for antitumor activity in vitro against two human cell lines: A549 (non-small cell lung carcinoma) and T47D (breast cancer). The results indicate a moderate antiproliferative activity of (2) against human cancer lines.

  8. 3,3',4',5,7-Pentamethylquercetin reduces angiotensin II-induced cardiac hypertrophy and apoptosis in rats.

    PubMed

    Mao, Zhangfan; Liang, Yuanxin; Du, Xinling; Sun, Zongquan

    2009-09-01

    Quercetin has been shown to possess beneficial pharmacological properties in treatment of heart disease, but lack of stability and bioavailability limits its clinical use. In this study, we investigated for the first time the effect of a methylated form of quercetin, 3,3',4',5,7-pentamethylquercetin (PMQ), on myocardial protection in rats. Angiotensin II was delivered to Sprague-Dawley rats subcutaneously, while PMQ (5 mg/kg) was administered by oral gavage; blood pressure was monitored daily. The production of NADPH oxidase was measured, and cardiac hypertrophy and apoptosis were detected. The results revealed that PMQ could downregulate the expression of the NADPH oxidase gene and reduce angiotensin II- induced cardiac hypertrophy and apoptosis in rats. Therefore, we believe that PMQ showed beneficial effects on myocardium in angiotensin II-administered rats, and its potential to be used for treatment of cardiovascular disease deserves further attention.

  9. Stability of ferric complexes with 3-hydroxyflavone (flavonol), 5,7-dihydroxyflavone (chrysin), and 3',4'-dihydroxyflavone.

    PubMed

    Engelmann, Mark D; Hutcheson, Ryan; Cheng, I Francis

    2005-04-20

    The acid dissociation and ferric stability constants for complexation by the flavonoids 3-hydroxyflavone (flavonol), 5,7-dihydroxyflavone (chrysin), and 3',4'-dihydroxyflavone in 50:50 (v/v) ethanol/water are determined by pH potentiometric and spectrophotometric titrations and the linear least-squares curve-fitting program Hyperquad. Over the entire range of pH and reagent concentrations spanning the titration experiments, the stoichiometry for iron-flavonoid complex formation was 1:1 for all three flavonoids examined. The three flavonoids were chosen for their hydroxy substitution pattern, with each possessing one of the three most commonly suggested sites for metal binding by the flavonoids. On the basis of the calculated stability constants, the intraflavonoid-binding site competition is illustrated as a function of pH via speciation curves. The curves indicate that the binding site comprised of the 3',4'-hydroxy substitutions, the catecholic site, is most influential for ferric complexation at the physiological pH of 7.4. The possibility for antioxidant activity by flavonoid chelation of ferric iron in the presence of other competitive physiological complexing agents is demonstrated through additional speciation calculations.

  10. 7-cyclopentyl-5-(4-phenoxyphenyl)-7H-pyrrolo[2,3-d] pyrimidin-4-ylamine inhibits the proliferation and migration of vascular smooth muscle cells by suppressing ERK and Akt pathways.

    PubMed

    Seo, Hyang-Hee; Kim, Sang Woo; Lee, Chang Youn; Lim, Kyu Hee; Lee, Jiyun; Lim, Soyeon; Lee, Seahyoung; Hwang, Ki-Chul

    2017-03-05

    Excessive vascular smooth muscle cell (VSMC) proliferation and migration after vascular injury significantly contributes to the development of occlusive vascular disease. Therefore, inhibiting the proliferation and migration of VSMCs is a validated therapeutic modality for occlusive vascular disease such as atherosclerosis and restenosis. In the present study, we screened chemical compounds for their anti-proliferative effects on VSMCs using multiple approaches, such as MTT assays, wound healing assays, and trans-well migration assays. Our data indicate that 7-cyclopentyl-5-(4-phenoxyphenyl)-7H-pyrrolo[2,3-d] pyrimidin-4-ylamine, a lymphocyte-specific protein tyrosine kinase (Lck) inhibitor, significantly inhibited both VSMC proliferation and migration. 7-cyclopentyl-5-(4-phenoxyphenyl)-7H-pyrrolo[2,3-d]pyrimidin-4-ylamine suppresses VSMC proliferation and migration via down-regulating the protein kinase B (Akt) and extracellular signal regulated kinase (ERK) pathways, and it significantly decreased the expression of proliferating cell nuclear antigen (PCNA) and cyclin D1 and, the phosphorylation of retinoblastoma protein (pRb). Additionally, 7-cyclopentyl-5-(4-phenoxyphenyl)-7H-pyrrolo[2,3-d] pyrimidin-4-ylamine suppressed the migration of VSMCs from endothelium-removed aortic rings, as well as neointima formation following rat carotid balloon injury. The present study identified 7-cyclopentyl-5-(4-phenoxyphenyl)-7H-pyrrolo[2,3-d]pyrimidin-4-ylamine as a potent VSMC proliferation and migration inhibitor and warrants further studies to elucidate its more detailed molecular mechanisms, such as its primary target, and to further validate its in vivo efficacy as a therapeutic agent for pathologic vascular conditions, such as restenosis and atherosclerosis.

  11. Crystal structure and absolute configuration of (3aS,4S,5R,7aR)-2,2,7-trimethyl-3a,4,5,7a-tetra­hydro-1,3-benzodioxole-4,5-diol

    PubMed Central

    Macías, Mario A.; Suescun, Leopoldo; Pandolfi, Enrique; Schapiro, Valeria; Tibhe, Gaurao D.; Mombrú, Álvaro W.

    2015-01-01

    The absolute configuration of the title compound, C10H16O4, determined as 3aS,4S,5R,7aR on the basis of the synthetic pathway, was confirmed by X-ray diffraction. The mol­ecule contains a five- and a six-membered ring that adopt twisted and envelope conformations, respectively. The dihedral angle between the mean planes of the rings is 76.80 (11)° as a result of their cis-fusion. In the crystal, mol­ecules are linked by two pairs of O—H⋯O hydrogen bonds, forming chains along [010]. These chains are further connected by weaker C—H⋯O inter­actions along [100], creating (001) sheets that inter­act only by weak van der Waals forces. PMID:26396837

  12. 7 CFR 7.5 - Eligible voters.

    Code of Federal Regulations, 2010 CFR

    2010-01-01

    ... 7 Agriculture 1 2010-01-01 2010-01-01 false Eligible voters. 7.5 Section 7.5 Agriculture Office of the Secretary of Agriculture SELECTION AND FUNCTIONS OF AGRICULTURAL STABILIZATION AND CONSERVATION STATE, COUNTY AND COMMUNITY COMMITTEES § 7.5 Eligible voters. (a) Voters eligible to participate in:...

  13. Fibronectin type III5 repeat contains a novel cell adhesion sequence, KLDAPT, which binds activated alpha4beta1 and alpha4beta7 integrins.

    PubMed

    Moyano, J V; Carnemolla, B; Domínguez-Jiménez, C; García-Gila, M; Albar, J P; Sánchez-Aparicio, P; Leprini, A; Querzé, G; Zardi, L; Garcia-Pardo, A

    1997-10-03

    The region of fibronectin encompassing type III repeats 4-6 contains a low affinity heparin binding domain, but its physiological significance is not clear. We have studied whether this domain is able to interact with cells as already shown for other heparin binding domains of fibronectin. A computer search based on homologies with known active sites in fibronectin revealed the sequence KLDAPT located in FN-III5. A synthetic peptide containing this sequence induced lymphoid cell adhesion upon treatment with the activating anti-beta1 monoclonal antibody (mAb) TS2/16 or with Mn2+, indicating that KLDAPT was binding to an integrin. A recombinant fragment containing repeat III5 (FN-III5) also mediated adhesion of TS2/16/Mn2+-treated cells while the FN-III6 fragment did not. Soluble KLDAPT peptide inhibited cell adhesion to FN-III5 as well as to a 38-kDa fibronectin fragment and VCAM-1, two previously known ligands for alpha4beta1 integrin. KLDAPT also competed with the binding of soluble alkaline phosphatase-coupled VCAM-Ig to Mn2+-treated alpha4beta1. Furthermore, mAbs anti-alpha4 and anti-alpha4beta7, but not mAbs to other integrins, inhibited cell adhesion to FN-III5 and KLDAPT. These results therefore establish a cell adhesive function for the FN-III5 repeat and show that KLDAPT is a novel fibronectin ligand for activated alpha4 integrins.

  14. Pressure distribution data from tests of 2.29-meter (7.5-ft.) span EET high-lift research model in Langley 4- by 7-meter tunnel

    NASA Technical Reports Server (NTRS)

    Morgan, H. L., Jr.

    1982-01-01

    A 2.29 m (7.5 ft.) span high-lift research model equipped with full-span leading-edge slat and part-span double-slotted trailing-edge flap was tested in the Langley 4- by 7-Meter Tunnel to determine the low speed performance characteristics of a representative high aspect ratio suprcritical wing. These tests were performed in support of the Energy Efficient Transport (EET) program which is one element of the Aircraft Energy Efficiency (ACEE) project. Static longitudinal forces and moments and chordwise pressure distributions at three spanwise stations were measured for cruise, climb, two take-off flap, and two landing flap wing configurations. The tabulated and plotted pressure distribution data is presented without analysis or discussion.

  15. Microwave-Assisted Synthesis of 2-Aryl-2-oxazolines, 5,6-Dihydro-4H-1,3-oxazines, and 4,5,6,7-Tetrahydro-1,3-oxazepines.

    PubMed

    Mollo, María C; Orelli, Liliana R

    2016-12-02

    The first general procedure for the synthesis of 5- to 7-membered cyclic iminoethers by microwave-assisted cyclization of ω-amido alcohols promoted by polyphosphoric acid (PPA) esters is presented. 2-Aryl-2-oxazolines and 5,6-dihydro-4H-1,3-oxazines were efficiently prepared using ethyl polyphosphate/CHCl3. Trimethylsilyl polyphosphate in solvent-free conditions allowed for the synthesis of hitherto-unreported 4,5,6,7-tetrahydro-1,3-oxazepines. The method involves good to excellent yields and short reaction times.The reaction mechanism and the role of PPA esters were investigated in a chiral substrate.

  16. Influence of structure 3,5,7,3‧,4‧-Pentahydroxyflavone-based polymer films on their optical transparency

    NASA Astrophysics Data System (ADS)

    Mishurov, Dmytro; Voronkin, Andrii; Roshal, Alexander; Bogatyrenko, Sergey

    2017-02-01

    Optical properties and morphology of polymer films based on diglycidyl ether of bis-phenol A and on natural compound 3,5,7,3‧,4‧-pentahydroxyflavone (quercetin) using UV-vis spectroscopy, scanning electron microscopy and powder X-ray diffraction methods have been investigated. The influence of ordering degree of the polymers, flexibility of their chains, intensity of intermolecular interaction between the quercetine moieties on the polymers' morphology was discussed. It is shown that all the quercetine-based polymer films are transparent at visible and near infrared regions beginning from 420 to 450 nm. Low optical transparency in the short-wavelength region can be explained the self-absorption of quercetin moieties in the polymer chains.

  17. Vibrational spectroscopy investigation using ab initio and DFT vibrational analysis of 7-chloro-2-methylamino-5-phenyl-3H-1,4-benzodiazepine-4-oxide

    NASA Astrophysics Data System (ADS)

    Prasath, M.; Muthu, S.; Arun Balaji, R.

    2013-09-01

    The FT-IR and FT-Raman spectrum of 7-chloro-2-methylamino-5-phenyl-3H-1, 4-benzodiazepine-4-oxide (7CMP4BO) has been recorded in the region 4000-400 and 4000-100 cm-1 respectively. The optimized geometry, Thermodynamic properties, NBO, Molecular Electrostatic Potentials, PES, frequency and intensity of the vibrational bands of 7CMP4BO were obtained by the ab initio HF and density functional theory (DFT), B3LYP/6-31G (d,p) basis set. The molecule orbital contributions were studied by using the total (TDOS), partial (PDOS), and overlap population (OPDOS) density of states. The harmonic vibrational frequencies were calculated and the scaled values have been compared with experimental FT-IR and FT-Raman spectra. A detailed interpretation of the vibrational spectra of this compound has been made on the basis of the calculated potential energy distribution (PED). The linear polarizability (α) and the first order hyperpolarizability (β) values of the investigated molecule have been computed using DFT quantum mechanical calculations. The observed and the calculated frequencies are found to be in good agreement. The experimental spectra also coincide satisfactorily with those of theoretically calculated values.

  18. Structures of Three Pyrazaboles: 1,3,5,7-Tetramethylpyrazabole; 4,4-Bis(pyrazol-1’-yl)pyrazabole; 4,4,8,8-Tetrakis(pyrazol-1’yl)pyrazabole.

    DTIC Science & Technology

    1984-11-01

    RL UNCLRSSIFIED NOV 84 UK/DC/TR-4 N88014-83-K-06ii F/G 7/ 3 NL I fl.m I .0i7 I I ~o II 1- 1111- 5 2- 111112.2 11111L -* ll l 40 ___ MICROCOPY RESOLUTION...Boron" • I. . - . . . ,--." " PACE 2 . b 21.765(2), c = 11.672(1) 1, = 09.51(1)’, V = 2118.9( 5 ) ? at 296 K, Z 4, D = 1.329 g cr- 3 IoKa, graphite...Positional parameters given in Table 5 and some bond lengths and angles in Tables 2 and 3 ; the molecular structure is illustrated in Figure 3

  19. Diastereoselective synthesis of 2-arylmethylene-6-hydroxyspiro[4.5]deca-7-ones via FeCl3·6H2O-catalyzed spiroannulation/hydride transfer of 6-(5-arylpent-4-yn-1-yl)-7-oxabicyclo[4.1.0]heptan-2-ols.

    PubMed

    Lin, Hsin-Hui; Lee, Kuan-Yi; Chen, Yin-An; Liu, Chi-Fan; Yeh, Ming-Chang P

    2014-12-05

    In the presence of a catalytic amount of FeCl3·6H2O, 6-(5-arylpent-4-yn-1-yl)-7-oxabicyclo[4.1.0]heptan-2-ols underwent attack of the pendant acetylene at the iron-activated oxirane to give a vinylic carbocation. Hydride transfer from the carbinol carbon to the newly formed cation center furnished 2-arylmethylene-6-hydroxyspiro[4.5]deca-7-ones in excellent stereoselectivity and good yields.

  20. Synthesis and evaluation of 1-[2-(4-[(11)C]methoxyphenyl)phenyl]piperazine for imaging of the serotonin 5-HT7 receptor in the rat brain.

    PubMed

    Shimoda, Yoko; Yui, Joji; Xie, Lin; Fujinaga, Masayuki; Yamasaki, Tomoteru; Ogawa, Masanao; Nengaki, Nobuki; Kumata, Katsushi; Hatori, Akiko; Kawamura, Kazunori; Zhang, Ming-Rong

    2013-09-01

    1-[2-(4-Methoxyphenyl)phenyl]piperazine (4) is a potent serotonin 5-HT7 receptor antagonist (Ki=2.6nM) with a low binding affinity for the 5-HT1A receptor (Ki=476nM). As a potential positron emission tomography (PET) radiotracer for the 5-HT7 receptor, [(11)C]4 was synthesized at high radiochemical yield and specific activity, by O-[(11)C]methylation of 2'-(piperazin-1-yl)-[1,1'-biphenyl]-4-ol (6) with [(11)C]methyl iodide. Autoradiography revealed that [(11)C]4 showed in vitro specific binding with 5-HT7 in the rat brain regions, such as the thalamus which is a region with high 5-HT7 expression. Metabolite analysis indicated that intact [(11)C]4 in the brain exceeded 90% of the radioactive components at 15min after the radiotracer injection, although two radiolabeled metabolites were found in the rat plasma. The PET study of rats showed moderated uptake of [(11)C]4 in the brain (1.2SUV), but no significant regional difference in radioactivity in the brain. Pretreatment with 5-HT7-selective antagonist SB269970 (3) did not decrease the uptake of [(11)C]4 in the rat brain. Further studies are warranted that focus on the development of PET ligand candidates with higher binding affinity for 5-HT7 and higher in vivo stability in brain than 4.

  1. 7-[4-(5,7-Dimethyl-1,8-naphthyridin-2-yl­oxy)phen­oxy]-2,4-dimethyl-1,8-naphthyridine methanol disolvate

    PubMed Central

    Jin, Shou-Wen; Wang, Da-Qi; Chen, Yun

    2008-01-01

    The title compound, C26H22N4O2·2CH3OH, was synthesized and characterized by 1H NMR spectroscopy and X-ray structure analysis. There is one half-mol­ecule in the asymmetric unit with a centre of symmetry located at the centre of the benzene ring. The two bridged naphthyridine ring systems are in an anti­parallel orientation. In the crystal structure, O—H⋯N, C—H⋯O and C—H⋯N inter­actions define the packing. PMID:21200814

  2. 7,7-Dimethyl-2-methyl­amino-4-(4-methyl­phenyl)-3-nitro-7,8-di­hydro-4H-chromen-5(6H)-one

    PubMed Central

    Inglebert, S. Antony; Kamalraja, Jayabal; Sethusankar, K.; Perumal, Paramasivam T.

    2014-01-01

    In the title compound, C19H22N2O4, the six-membered cyclo­hexenone ring of the chromene unit adopts an envelope conformation, with the dimethyl-substituted C atom as the flap, while the pyran ring has a boat conformation. These two mean planes are inclined to one another by 6.65 (13)°·The benzene ring is normal to the 4H-chromene moiety mean plane, making a dihedral angle of 89.18 (5)°. The methyl­amine and nitro groups are slightly twisted from the chromene moiety mean plane, with torsion angles C—N—C—O = 1.70 (18) and O—N—C—C = 0.15 (18)°. The mol­ecular structure is characterized by an intra­molecular N—H⋯O hydrogen bond, which generates an S(6) ring motif. In the crystal, mol­ecules are linked via pairs of weak C—H⋯O hydrogen bonds, forming inversion dimers. These dimers are connected by further C—H⋯O hydrogen bonds, forming sheets lying parallel to (10-1). PMID:24940281

  3. Synthesis and crystal structures of 7-bromo-5-(2‧-chloro)phenyl-3-hydroxy-1-methyl-1,2-dihydro-3H-1,4-benzodiazepin-2-one and 7-bromo-5-(2‧-chloro)phenyl-1-hexyl-1,2,4,5-tetrahydro-3H-1,4-benzodiazepin-2,3-dione

    NASA Astrophysics Data System (ADS)

    Kravtsov, Victor Ch.; Fonari, Marina S.; Gdaniec, Мaria; Pavlovsky, Victor I.; Andronati, Sergei A.; Semenishyna, Ekaterina A.

    2012-06-01

    Treatment of 7-bromo-5-(2'-chloro)phenyl-3-hydroxy-1,2-dihydro-3H-1,4-benzodiazepin-2-one (1) with methyl or hexyl tosylate resulted in 7-bromo-5-(2'-chloro)phenyl-3-hydroxy-1-methyl-1,2-dihydro-3H-1,4-benzodiazepin-2-one (2) and 7-bromo-5-(2'-chloro)phenyl-1-hexyl-1,2,4,5-tetrahydro-3H-1,4-benzodiazepin-2,3-dione (3). As confirmed by X-ray crystallography, the two products differ not only in the identity of the alkyl substituent in position 1 of the benzodiazepine fragment but also crystallize in different molecular forms resulting from proton migration. This alteration of the molecular structure leads to a significant change in the conformation of the central molecular fragment and influences the assembly mode in the crystal. In 3, centrosymmetric dimers formed via a pair of Nsbnd H⋯O hydrogen bonds are further linked into chains via Csbnd Br⋯Odbnd C halogen bond interaction. In turn in 2 there are two symmetry independent molecules, each giving a different set of intermolecular interactions. One of the molecules forms a dimer via Osbnd H⋯O interactions whereas the second one generates chain via Csbnd Br⋯Odbnd C halogen bond that is also assisted by a weak Osbnd H⋯Br hydrogen bond.

  4. A convenient synthesis of 7 alpha-hydroxycholest-4-en-3-one by the hydroxypropyl-beta-cyclodextrin-facilitated cholesterol oxidase oxidation of 3 beta,7 alpha-cholest-5-ene-3,7-diol.

    PubMed

    Alexander, D L; Fisher, J F

    1995-03-01

    The initial biosynthetic conversions of cholesterol to the bile acids involve sequential 7 alpha-hydroxylation (catalyzed by cholesterol 7 alpha-hydroxylase) followed by C-3 oxidation and concomitant double bond migration (to a delta 4-configuration, catalyzed by 3 beta-delta 5-C27-steroid oxidoreductase) to provide 7 alpha-hydroxycholest-4-en-3-one. A straightforward, and economical, preparation (on a 0.1 g scale) of this pivotal biosynthetic intermediate has been devised. Reduction of 3 beta-(benzoyloxy)-cholest-5-en-7-one with LiB(sec-butyl)3H provided a 4:1 mixture, respectively, of the 7 alpha- and 7 beta-hydroxy diastereomers, which were separated chromatographically. Solvolytic removal of the C-3 benzoyl group gave 3 beta,7 alpha-cholest-5-ene-3,7-diol. A suspension of the 1:1 (v/v) complex (formed by mutual dissolution in MeOH, followed by evaporation of the solvent) of this diol with hydroxypropyl-beta-cyclodextrin, at a concentration of 1 mg mL-1 (in neutral phosphate buffer), was converted by Brevibacterium sp cholesterol oxidase (0.25 U mg-1 of substrate) and catalase (70 U mg-1 of substrate, to recover O2 from the H2O2 produced by the enzymatic oxidation) to a suspension of 7 alpha-hydroxycholest-4-en-3-one and the hydroxypropyl-beta-cyclodextrin. The yield for the enzymatic conversion was in excess of 90%. A much poorer and less reproducible yield (< 20%) was seen in the absence of the hydroxypropyl-beta-cyclodextrin. Routine extraction of this aqueous suspension, and chromatographic purification (85:15 CHCl3/acetone v/v on silica) of the residue, gave pure 7 alpha-hydroxycholest-4-en-3-one in 68% isolated yield. This route is a significant improvement, in terms of reaction scale and convenience, over the previous procedures for the preparation of this steroid.

  5. Arangasite, Al2(PO4)(SO4)F · 7.5H2O, a new mineral from the Alyaskitovy deposit, Eastern Yakutia, Russia

    NASA Astrophysics Data System (ADS)

    Gamyanin, G. N.; Zayakina, N. V.; Galenchikova, L. T.

    2014-12-01

    A new hydrous aluminum sulfate-phosphate-fluoride arangasite, Al2(PO4)(SO4)F · 7.5H2O, has been found in cassiterite-silicate-sulfide ore at the Alyaskitovy deposit, Indigirka River basin, eastern Sakha (Yakutia) (64°39' N, 142°70' E). The new mineral was named after its type locality, Arangas Creek. It belongs to the secondary minerals of the oxidation zone and occurs in cavities within quartz-muscovite-tourmaline-sulfide veins and adjacent greisen. Arangasite is associated with other secondary minerals: phosphorscorodite, fluellite, gypsum, colquiriite, strengite, mansfieldite, and sinkankasite. Arangasite forms white compact segregations composed of fine-lamellar aggregates. This paper reports data on its chemical composition, optical, radiographic, thermal, and IR-spectroscopic characteristics.

  6. Discovery of novel 5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridine derivatives as γ-secretase modulators (Part 2).

    PubMed

    Takai, Takafumi; Koike, Tatsuki; Nakamura, Minoru; Kajita, Yuichi; Yamashita, Toshiro; Taya, Naohiro; Tsukamoto, Tetsuya; Watanabe, Tomomichi; Murakami, Koji; Igari, Tomoko; Kamata, Makoto

    2016-07-15

    γ-Secretase modulators (GSMs), which lower pathogenic amyloid beta (Aβ) without affecting the production of total Aβ or Notch signal, have emerged as a potential therapeutic agent for Alzheimer's disease (AD). A novel series of 5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridine derivatives was discovered and characterized as GSMs. Optimization of substituents at the 8-position of the core scaffold using ligand-lipophilicity efficiency (LLE) as a drug-likeness guideline led to identification of various types of high-LLE GSMs. Phenoxy compound (R)-17 exhibited especially high LLE as well as potent in vivo Aβ42-lowering effect by single administration. Furthermore, multiple oral administration of (R)-17 significantly reduced soluble and insoluble brain Aβ42, and ameliorated cognitive deficit in novel object recognition test (NORT) using Tg2576 mice as an AD model.

  7. Stability of Behavioral and Emotional Problems over 6 Years in Children Ages 4 to 5 or 6 to 7 at Time 1

    ERIC Educational Resources Information Center

    Bilancia, Sarah D.; Rescorla, Leslie

    2010-01-01

    This study tests the hypothesis that 6-year longitudinal stability of behavioral and emotional problems would be greater for children ages 6 to 7 than for those ages 4 to 5 at Time 1. Six-year outcome data for a nationally representative sample of 4- to 7-year-olds (N = 733) were used to examine longitudinal stability of internalizing,…

  8. Synthesis, spectral characterization, crystal structure and molecular docking study of 2,7-diaryl-1,4-diazepan-5-ones

    NASA Astrophysics Data System (ADS)

    Sethuvasan, S.; Sugumar, P.; Maheshwaran, V.; Ponnuswamy, M. N.; Ponnuswamy, S.

    2016-07-01

    In this study, a series of variously substituted r-2,c-7-diaryl-1,4-diazepan-5-ones 9-16 have been synthesized using Schmidt rearrangement and are characterized by IR, mass and 1D & 2D NMR spectral data. The proton NMR coupling constant and estimated dihedral angles reveal that the compounds 9-16 prefer a chair conformation with equatorial orientation of alkyl and aryl groups. Single crystal X-ray structure has been solved for compounds 9 and 11 which also indicates the preference for distorted chair conformation with equatorial orientation of substituents. The compounds 9-16 have been docked with the structure of Methicillin-resistant Staphylococcus aureus (MRSA) and the results demonstrate that compound 10 is having better docking score and glide energy than others and it is comparable to co-crystal ligand. Furthermore, all the compounds have been evaluated for their antibacterial and antioxidant activities. All the compounds show moderate antibacterial activity and only 11 exhibits better activity against S. aures and Escherichia coli. The compounds 11, 13 and 14 exhibit half of the antioxidant power when compared to the BHT and the remaining compounds show moderate activity.

  9. A concise synthesis of 1,4-dihydro-[1,4]diazepine-5,7-dione, a novel 7-TM receptor ligand core structure with melanocortin receptor agonist activity.

    PubMed

    Szewczyk, Jerzy R; Laudeman, Chris P; Sammond, Doug M; Villeneuve, Manon; Minick, Douglas J; Grizzle, Mary K; Daniels, Alejandro J; Andrews, John L; Ignar, Diane M

    2010-03-01

    Finding small non-peptide molecules for G protein-coupled receptors (GPCR) whose endogenous ligands are peptides, is a very important task for medicinal chemists. Over the years, compounds mimicking peptide structures have been discovered, and scaffolds emulating peptide backbones have been designed. In our work on GPCR ligands, including cholecystokinin receptor-1 (CCKR-1) agonists, we have employed benzodiazepines as a core structure. Looking for ways to reduce molecular weight and possibly improve physical properties of GPCR ligands, we embarked on the search for molecules providing similar scaffolds to the benzodiazepine with lower molecular weight. One of our target core structures was 1,4-dihydro-[1,4]diazepine-5,7-dione. There was not, however, a known synthetic route to such molecules. Here we report the discovery of a simple and concise method for synthesis of 2-[6-(1H-indazol-3-ylmethyl)-5,7-dioxo-4-phenyl-4,5,6,7-tetrahydro-[1,4]diazepin-1-yl]-N-isopropyl-N-phenyl-acetamide as an example of a compound containing the tetrahydrodiazepine-5,7-dione core. Compounds from this series were tested in numerous GPCR assays and demonstrated activity at melanocortin 1 and 4 receptors (MC1R and MC4R). Selected compounds from this series were tested in vivo in Peptide YY (PYY)-induced food intake. Compounds dosed by intracerebroventricular and oral routes reduced PYY-induced food intake and this effect was reversed by the cyclic peptide MC4R antagonist SHU9119.

  10. Effect of thermomechanical treatment on the superelasticity of Ti-7.5Nb-4Mo-2Sn biomedical alloy.

    PubMed

    Zhang, D C; Tan, C G; Tang, D M; Zhang, Y; Lin, J G; Wen, C E

    2014-11-01

    Effects of thermomechanical treatment on the microstructure and superelasticity of Ti-7.5Nb-4Mo-2Sn biomedical alloy were investigated by using XRD measurement, optical microscope (OM), transmission electron microscope (TEM) and tensile tests. The titanium alloy samples were prepared by annealing at a temperature in the range of 600 to 1000°C after severe cold rolling; and the samples that were annealed at 800°C were further aged at 600 and 700°C. The volume fraction of α phases decreased while that of ω phases increase with increasing annealing temperature. The α→β transformation temperature of the alloy was determined to be between 700 and 800°C. The alloy that was annealed at 700°C exhibited a high level of superelasticity with relatively high first yield stress (σSIM) at room temperature because it contained a fine α phase. A certain amount of ω phases also resulted in an increase in σSIM, leading to an improvement in the superelasticity of the alloys that were annealed at 900 and 1000°C. Aging treatment led to the precipitations of α and ω phases in the alloy after annealing at 800°C; and the volume fraction of α phases decreased while that of ω phases increased with increasing aging temperature. Excellent superelasticity with high recovered strain (εrecoverable) and strain recovery rate (η) were obtained in the aged alloy due to the reinforcement of α and ω phases induced by aging treatment. The alloy annealed at 700°C for 0.5h exhibited the best superelasticity in all the thermomechanically treated alloys due to the strengthening from the subgrain refining and the precipitating of fine α phases.

  11. 28 CFR 7.5 - Certification.

    Code of Federal Regulations, 2010 CFR

    2010-07-01

    ... 28 Judicial Administration 1 2010-07-01 2010-07-01 false Certification. 7.5 Section 7.5 Judicial Administration DEPARTMENT OF JUSTICE REWARDS FOR CAPTURE OF ESCAPED FEDERAL PRISONERS § 7.5 Certification. The claim letter required under § 7.4 shall contain the following certification immediately proceeding...

  12. A new flavone glycoside, 5-hydroxy 7,3',4',5'-tetra-methoxyflavone 5-O-beta-D-xylopyranosyl-(1-->2)-alpha-L-rhamnopyranoside from Bauhinia variegata Linn.

    PubMed

    Yadava, R N; Reddy, V M

    2001-01-01

    A new flavone glycoside m.f. C(30)H(36)O(15) m.p. 252-253 degrees C, [M]+ 636 (EIMS) was isolated from the acetone soluble fraction of the concentrated 95% ethanolic extract of the seeds of Bauhinia variegata (Linn). It was identified as 5-hydroxy7,3',4',5'-tetra-methoxyflavone 5-O-beta-D-xylopyranosyl-(1-->2)-alpha-L-rhamnopyranoside (1) by various colour reactions, chemical degradations and spectral techniques.

  13. Thermal expansion, thermal conductivity, and heat capacity measurements for boreholes UE25 NRG-4, UE25 NRG-5, USW NRG-6, and USW NRG-7/7A

    SciTech Connect

    Brodsky, N.S.; Riggins, M.; Connolly, J.; Ricci, P.

    1997-09-01

    Specimens were tested from four thermal-mechanical units, namely Tiva Canyon (TCw), Paintbrush Tuff (PTn), and two Topopah Spring units (TSw1 and TSw2), and from two lithologies, i.e., welded devitrified (TCw, TSw1, TSw2) and nonwelded vitric tuff (PTn). Thermal conductivities in W(mk){sup {minus}1} averaged over all boreholes, ranged (depending upon temperature and saturation state) from 1.2 to 1.9 for TCw, from 0.4 to 0.9 for PTn, from 1.0 to 1.7 for TSw1, and from 1.5 to 2.3 for TSw2. Mean coefficients of thermal expansion were highly temperature dependent and values, averaged over all boreholes, ranged (depending upon temperature and saturation state) from 6.6 {times} 10{sup {minus}6} to 49 {times} 10{sup {minus}6} C{sup {minus}1} for TCw, from the negative range to 16 {times} 10{sup {minus}6} {center_dot} {degree}C{sup {minus}1} for PTn, from 6.3 {times} 10{sup {minus}6} to 44 {times} 10{sup {minus}6} C{sup {minus}1} for TSw1, and from 6.7 {times} 10{sup {minus}6} to 37 {times} 10{sup {minus}6} {center_dot} {degree}C{sup {minus}1} for TSw2. Mean values of thermal capacitance in J/cm{sup 3}K (averaged overall specimens) ranged from 1.6 J to 2.1 for TSw1 and from 1.8 to 2.5 for TSw2. In general, the lithostratigraphic classifications of rock assigned by the USGS are consistent with the mineralogical data presented in this report.

  14. Sensitivity of lake sturgeon (Acipenser fulvescens) early life stages to 2,3,7,8-tetrachlorodibenzo-P-dioxin and 3,3',4,4',5-pentachlorobiphenyl.

    PubMed

    Tillitt, Donald E; Buckler, Justin A; Nicks, Diane K; Candrl, James S; Claunch, Rachel A; Gale, Robert W; Puglis, Holly J; Little, Edward E; Linbo, Tiffany L; Baker, Mary

    2017-04-01

    The aquatic food web of the Great Lakes has been contaminated with polychlorinated biphenyls (PCBs) since the mid-20th century. Threats of PCB exposures to long-lived species of fish, such as lake sturgeon (Acipenser fulvescens), have been uncertain because of a lack of information on the relative sensitivity of the species. The objective of the present study was to evaluate the sensitivity of early-life stage lake sturgeon to 3,3',4,4',5-pentachlorobiphenyl (PCB-126) or 2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD) exposure. Mortality, growth, morphological and tissue pathologies, swimming performance, and activity levels were used as assessment endpoints. Pericardial and yolk sac edema, tubular heart, yolk sac hemorrhaging, and small size were the most commonly observed pathologies in both TCDD and PCB-126 exposures, beginning as early as 4 d postfertilization, with many of these pathologies occurring in a dose-dependent manner. Median lethal doses for PCB-126 and TCDD in lake sturgeon were 5.4 ng/g egg (95% confidence interval, 3.9-7.4 ng/g egg) and 0.61 ng/g egg (0.47-0.82 ng/g egg), respectively. The resulting relative potency factor for PCB-126 (0.11) was greater than the World Health Organization estimate for fish (toxic equivalency factor = 0.005), suggesting that current risk assessments may underestimate PCB toxicity toward lake sturgeon. Swimming activity and endurance were reduced in lake sturgeon survivors from the median lethal doses at 60 d postfertilization. Threshold and median toxicity values indicate that lake sturgeon, like other Acipenser species, are more sensitive to PCB and TCDD than the other genus of sturgeon, Scaphirhynchus, found in North America. Indeed, lake sturgeon populations in the Great Lakes and elsewhere are susceptible to PCB/TCDD-induced developmental toxicity in embryos and reductions in swimming performance. Environ Toxicol Chem 2017;36:988-998. Published 2016 Wiley Periodicals Inc. on behalf of SETAC. This

  15. 5-(4-Chlorophenyl)-5,6-dihydro-1,3-oxazepin-7(4H)-one derivatives as lipophilic cyclic analogues of baclofen: design, synthesis, and neuropharmacological evaluation.

    PubMed

    Abdel-Hafez, Atef A; Abdel-Wahab, Basel A

    2008-09-01

    In trials to preserve the pharmacological profile and improve the bioavailability via lipophilicity increment of baclofen 1 and searching for more potent and less toxic muscle relaxants and analgesics, nine substituted cyclic analogues of 1 were designed and synthesized. The target derivatives 5-(4-chlorophenyl)-5,6-dihydro-1,3-oxazepin-7(4H)-one (11-19) were obtained through amide formation to the corresponding intermediates (2-10) followed by cyclization using acetic anhydride. The structures of the target compounds (11-19) were confirmed by IR, (1)H NMR, MS, and elemental analyses. The neuropharmacological activities of these lipophilic cyclic analogues (11-19) were assessed for their effects on motor activity, muscle relaxation, pain relief and impaired cognition, by intraperitoneal administration at a dose of 3mg/kg with reference to those of baclofen 1. Our results showed that compounds 11-14 are devoid of all of the tested pharmacological effects associated with 1. In all paradigms tested, undecyl, tridecyl, heptdec-8-enyl and benzyl substituted analogue derivatives (15, 16, 18, and 19) revealed a significant neurological activity being vividly favorable comparable with baclofen 1. 2-Benzyl-5-(4-chlorophenyl)-5,6-dihydro-1,3-oxazepin-7(4H)-one derivative 19 is the most active candidate with high significant neurological potencies, while 5-(4-chlorophenyl)-2-(dec-8-enyl)-5,6-dihydro-1,3-oxazepin-7(4H)-one derivative 17 displayed activity at relatively higher time interval. These results probe a new structurally distinct class incorporating 1,3-oxazepine nucleus as promising candidates as GABA(B) agonists for further investigations.

  16. Spin dynamics, short range order and spin freezing in Y0.5Ca0.5BaCo4O7

    SciTech Connect

    Stewart, John Ross; Ehlers, Georg; Fouquet, Peter; Mutka, Hannu; Payen, Christophe; Lortz, Rolf

    2011-01-01

    Y0.5Ca0.5BaCo4O7 was recently introduced as a possible candidate for capturing some of the predicted classical spin kagome ground-state features. Stimulated by this conjecture, we have taken up a more complete study of the spin correlations in this compound with neutron scattering methods on a powder sample characterized with high-resolution neutron diffraction and the temperature dependence of magnetic susceptibility and specific heat. We have found that the frustrated near-neighbor magnetic correlations involve not only the kagome planes but concern the full Co sublattice, as evidenced by the analysis of the wave-vector dependence of the short-range order. We conclude from our results that the magnetic moments are located on the Co sublattice as a whole and that correlations extend beyond the two-dimensional kagome planes. We identify intriguing dynamical properties, observing high-frequency fluctuations with a Lorentzian linewidth G?20 meV at ambient temperature. On cooling a low-frequency ({approx}1 meV) dynamical component develops alongside the high-frequency fluctuations, which eventually becomes static at temperatures below T {approx} 50 K. The high-frequency response with an overall linewidth of {approx}10 meV prevails at T?2 K, coincident with a fully elastic short-range-ordered contribution.

  17. 3′,4′,5′,5,7-Pentamethoxyflavone Sensitizes Cisplatin-Resistant A549 Cells to Cisplatin by Inhibition of Nrf2 Pathway

    PubMed Central

    Hou, Xiangyu; Bai, Xupeng; Gou, Xiaoli; Zeng, Hang; Xia, Chen; Zhuang, Wei; Chen, Xinmeng; Zhao, Zhongxiang; Huang, Min; Jin, Jing

    2015-01-01

    Nuclear factor erythroid 2-related factor 2 (Nrf2) is an important redox-sensitive transcription factor that regulates the expression of several cytoprotective genes. More recently, genetic analyses of human tumors have indicated that Nrf2 may cause resistance to chemotherapy. In this study, we found that the expression levels of Nrf2 and its target genes GCLC, HO-1, NQO1 were significantly higher in cisplatin-resistant A549 (A549/CDDP) cells than those in A549 cells, and this resistance was partially reversed by Nrf2 siRNA. 3′,4′,5′,5,7-Pentamethoxyflavone (PMF), a natural flavonoid extracted from Rutaceae plants, sensitized A549/CDDP to CDDP and substantially induced apoptosis compared with that of CDDP alone treated group, and this reversal effect decreased when Nrf2 was downregulated by siRNA. Mechanistically, PMF reduced Nrf2 expression leading to a reduction of Nrf2 downstream genes, and in contrast, this effect was decreased by blocking Nrf2 with siRNA. Taken together, these results demonstrated that PMF could be used as an effective adjuvant sensitizer to increase the efficacy of chemotherapeutic drugs by downregulating Nrf2 signaling pathway. PMID:25843086

  18. Exploring the binding mechanism of 5-hydroxy-3',4',7-trimethoxyflavone with bovine serum albumin: Spectroscopic and computational approach.

    PubMed

    Sudha, A; Srinivasan, P; Thamilarasan, V; Sengottuvelan, N

    2016-03-15

    The current study was carried out to investigate the binding mechanism of a potential flavonoid compound 5-hydroxy-3',4',7-trimethoxyflavone (HTMF) with bovine serum albumin (BSA) using ultraviolet-visible, fluorescence, circular dichroism (CD) spectral measurements along with molecular docking and molecular dynamics (MD) simulation. It was confirmed from fluorescence spectra that the intrinsic fluorescence of BSA was robustly quenched by HTMF through a static quenching mechanism. The number of binding sites (n) for HTMF binding on BSA was found to be about one. The thermodynamic parameters estimated from the van't Hoff plot specified that hydrophobic force was the predominant force in the HTMF-BSA complex and there also exist hydrogen bonds and electrostatic interactions. The effect of HTMF on the BSA conformation examined using CD studies revealed that there is a decrease in the helical content of BSA upon HTMF interaction. The results of molecular docking study shed light on the binding mode which exposed that HTMF bind within the hydrophobic pocket of the subdomain IIIA of BSA. The stability of HTMF-BSA complex with respect to free protein was analyzed from the molecular dynamic studies. The electronic structure analysis of HTMF was achieved by using density functional theory (DFT) calculations at B3LYP/6-31G** level to support its antioxidant role. The results of computational analysis are in good consistence with the experimental data and the present findings suggested that HTMF exhibits a good binding propensity to BSA protein which will be helpful for the drug design.

  19. Crystal structure of μ-4-oxidobenzoato-κ(2)O(1):O(4)-bis-[bis-(1,10-phenanthroline-κ(2)N,N')copper(II)] bis-(4-hy-droxy-benzoate) 7.5-hydrate.

    PubMed

    Su, Jian-Rong; Li, Yu

    2016-10-01

    The title hydrated complex, [Cu2(C7H4O3)(C12H8N2)4](C7H5O3)2·7.5H2O, is composed of dinuclear Cu(II) complex cations, noncoordinating 4-hy-droxy-benzoate anions and water mol-ecules of crystallization. In the dinuclear complex cation, the Cu(II) ions are bridged by a 4-oxidobenzoate ligand and thus each metal ion is five-coordinated by two chelating 1,10-phenanthroline (phen) mol-ecules and one anionic O atom in a distorted trigonal-bipyramid geometry. In the crystal, aromatic π-π stacking occurs between phen rings of neighbouring dinuclear Cu(II) complex cations, forming two-dimensional supra-molecular systems parallel to (100).

  20. Enantioseparation, absolute configuration determination, and anticonvulsant activity of (+/-)-1-(4-aminophenyl)-7,8-methylenedioxy-1,2,3,5-tetrahydro-4H-2,3-benzodiazepin-4-one.

    PubMed

    Calabrò, Maria Luisa; Raneri, Daniela; Ficarra, Paola; Ferreri, Guido; De Sarro, Giovambattista; Bruno, Giuseppe; Zappalà, Maria; Micale, Nicola; Grasso, Silvana

    2007-01-01

    The resolution of 1-(4-aminophenyl)-7,8-methylenedioxy-1,2,3,5-tetrahydro-4H-benzodiazepin-4-one (+/-)-(R,S)-2 was accomplished by chiral HPLC. The absolute configuration of (+)-2, determined by X-ray crystallographic analysis, was R. The in vivo anticonvulsant activity of the enantiomers (+)-(R)-2 and (-)-(S)-2 is reported. It has been also demonstrated that compound (+/-)-(R,S)-2 in vivo undergoes oxidative metabolism to derivative 1.

  1. Synthesis and modulation properties of imidazo[4,5-b]pyridin-7-one and indazole-4,7-dione derivatives towards the Cryptosporidium parvum CpABC3 transporter.

    PubMed

    Zeinyeh, Waël; Xia, Hexue; Lawton, Philippe; Radix, Sylvie; Marminon, Christelle; Nebois, Pascal; Walchshofer, Nadia

    2010-06-01

    The syntheses of new N-polysubstituted imidazo[4,5-b]pyridine-7-one (IP, 5 and 8a-8f) and indazole-4,7-dione (ID, 9 and 10) derivatives are described. The binding affinity of IP and ID towards the recombinant Nucleotide Binding Domain NBD1 of Cryptosporidium parvum CpABC3 was evaluated by intrinsic fluorescence quenching. IP induced a moderate quenching of the intrinsic fluorescence of H6-NBD1 whereas IDs 9 and 10 showed a binding affinity comparable to the ATP analogue TNP-ATP. In addition, 8d, 8e and 10 were shown to be competitive inhibitors of the ATPase activity, but with low affinity. These compounds could thus act like some flavonoid derivatives, which can partly overlap both the nucleotide-binding site and the adjacent hydrophobic steroid-binding region of mammalian P-glycoproteins.

  2. Facile synthesis of SSR180575 and discovery of 7-chloro-N,N,5-trimethyl-4-oxo-3(6-[18F]fluoropyridin-2-yl)-3,5-dihydro-4H-pyridazino[4,5-b]indole-1-acetamide, a potent pyridazinoindole ligand for PET imaging of TSPO in cancer

    PubMed Central

    Cheung, Yiu-Yin; Nickels, Michael L.; Tang, Dewei; Buck, Jason R.

    2014-01-01

    A novel synthesis of the translocator protein (TSPO) ligand 7-chloro-N,N,5-trimethyl-4-oxo-3-phenyl-3,5-dihydro-4H-pyridazino[4,5-b]indole-1-acetamide (SSR180575, 3) was achieved in four steps from commercially available starting materials. Focused structure−activity relationship development about the pyridazinoindole ring at the N3 position led to the discovery of 7-chloro-N,N,5-trimethyl-4-oxo-3(6-fluoropyridin-2-yl)-3,5-dihydro-4H-pyridazino[4,5-b]indole-1-acetamide (14), a novel ligand of comparable affinity. Radiolabeling with fluorine-18 (18F) yielded 7-chloro-N,N,5-trimethyl-4-oxo-3(6-[18F]fluoropyridin-2-yl)-3,5-dihydro-4H-pyridazino[4,5-b]indole-1-acetamide (18F-14) in high radiochemical yield and specific activity. In vivo studies of [18F]-14 revealed this agent as a promising probe for molecular imaging of glioma. PMID:25172419

  3. Turtle sex determination assay: Mass balance and responses to 2,3,7,8-tetrachlorodibenzo-p-dioxin and 3,3',4,4',5-pentachlorobiphenyl

    USGS Publications Warehouse

    Gale, Robert W.; Bergeron, Judith M.; Willingham, Emily J.; Crews, David

    2002-01-01

    Polyhalogenated hydrocarbons have been implicated in the anomalous sexual differentiation of mammals and reptiles. Here, a temperature-sensitive turtle sex determination assay using the red-eared slider (Trachemys scripta elegans) was used to determine the estrogenic or antiestrogenic activity of 2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD) and 3,3′,4,4′,5-pentachlorobiphenyl (PCB-126). Neither TCDD nor PCB-126 showed a statistically significant difference in the resulting sex ratios (Fisher's exact test, p < 0.45). As a consequence of the dosing technique (eggshell spotting), the shell retained 90 and 96% of the dose for PCB-126 and TCDD, respectively, similar to retention of estradiol-17β. However, the dosing allowed transfer of sufficient chemical to achieve tissue concentrations that were greater than most concentrations reported for environmentally incurred residues. Similar relative mass distributions of PCB-126 and TCDD were observed in albumin (14–20%), yolk (55–70%), and embryo (16–25%). Relative concentration distributions in the embryo approached those in the yolk, 37 to 40% and 40 to 52%, respectively, while relative concentrations in the albumin remained at 11 to 20%. Lipid-normalized TCDD and PCB-126 concentrations were 30- to 40-fold greater in the embryo than in the yolk. It is hypothesized that nonpassive partitioning processes may have occurred in the embryo.

  4. Crystal structure of 4,4'-[(1,3,5,7-tetra-oxo-1,3,3a,4,4a,5,7,7a,8,8a-deca-hydro-4,8-etheno-pyrrolo-[3,4-f]iso-indole-2,6-di-yl)bis-(methyl-ene)]bis-(pyridin-1-ium) dinitrate.

    PubMed

    Liu, Zhimin

    2015-12-01

    In the title salt, C24H22N4O4 (2+)·2NO3 (-), the cation is U-shaped with the two iso-indole dione rings inclined to one another by 60.41 (13)°, while the two outer pyridine rings are inclined to one another by 2.77 (12)°. The dihedral angles between the pyridine ring and the adjacent iso-indole dione ring are 71.82 (12) and 86.44 (13)°. In the crystal, each nitrate anion is linked to a protonated pyridine ring by N-H⋯O hydrogen bonds. These units are linked by a series of C-H⋯O hydrogen bonds, forming a three-dimensional structure.

  5. Eaf5/7/3 form a functionally independent NuA4 submodule linked to RNA polymerase II-coupled nucleosome recycling

    PubMed Central

    Rossetto, Dorine; Cramet, Myriam; Wang, Alice Y; Steunou, Anne-Lise; Lacoste, Nicolas; Schulze, Julia M; Côté, Valérie; Monnet-Saksouk, Julie; Piquet, Sandra; Nourani, Amine; Kobor, Michael S; Côté, Jacques

    2014-01-01

    The NuA4 histone acetyltransferase complex is required for gene regulation, cell cycle progression, and DNA repair. Dissection of the 13-subunit complex reveals that the Eaf7 subunit bridges Eaf5 with Eaf3, a H3K36me3-binding chromodomain protein, and this Eaf5/7/3 trimer is anchored to NuA4 through Eaf5. This trimeric subcomplex represents a functional module, and a large portion exists in a native form outside the NuA4 complex. Gene-specific and genome-wide location analyses indicate that Eaf5/7/3 correlates with transcription activity and is enriched over the coding region. In agreement with a role in transcription elongation, the Eaf5/7/3 trimer interacts with phosphorylated RNA polymerase II and helps its progression. Loss of Eaf5/7/3 partially suppresses intragenic cryptic transcription arising in set2 mutants, supporting a role in nucleosome destabilization. On the other hand, loss of the trimer leads to an increase of replication-independent histone exchange over the coding region of transcribed genes. Taken together, these results lead to a model where Eaf5/7/3 associates with elongating polymerase to promote the disruption of nucleosomes in its path, but also their refolding in its wake. PMID:24843044

  6. Eco-friendly methodology to prepare N-heterocycles related to dihydropyridines: microwave-assisted synthesis of alkyl 4-arylsubstituted-6-chloro-5-formyl-2-methyl-1,4-dihydropyridine-3-carboxylate and 4-arylsubstituted-4,7-dihydrofuro[3,4-b]pyridine-2,5(1H,3H)-dione.

    PubMed

    Rodríguez, Hortensia; Martin, Osnieski; Suarez, Margarita; Martín, Nazario; Albericio, Fernando

    2011-11-21

    Here we describe the efficient synthesis of alkyl 4-arylsubstituted-6-chloro-5-formyl-2-methyl-1,4-dihydropyridine-3-carboxylates and 4-arylsubstituted-4,7-dihydro-furo[3,4-b]pyridine-2,5(1H,3H)-diones via microwave-accelerated reaction of alkyl 4-arylsubstituted-2-methyl-6-oxo-1,4,5,6-tetrahydro-3-pyridinecarboxylates with the appropriate reagents. This eco-friendly approach to these valuable dihydropyridine derivatives does not involve the harsh or highly contaminating conditions common in classical heating and offers a reduction or even elimination of solvent use and recovery, simplification of the work-up procedures, facility of scale up, and low energy consumption, in addition to moderate to higher yields.

  7. DFT studies on a high-energy density cage compound 1, 3, 5, 7, 9, 11-hexo(N(CH3)NO2)-2, 4, 6, 8, 10, 12-hexaazatetracyclo[5, 5, 0, 0, 0] dodecane

    NASA Astrophysics Data System (ADS)

    Li, Xiao-Hong; Yong, Yong-Liang; Zhang, Xian-Zhou

    2014-04-01

    The infrared and Raman spectra, heat of formation (HOF) and thermodynamic properties were investigated by B3LYP/6-31G** method for a new designed polynitro cage compound 1,3,5,7,9,11-hexo(N(CH3)NO2)-2,4,6,8,10,12-hexaazatetracyclo[5,5,0,0,0]dodecane. The detonation velocity (D) and pressure (P) were predicted by the Kamlet-Jacobs equations based on the theoretical density and condensed HOF. The bond dissociation energies and bond orders for the weakest bonds were analysed to investigate the thermal stability of the title compound. The computational result shows that the detonation velocity and pressure of the title compound are superior to those of hexahydro-1,3,5-trinitro-1,3,5-triazine (RDX), but inferior to those of 1,3,5,7-tetranitro-1,3,5,7-tetraazacyclooctane (HMX) and hexanitrohexaazaisowurtzitane (HNIW). And the analysis of thermal stability shows that the first step of pyrolysis is the rupture of the N7-NO2 bond. The crystal structure obtained by molecular mechanics belongs to the P21 space group, with the lattice parameters Z = 2, a = 11.8246 Å, b = 10.4632 Å, c = 15.9713 Å, ρ = 1.98 g cm-3.

  8. Development of 4-Heteroarylamino-1'-azaspiro[oxazole-5,3'-bicyclo[2.2.2]octanes] as α7 Nicotinic Receptor Agonists.

    PubMed

    Hill, Matthew D; Fang, Haiquan; King, H Dalton; Iwuagwu, Christiana I; McDonald, Ivar M; Cook, James; Zusi, F Christopher; Mate, Robert A; Knox, Ronald J; Post-Munson, Debra; Easton, Amy; Miller, Regina; Lentz, Kimberley; Clarke, Wendy; Benitex, Yulia; Lodge, Nicholas; Zaczek, Robert; Denton, Rex; Morgan, Daniel; Bristow, Linda; Macor, John E; Olson, Richard

    2017-01-12

    We describe the synthesis of quinuclidine-containing spiroimidates and their utility as α7 nicotinic acetylcholine receptor (nAChR) partial agonists. A convergent synthetic route allowed for rapid SAR investigation and provided a diverse set of fused 6,5-heteroaryl analogs. Two potent and selective α7 nAChR partial agonists, (1'S,3'R,4'S)-N-(7-bromopyrrolo[2,1-f][1,2,4]triazin-4-yl)-4H-1'-azaspiro[oxazole-5,3'-bicyclo[2.2.2]octan]-2-amine (20) and (1'S,3'R,4'S)-N-(7-chloropyrrolo[2,1-f][1,2,4]triazin-4-yl)-4H-1'-azaspiro[oxazole-5,3'-bicyclo[2.2.2]octan]-2-amine (21), were identified. Both agonists improved cognition in a preclinical rodent model of learning and memory. Additionally, 5-HT3A receptor SAR suggested the presence of a steric site that when engaged led to significant loss of affinity at that receptor.

  9. cis-trans photoisomerization of 1,3,5,7-octatetraene in n-hexane at 4.2 K

    PubMed Central

    Granville, Mark F.; Holtom, Gary R.; Kohler, Bryan E.

    1980-01-01

    Photoisomerization of the linear polyene 1,3,5,7-octatetraene has been observed in an n-hexane matrix maintained at the boiling point of helium. To a good approximation, only the trans,trans and cis,trans isomers participate in the photochemistry. These compounds have been unambiguously identified by comparing the observed high-resolution fluorescence spectra to those of chromatographically purified reference compounds. Although the quantum yield of this process is probably low, its microscopic rate seems to compete favorably with vibrational deactivation. PMID:16592751

  10. Accelerators (4/5)

    ScienceCinema

    None

    2016-07-12

    1a) Introduction and motivation 1b) History and accelerator types 2) Transverse beam dynamics 3a) Longitudinal beam dynamics 3b) Figure of merit of a synchrotron/collider 3c) Beam control 4) Main limiting factors 5) Technical challenges Prerequisite knowledge: Previous knowledge of accelerators is not required.

  11. Modeling, Synthesis and Biological Evaluation of Potential Retinoid-X-Receptor (RXR) Selective Agonists: Novel Analogs of 4-[1-(3,5,5,8,8-Pentamethyl-5,6,7,8-tetrahydro-2-naphthyl)ethynyl]benzoic Acid (Bexarotene) and (E)-3-(3-(1,2,3,4-tetrahydro-1,1,4,4,6-pentamethylnaphthalen-7-yl)-4-hydroxyphenyl)acrylic acid (CD3254)

    PubMed Central

    Jurutka, Peter W.; Kaneko, Ichiro; Yang, Joanna; Bhogal, Jaskaran S.; Swierski, Johnathon C.; Tabacaru, Christa R.; Montano, Luis A.; Huynh, Chanh C.; Jama, Rabia A.; Mahelona, Ryan D.; Sarnowski, Joseph T.; Marcus, Lisa M.; Quezada, Alexis; Lemming, Brittney; Tedesco, Maria A.; Fischer, Audra J.; Mohamed, Said A.; Ziller, Joseph W.; Ma, Ning; Gray, Geoffrey M.; van der Vaart, Arjan; Marshall, Pamela A.; Wagner, Carl E.

    2014-01-01

    Three unreported analogs of 4-[1-(3,5,5,8,8-pentamethyl-5-6-7-8-tetrahydro-2-naphthyl)ethynyl]benzoic acid (1), otherwise known as bexarotene, as well as four novel analogs of (E)-3-(3-(1,2,3,4-tetrahydro-1,1,4,4,6-pentamethylnaphthalen-7-yl)-4-hydroxyphenyl)acrylic acid (CD3254) are described, and evaluated for their retinoid-X-receptor (RXR)-selective agonism. Compound 1 has FDA approval as a treatment for cutaneous T-cell lymphoma (CTCL); though, treatment with 1 can elicit side-effects by disrupting other RXR-heterodimer receptor pathways. Of the 7 modeled novel compounds, all analogs stimulate RXR-regulated transcription in mammalian-2-hybrid and RXRE-mediated assays, possess comparable or elevated biological activity based on EC50 profiles, and retain similar or improved apoptotic activity in CTCL assays compared to 1. All novel compounds demonstrate selectivity for RXR and minimal crossover onto the retinoic-acid-receptor (RAR) compared to all-trans-retinoic acid, with select analogs also reducing inhibition of other RXR-dependent pathways (e.g., VDR-RXR). Our results demonstrate that further improvements in biological potency and selectivity of bexarotene can be achieved through rational drug design. PMID:24180745

  12. Clarification of anomalous chiroptical behaviour and determination of the absolute configuration of 1-(3,4-dimethoxyphenyl)-4-methyl-5-ethyl-7,8-dimethoxy-5 H-2,3-benzodiazepine

    NASA Astrophysics Data System (ADS)

    Fogassy, Elemér; Ács, Mária; Tóth, Gábor; Simon, Kálmán; Láng, Tibor; Ladányi, L.; Párkányi, L.

    1986-09-01

    An optically active hydrogen bromide salt of 1-(3,4-dimethoxyphenyl)-4-methyl-5-ethyl-7,8-dimethoxy-5 H-2,3-benzodiazepine has been prepared and the R5 configuration studied by single-crystal X-ray analysis. The crystals are triclinic with space group P1, with two molecules in a unit cell of dimensions a = 10.798(1), b = 12.669(1) and c = 8.681(1) Å, and α = 97.15(1), β = 99.36(1) and γ = 68.74(1)°. The anomalous chiroptical behaviour is explained on the basis of the chiral interactions between the optically active conformers.

  13. A survey of z > 5.7 quasars in the sloan digital sky survey. 4. discovery of seven additional quasars

    SciTech Connect

    Fan, Xiao-Hui; Strauss, Michael A.; Richards, Gordon T.; Hennawi, Joseph F.; Becker, Robert H.; White, Richard L.; Diamond-Stanic, Aleksandar M.; onley, Jennifer L.D; Jiang, Lin-Hua; Kim, J.Serena; Vestergaard, Marianne; Young, Jason E.; Gunn, James E.; Lupton, Robert H.; Knapp, Gillian R.; Schneider, Donald P.; Brandt, W.N.; Bahcall, Neta A.; Barentine, J.C.; Brinkmann, J.; Brewington, Howard J.; /Arizona U., Astron. Dept. - Steward Observ. /Princeton U. Observ. /Johns Hopkins U. /UC, Berkeley, Astron. Dept. /UC, Davis /LLNL, Livermore /Baltimore, Space Telescope Sci. /Penn State U., Astron. Astrophys. /Apache Point Observ. /Tokyo U., ICRR /Mt. Suhora Observ., Cracow /Fermilab /Garching, Max Planck Inst., MPE

    2005-12-01

    We present the discovery of seven quasars at z > 5.7, selected from {approx}2000 deg{sup 2} of multicolor imaging data of the Sloan Digital Sky Survey (SDSS). The new quasars have redshifts z from 5.79 to 6.13. Five are selected as part of a complete flux-limited sample in the SDSS Northern Galactic Cap; two have larger photometric errors and are not part of the complete sample. One of the new quasars, SDSS J1335+3533 (z = 5.93), exhibits no emission lines; the 3-{sigma} limit on the rest-frame equivalent width of Ly{alpha} + NV line is 5 {angstrom}. It is the highest redshift lineless quasar known, and could be a gravitational lensed galaxy, a BL Lac object or a new type of quasar. Two new z > 6 quasars, SDSS 1250+3130 (z = 6.13) and SDSS J1137+3549 (z = 6.01), show deep Gunn-Peterson absorption gaps in Ly{alpha}. These gaps are narrower the complete Gunn-Peterson absorption troughs observed among quasars at z > 6.2 and do not have complete Ly{beta} absorption.

  14. Reaction of (chloro carbonyl) phenyl ketene with 5-amino pyrazolones: Synthesis, characterization and theoretical studies of 7-hydroxy-6-phenyl-3-(phenyldiazenyl)pyrazolo[1,5-a]pyrimidine-2,5(1H,4H)-dione derivatives

    NASA Astrophysics Data System (ADS)

    Zahedifar, Mahboobeh; Razavi, Razieh; Sheibani, Hassan

    2016-12-01

    New 7-hydroxy-6-phenyl-3-(phenyldiazenyl)pyrazolo[1,5-a]pyrimidine-2,5(1H,4H)-dione derivatives were synthesized from the reaction of (chlorocarbonyl)phenyl ketene and 5-amino pyrazolones in high to excellent yields and short reaction times. Structures of the new compounds were fully characterized by their spectral data IR, 1H NMR, and 13C NMR and by the theoretical results. Density Functional Theory (DFT) was used to optimize the structures, compute the energies and vibrational frequencies IR and 1H NMR shielding tensors of the desired products. The theoretical results excellent are compared with the experimental data.

  15. Thermodynamic studies on Cs 4U 5O 17(s) and Cs 2U 2O 7(s) by emf and calorimetric measurements

    NASA Astrophysics Data System (ADS)

    Jayanthi, K.; Iyer, V. S.; Venugopal, V.

    1997-12-01

    The oxygen potentials over the phase field: Cs 4U 5O 17(s)+Cs 2U 2O 7(s)+Cs 2U 4O 12(s) was determined by measuring the emf values between 1048 and 1206 K using a solid oxide electrolyte galvanic cell. The oxygen potential existing over the phase field for a given temperature can be represented by: Δ μ(O 2) (kJ/mol) (±0.5)=-272.0+0.207 T (K). The differential thermal analysis showed that Cs 4U 5O 17(s) is stable in air up to 1273 K. The molar Gibbs energy formation of Cs 4U 5O 17(s) was calculated from the above oxygen potentials and can be given by, Δ fG0 (kJ/mol)±6=-7729+1.681 T (K). The enthalpy measurements on Cs 4U 5O 17(s) and Cs 2U 2O 7(s) were carried out from 368.3 to 905 K and 430 to 852 K respectively, using a high temperature Calvet calorimeter. The enthalpy increments, ( H0T- H0298), in J/mol for Cs 4U 5O 17(s) and Cs 2U 2O 7(s) can be represented by, H0T- H0298.15 (Cs 4U 5O 17) kJ/mol±0.9=-188.221+0.518 T (K)+0.433×10 -3T2 (K)-2.052×10 -5T3 (K) (368 to 905 K) and H0T- H0298.15 (Cs 2U 2O 7) kJ/mol±0.5=-164.210+0.390 T (K)+0.104×10 -4T2 (K)+0.140×10 5(1/ T (K)) (411 to 860 K). The thermal properties of Cs 4U 5O 17(s) and Cs 2U 2O 7(s) were derived from the experimental values. The enthalpy of formation of (Cs 4U 5O 17, s) at 298.15 K was calculated by the second law method and is: Δ fH0298.15=-7645.0±4.2 kJ/mol.

  16. Chiral resolution and pharmacological characterization of the enantiomers of the Hsp90 inhibitor 2-amino-7-[4-fluoro-2-(3-pyridyl)phenyl]-4-methyl-7,8-dihydro-6H-quinazolin-5-one oxime.

    PubMed

    Amici, Raffaella; Bigogno, Chiara; Boggio, Roberto; Colombo, Andrea; Courtney, Stephen M; Dal Zuffo, Roberto; Dondio, Giulio; Fusar, Fulvia; Gagliardi, Stefania; Minucci, Saverio; Molteni, Marco; Montalbetti, Christian A G N; Mortoni, Annalisa; Varasi, Mario; Vultaggio, Stefania; Mercurio, Ciro

    2014-07-01

    Heat-shock protein 90 (Hsp90) is a molecular chaperone involved in the stabilization of key oncogenic signaling proteins, and therefore, inhibition of Hsp90 represents a new strategy in cancer therapy. 2-Amino-7-[4-fluoro-2-(3-pyridyl)phenyl]-4-methyl-7,8-dihydro-6H-quinazolin-5-one oxime is a racemic Hsp90 inhibitor that targets the N-terminal adenosine triphosphatase site. We developed a method to resolve the enantiomers and evaluated their inhibitory activity on Hsp90 and the consequent antitumor effects. The (S) stereoisomer emerged as a potent Hsp90 inhibitor in biochemical and cellular assays. In addition, this enantiomer exhibited high oral bioavailability in mice and excellent antitumor activity in two different human cancer xenograft models.

  17. Synthesis and in vitro anticancer activity of 6,7-methylenedioxy (or 5-hydroxy-6-methoxy)-2-(substituted selenophenyl)quinolin-4-one analogs.

    PubMed

    Chen, Chien-Ting; Hsu, Mei-Hua; Cheng, Yung-Yi; Liu, Chin-Yu; Chou, Li-Chen; Huang, Li-Jiau; Wu, Tian-Shung; Yang, Xiaoming; Lee, Kuo-Hsiung; Kuo, Sheng-Chu

    2011-12-01

    6,7-Methylenedioxy (or 5-hydroxy-6-methoxy)-2-(substituted selenophenyl)quinolin-4-ones and their isosteric compounds were synthesized and evaluated for anticancer activity. Structure-activity relationships (SAR) of these compounds were established. Among all tested compounds, 6,7-methylenedioxy-2-(5-methylselenophen-2-yl)quinolin-4-one (4d) was found to be the most promising anticancer agent. In screening against NCI's 60 human tumor cell line panel, 4d exhibited highly selective and potent inhibitory activity against MDA-MB-435 melanoma. Furthermore, the results of COMPARE analysis suggested that 4d is an antimitotic agent with a different mechanism of action from the conventional antimitotic agents, such as colchicine, vinca alkaloids and paclitaxel. Therefore, 4d was identified as a new lead compound that merits further optimization.

  18. Sr9Mg(1.5)(PO4)7:Eu(2+): A Novel Broadband Orange-Yellow-Emitting Phosphor for Blue Light-Excited Warm White LEDs.

    PubMed

    Sun, Wenzhi; Jia, Yonglei; Pang, Ran; Li, Haifeng; Ma, Tengfei; Li, Da; Fu, Jipeng; Zhang, Su; Jiang, Lihong; Li, Chengyu

    2015-11-18

    A new orange-yellow-emitting Sr9Mg(1.5)(PO4)7:Eu(2+) phosphor was prepared via high-temperature solid-state reaction. The structure and optical properties of it were studied systematically. Sr9Mg(1.5)(PO4)7:Eu(2+) can be well-excited by 460 nm blue InGaN chips and exhibit a wide emission band covering from 470 to 850 nm with two main peaks centered at 523 and 620 nm, respectively, which originate from 5d-4f dipole-allowed transitions of Eu(2+) in different crystallographic sites. The sites attribution, concentration quenching, fluorescence decay analysis, and temperature-dependent luminescence properties were investigated in detail. Furthermore, a warm white LED device was fabricated by combining a 460 nm blue InGaN chip with the optimized orange-yellow-emitting Sr9Mg(1.5)(PO4)7:Eu(2+). The color coordinate, correlated color temperature and color rendering index of the fabricated LED device were (0.393, 0.352), 3437 K, and 86.07, respectively. Sr9Mg(1.5)(PO4)7:Eu(2+) has great potential to serve as an attractive candidate in the application of blue light-excited warm white LEDs.

  19. (4R*,4aS*,4bS*,5R*,10aR*)-4-Hy­droxy-4a,5-dimethyl-2-(propan-2-yl)-1,4,4a,4b,5,6,7,8,10,10a-deca­hydro­phenan­thren-1-one

    PubMed Central

    Caracelli, Ignez; Zukerman-Schpector, Julio; Machado, André T. Lousada; Brocksom, Timothy J.; Ferreira, M. Lúcia; Tiekink, Edward R. T.

    2011-01-01

    In the title compound, C19H28O2, the A ring adopts a chair conformation. Both the B and C rings adopt envelope conformations with the C atoms common to both rings and adjacent to the carbonyl and hydroxyl groups, respectively, lying 0.604 (3) and 0.634 (3) Å out of the mean planes defined by the remaining five C atoms of rings B and C, respectively (r.m.s. deviations = 0.0100 and 0.0157 Å, respectively). The formation of linear supra­molecular C(7) chains along the a axis mediated by hy­droxy-O—H⋯O(carbon­yl) hydrogen bonds is the most prominent feature of the crystal packing. PMID:22199834

  20. Penta­cobalt(II) divanadium(III) tetrakis(diphosphate), Co5V2(P2O7)4

    PubMed Central

    Bronova, Anna; Glaum, Robert; Litterscheid, Christian

    2013-01-01

    Co5V2(P2O7)4 was crystallized by chemical vapour transport using HCl as transport agent. Its crystal structure is isotypic to that of FeII 5FeIII 2(P2O7)4 and can be regarded as a member of the thortveitite structure family with corrugated layers of metal–oxygen polyhedra extending parallel to (010). Significant occupational disorder between cobalt(II) and vanadium(III) is observed. Four of the five cation sites are occupied by both cobalt and vanadium. The fifth cation site (Co1) is occupied by cobalt only. Sites Co1, M3 and M4 are located on twofold axes. Sites Co1, M2, M3 and M4 show o­cta­hedral coordination by oxygen; M5 has a square-pyramidal environment. PMID:23723750

  1. An electron spin resonance study of Eu doping effect in La4/3Sr5/3Mn2O7 single crystal

    NASA Astrophysics Data System (ADS)

    He, Li-Min; Ji, Yu; Wu, Hong-Ye; Xu, Bao; Sun, Yun-Bin; Zhang, Xue-Feng; Lu, Yi; Zhao, Jian-Jun

    2014-07-01

    The effect of Eu3+ ion doping in the La sites of single-crystal La4/3Sr5/3Mn2O7 was investigated. Electron spin resonance (ESR) was applied to La4/3Sr5/3Mn2O7 and (La0.8Eu0.2)4/3Sr5/3Mn2O7 single crystals. A phase separation and phase transitions were observed from the ESR spectra data. Between 350 K and 300 K, both paramagnetic resonance (PMR) and anisotropic ferromagnetic resonance (FMR) lines were observed in the ab plane and the c axis direction, suggesting a coexistence of the paramagnetic (PM) phase and the ferromagnetic (FM) phase. The magnetization measurement reveals a spin-glass-like behavior in single-crystal (La0.8Eu0.2)4/3Sr5/3Mn2O7 below the temperature of spin freezing Tf (~ 29.5 K).

  2. The new truncated somatostatin receptor variant sst5TMD4 is associated to poor prognosis in breast cancer and increases malignancy in MCF-7 cells.

    PubMed

    Durán-Prado, M; Gahete, M D; Hergueta-Redondo, M; Martínez-Fuentes, A J; Córdoba-Chacón, J; Palacios, J; Gracia-Navarro, F; Moreno-Bueno, G; Malagón, M M; Luque, R M; Castaño, J P

    2012-04-19

    Somatostatin receptors (sst1-5) are present in different types of tumors, where they inhibit key cellular processes such as proliferation and invasion. Although ssts are densely expressed in breast cancer, especially sst2, their role and therapeutic potential remain uncertain. Recently, we identified a new truncated sst5 variant, sst5TMD4, which is related to the abnormal response of certain pituitary tumors to treatment with somatostatin analogs. Here, we investigated the possible role of sst5TMD4 in breast cancer. This study revealed that sst5TMD4 is absent in normal mammary gland, but is abundant in a subset of poorly differentiated human breast tumors, where its expression correlated to that of sst2. Moreover, in the MCF-7 breast cancer model cell, sst5TMD4 expression increased malignancy features such as invasion and proliferation abilities (both in cell cultures and nude mice). This was likely mediated by sst5TMD4-induced increase in phosphorylated extracellular signal-regulated kinases 1 and 2 and p-Akt levels, and cyclin D3 and Arp2/3 complex expression, which also led to mesenchymal-like phenotype. Interestingly, sst5TMD4 interacts physically with sst2 and thereby alters its signaling, enabling disruption of sst2 inhibitory feedback and providing a plausible basis for our findings. These results suggest that sst5TMD4 could be involved in the pathophysiology of certain types of breast tumors.

  3. Neonatal co-lesion by DSP-4 and 5,7-DHT produces adulthood behavioral sensitization to dopamine D(2) receptor agonists.

    PubMed

    Nowak, Przemysław; Nitka, Dariusz; Kwieciński, Adam; Jośko, Jadwiga; Drab, Jacek; Pojda-Wilczek, Dorota; Kasperski, Jacek; Kostrzewa, Richard M; Brus, Ryszard

    2009-01-01

    To assess the possible modulatory effects of noradrenergic and serotoninergic neurons on dopaminergic neuronal activity, the noradrenergic and serotoninergic neurotoxins DSP-4 N-(2-chlorethyl)-N-ethyl-2-bromobenzylamine (50.0 mg/kg, sc) and 5,7-dihydroxytryptamine (5,7-DHT) (37.5 microg icv, half in each lateral ventricle), respectively, were administered toWistar rats on the first and third days of postnatal ontogeny, and dopamine (DA) agonist-induced behaviors were assessed in adulthood. At eight weeks, using an HPLC/ED technique, DSP-4 treatment was associated with a reduction in NE content of the corpus striatum (> 60%), hippocampus (95%), and frontal cortex (> 85%), while 5,7-DHT was associated with an 80-90% serotonin reduction in the same brain regions. DA content was unaltered in the striatum and the cortex. In the group lesioned with both DSP-4 and 5,7-DHT, quinpirole-induced (DA D(2) agonist) yawning, 7-hydroxy-DPAT-induced (DA D(3) agonist) yawning, and apomorphine-induced (non-selective DA agonist) stereotypies were enhanced. However, SKF 38393-induced (DA D(1) agonist) oral activity was reduced in the DSP-4 + 5,7-DHT group. These findings demonstrate that DA D(2)- and D(3)-agonist-induced behaviors are enhanced while DA D(1)-agonist-induced behaviors are suppressed in adult rats in which brain noradrenergic and serotoninergic innervation of the brain has largely been destroyed. This study indicates that noradrenergic and serotoninergic neurons have a great impact on the development of DA receptor reactivity (sensitivity).

  4. Pharmacological characterization of (4R)-alkyl glutamate analogues at the ionotropic glutamate receptors--focus on subtypes iGlu(5-7).

    PubMed

    Bunch, Lennart; Gefflaut, Thierry; Alaux, Sebastien; Sagot, Emanuelle; Nielsen, Birgitte; Pickering, Darryl S

    2009-05-01

    The kainic acid (kainate, KA) receptors belong to the class of ionotropic glutamate (iGlu) receptors in the central nervous system. Five subtypes have been identified, which have been termed KA(1,2) and iGlu(5-7). In the search for subtype selective ligands, alpha-amino-5-tert-butyl-3-hydroxy-4-isoxazolyl)propionic acid (ATPA), (4R)-methyl Glu (1a), and E-4-neopentylidene Glu (2f) have all previously been reported as selective agonists for the iGlu(5) receptor subtype. In this paper, we present the pharmacological evaluation of a five-compound series of (4R)-alkyl Glu analogs (1b-e,g) which may be envisaged as conformationally released designs of ATPA and 4-alkylidenes 2a-h. Most notable is the pharmacological profile for (4R)-isopentyl Glu (1g) which shows a 10-fold increase in binding affinity for the iGlu(5) receptor subtype (K(i)=20.5 nM) in comparison with its E-4-alkylidene structural isomer 2g. Furthermore, 1g displays high selectivity over other KA receptor subtypes (KA(1,2) and iGlu(6,7)), AMPA-, and NMDA receptors (2050 and >5000 fold, respectively).

  5. Early-onset epileptic encephalopathy caused by a reduced sensitivity of Kv7.2 potassium channels to phosphatidylinositol 4,5-bisphosphate

    PubMed Central

    Soldovieri, Maria Virginia; Ambrosino, Paolo; Mosca, Ilaria; De Maria, Michela; Moretto, Edoardo; Miceli, Francesco; Alaimo, Alessandro; Iraci, Nunzio; Manocchio, Laura; Medoro, Alessandro; Passafaro, Maria; Taglialatela, Maurizio

    2016-01-01

    Kv7.2 and Kv7.3 subunits underlie the M-current, a neuronal K+ current characterized by an absolute functional requirement for phosphatidylinositol 4,5-bisphosphate (PIP2). Kv7.2 gene mutations cause early-onset neonatal seizures with heterogeneous clinical outcomes, ranging from self-limiting benign familial neonatal seizures to severe early-onset epileptic encephalopathy (Kv7.2-EE). In this study, the biochemical and functional consequences prompted by a recurrent variant (R325G) found independently in four individuals with severe forms of neonatal-onset EE have been investigated. Upon heterologous expression, homomeric Kv7.2 R325G channels were non-functional, despite biotin-capture in Western blots revealed normal plasma membrane subunit expression. Mutant subunits exerted dominant-negative effects when incorporated into heteromeric channels with Kv7.2 and/or Kv7.3 subunits. Increasing cellular PIP2 levels by co-expression of type 1γ PI(4)P5-kinase (PIP5K) partially recovered homomeric Kv7.2 R325G channel function. Currents carried by heteromeric channels incorporating Kv7.2 R325G subunits were more readily inhibited than wild-type channels upon activation of a voltage-sensitive phosphatase (VSP), and recovered more slowly upon VSP switch-off. These results reveal for the first time that a mutation-induced decrease in current sensitivity to PIP2 is the primary molecular defect responsible for Kv7.2-EE in individuals carrying the R325G variant, further expanding the range of pathogenetic mechanisms exploitable for personalized treatment of Kv7.2-related epilepsies. PMID:27905566

  6. (2R)-4-Oxo-4[3-(Trifluoromethyl)-5,6-diihydro:1,2,4}triazolo[4,3-a}pyrazin-7(8H)-y1]-1-(2,4,5-trifluorophenyl)butan-2-amine: A Potent, Orally Active Dipeptidyl Peptidase IV Inhibitor for the Treatment of Type 2 Diabetes

    SciTech Connect

    Kim, D.; Wang, L.; Beconi, M.; Eiermann, G.; Fisher, M.; He, H.; Hickey, G.; Kowalchick, Jennifer; Leiting, Barbara; Lyons, K.; Marsilio, F.; McCann, F.; Patel, R.; Petrov, A.; Scapin, G.; Patel, S.; Roy, R.; Wu, J.; Wyvratt, M.; Zhang, B.; Zhu, L.; Thornberry, N.; Weber, A.

    2010-11-10

    A novel series of {beta}-amino amides incorporating fused heterocycles, i.e., triazolopiperazines, were synthesized and evaluated as inhibitors of dipeptidyl peptidase IV (DPP-IV) for the treatment of type 2 diabetes. (2R)-4-Oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine (1) is a potent, orally active DPP-IV inhibitor (IC{sub 50} = 18 nM) with excellent selectivity over other proline-selective peptidases, oral bioavailability in preclinical species, and in vivo efficacy in animal models. MK-0431, the phosphate salt of compound 1, was selected for development as a potential new treatment for type 2 diabetes.

  7. 5HT4 agonists inhibit interferon-gamma-induced MHC class II and B7 costimulatory molecules expression on cultured astrocytes.

    PubMed

    Zeinstra, Esther M; Wilczak, Nadine; Wilschut, Jan C; Glazenburg, Lisa; Chesik, Daniel; Kroese, Frans G M; De Keyser, Jacques

    2006-10-01

    A failure of tight control of MHC class II expression on astrocytes may play a role in the development of autoimmune responses in multiple sclerosis. The 5-HT(4) serotonin receptor agonists cisapride and prucalopride, at concentrations between 10(-10) M and 10(-8) M, reduced interferon-gamma-induced MHC class II immunostaining in cultured astrocytes derived from newborn Wistar rats by approximately 50-60%. The magnitude of MHC class II inhibition by 5-HT(4) agonists was comparable to that of interferon-beta. The alpha(1)-adrenergic receptor agonist phenylephrine was without effect. Cisapride (10(-9) M) also prevented interferon-gamma-induced B7-1 and B7-2 immunostaining. Our results suggest that 5-HT(4) agonists may have therapeutic potential in multiple sclerosis by inhibiting the up-regulation of immune responsiveness of astrocytes in the central nervous system.

  8. N-Benzyl-2,7-diphenyl-1,4-diazepan-5-one analogues: Synthesis, spectral characterization, stereochemistry, crystal structure and molecular docking studies

    NASA Astrophysics Data System (ADS)

    Sethuvasan, S.; Sugumar, P.; Ponnuswamy, M. N.; Ponnuswamy, S.

    2016-10-01

    Three novel N-benzyl-2,7-diphenyl-1,4-diazepan-5-ones 10-12 have been synthesized via two routes starting from 2,7-diphenyl-1,4-diazepan-5-ones 4-6 and N-benzyl-2,6-diphenylpiperidin-4-ones 7-9. The structural characterization and conformational analysis of these synthesized compounds have been carried out using IR, mass and 1H, 13C, DEPT-135 and 2D (COSY and HSQC) NMR spectral techniques. The N-benzyldiazepan-5-one 10 is found to prefer chair conformation with equatorial orientation of alkyl and phenyl groups while N-benzyldiazepan-5-ones 11 &12 prefer to adopt twist-boat conformation with phenyl rings at C-2 & C-7 occupying equatorial and pseudo-axial orientations, respectively. The single crystal X-ray structure of compound 12 has been determined which also supports the twist-boat conformation. In silico molecular docking study has also been performed and the results show that the compounds 10-12 might exhibit inhibitory activity against HIV-1 protease. All the compounds are screened for their antibacterial activity against three bacterial strains (Staphylococcus aureus, Escherichia coli and Bacillus cereus) and only compound 11 shows moderate activity.

  9. Formal (4+1) Cycloaddition of Methylenecyclopropanes with 7-Aryl-1,3,5-cycloheptatrienes by Triple Gold(I) Catalysis**

    PubMed Central

    Wang, Yahui; Muratore, Michael E; Rong, Zhouting; Echavarren, Antonio M

    2014-01-01

    7-Aryl-1,3,5-cycloheptatrienes react intermolecularly with methylenecyclopropanes in a triple gold(I)-catalyzed reaction to form cyclopentenes. The same formal (4+1) cycloaddition occurs with cyclobutenes. Other precursors of gold(I) carbenes can also be used as the C1 component of the cycloaddition. PMID:24898850

  10. A facile access to new diazepines derivatives: Spectral characterization and crystal structures of 7-(thiophene-2-yl)-5-(trifluoromethyl)-2,3-dihydro-1H-1,4-diazepine and 2-thiophene-4-trifluoromethyl-1,5-benzodiazepine

    NASA Astrophysics Data System (ADS)

    Ahumada, Guillermo; Carrillo, David; Manzur, Carolina; Fuentealba, Mauricio; Roisnel, Thierry; Hamon, Jean-René

    2016-12-01

    The one-pot double condensation reaction of 2-thenoyltrifluoroacetone (2-TTA) with ethylendiamine or o-phenylenediamine, in a 2:1 stoichiometric molar ratio, leads to the formation of 7-(thiophene-2-yl)-5-(trifluoromethyl)-2,3-dihydro-1H-1,4-diazepine 2 and 2-thiophene-4-trifluoromethyl-1,5-benzodiazepine 3, that were isolated in 56 and 53% yields, respectively. The bis(trifluoroacetamide)ethylene derivative 1 was also isolated in 32% yield as a side-product in the reaction of 2-TTA and ethylenediamine. Compounds 1-3 were fully characterized by elemental analysis, FT-IR and multinuclear (1H, 13C and 19F) NMR spectroscopy. In addition, their molecular identities and geometries have been authenticated by single-crystal X-ray diffraction analysis. The spectroscopic and structural data confirm that the 1,4-diazepine 2 and the 1,5-benzodiazepine 3 exist in the imine-enamine and diimine tautomeric forms, respectively, both in solution and in the solid-state.

  11. Transcriptome Sequencing Identifies SPL7-Regulated Copper Acquisition Genes FRO4/FRO5 and the Copper Dependence of Iron Homeostasis in Arabidopsis[C][W

    PubMed Central

    Bernal, María; Casero, David; Singh, Vasantika; Wilson, Grandon T.; Grande, Arne; Yang, Huijun; Dodani, Sheel C.; Pellegrini, Matteo; Huijser, Peter; Connolly, Erin L.; Merchant, Sabeeha S.; Krämer, Ute

    2012-01-01

    The transition metal copper (Cu) is essential for all living organisms but is toxic when present in excess. To identify Cu deficiency responses comprehensively, we conducted genome-wide sequencing-based transcript profiling of Arabidopsis thaliana wild-type plants and of a mutant defective in the gene encoding SQUAMOSA PROMOTER BINDING PROTEIN-LIKE7 (SPL7), which acts as a transcriptional regulator of Cu deficiency responses. In response to Cu deficiency, FERRIC REDUCTASE OXIDASE5 (FRO5) and FRO4 transcript levels increased strongly, in an SPL7-dependent manner. Biochemical assays and confocal imaging of a Cu-specific fluorophore showed that high-affinity root Cu uptake requires prior FRO5/FRO4-dependent Cu(II)-specific reduction to Cu(I) and SPL7 function. Plant iron (Fe) deficiency markers were activated in Cu-deficient media, in which reduced growth of the spl7 mutant was partially rescued by Fe supplementation. Cultivation in Cu-deficient media caused a defect in root-to-shoot Fe translocation, which was exacerbated in spl7 and associated with a lack of ferroxidase activity. This is consistent with a possible role for a multicopper oxidase in Arabidopsis Fe homeostasis, as previously described in yeast, humans, and green algae. These insights into root Cu uptake and the interaction between Cu and Fe homeostasis will advance plant nutrition, crop breeding, and biogeochemical research. PMID:22374396

  12. BMP4 and BMP7 Suppress StAR and Progesterone Production via ALK3 and SMAD1/5/8-SMAD4 in Human Granulosa-Lutein Cells.

    PubMed

    Zhang, Han; Klausen, Christian; Zhu, Hua; Chang, Hsun-Ming; Leung, Peter C K

    2015-11-01

    Adequate production of progesterone by the corpus luteum is critical to the successful establishment of pregnancy. In animal models, bone morphogenetic protein (BMP) 4 and BMP7 have been shown to suppress either basal or gonadotropin-induced progesterone production, depending on the species examined. However, the effects of BMP4 and BMP7 on progesterone production in human granulosa cells are unknown. In the present study, we used immortalized (SVOG) and primary human granulosa-lutein cells to investigate the effects of BMP4 and BMP7 on steroidogenic acute regulatory protein (StAR) expression and progesterone production and to examine the underlying molecular mechanism. Treatment of primary and immortalized human granulosa cells with recombinant BMP4 or BMP7 decreased StAR expression and progesterone accumulation. In SVOG cells, the suppressive effects of BMP4 and BMP7 on StAR expression were blocked by pretreatment with inhibitors of activin receptor-like kinase (ALK)2/3/6 (dorsomorphin) or ALK2/3 (DMH1) but not ALK4/5/7 (SB-431542). Moreover, small interfering RNA-mediated depletion of ALK3, but not ALK2 or ALK6, reversed the effects of BMP4 and BMP7 on StAR expression. Likewise, BMP4- and BMP7-induced phosphorylation of SMAD 1/5/8 was reversed by treatment with DMH1 or small interfering RNA targeting ALK3. Knockdown of SMAD4, the essential common SMAD for BMP/TGF-β signaling, abolished the effects of BMP4 and BMP7 on StAR expression. Our results suggest that BMP4 and BMP7 down-regulate StAR and progesterone production via ALK3 and SMAD1/5/8-SMAD4 signaling in human granulosa-lutein cells.

  13. Formation of a highly stable complex between BN 50730 [tetrahydro-4,7,8,10 methyl-1(chloro-2 phenyl)-6 (methoxy-4 phenyl-carbamoyl)-9 pyrido [4',3'-4,5] thieno [3,2-f] triazolo-1,2,4 [4,3-a] diazepine-1,4] and the platelet-activating factor receptor in rabbit platelet membranes.

    PubMed

    Silva, C L; Cruz, H N; Violante, F A; Cordeiro, R S; Martins, M A; Noël, F

    1996-01-26

    BN 50730 [tetrahydro-4,7,8,10 methyl-1(chloro-2 phenyl)-6 (methoxy-4 phenyl-carbamoyl)-9 pyrido [4',3'-4,5] thieno [3,2-f] triazolo-1,2,4 [4,3-alpha] diazepine-1,4], a novel platelet-activating factor (PAF) receptor antagonist with a hetrazepine structure, decreased the maximal number of binding sites (Bmax) of [3H]PAF in rabbit platelet membranes without altering its dissociation constant. Platelet aggregation induced by 1 microM PAF was prevented by preincubation with 1 microM BN 50730. The washing of the platelets preincubated with BN 50730 failed to revert its inhibitory effects. We conclude that BN 50730 acts as a non-competitive antagonist of the PAF receptor, due to the formation of a highly stable drug-receptor complex.

  14. Synthesis of new mixed valence compounds MV{sup 5+}V{sub 2}{sup 4+}O{sub 7}(M=NH{sub 4},K): Crystal structure of NH{sub 4}V{sub 3}O{sub 7} and electrical properties of KV{sub 3}O{sub 7}

    SciTech Connect

    Trombe, J.C. Szajwaj, O.; Salles, Ph.; Galy, Jean

    2007-07-15

    A new mixed valence compound, NH{sub 4}V{sub 3}O{sub 7}, as single crystals, has been synthesized hydrothermally. It crystallizes in the monoclinic system, space group I2/m with lattice parameters a=12.198(1)A, b=3.7530(2)A, c=13.178(1)A, {beta}=100.532(6){sup o}, V=593.11(7)A{sup 3}, Z=4. The crystal structure determined with R=0.038 consists of (V{sub 3}O{sub 7}){sub n} layers linked by ammonium cations. The layer is built up by replication through symmetry elements of three independent distorted octahedra sharing edges and corners. The distortion of vanadium octahedra tends to vary and the coordination number CN is reasonably selected as equal to 5+1. KV{sub 3}O{sub 7}, synthesized by the mild hydrothermal route as a largely pure phase, is isostructural and its semi-conductive character is indicative of the presence of V{sup 4+} and V{sup 5+} sites. These are mixed valence compounds MV{sup 5+}V{sub 2}{sup 4+}O{sub 7}, the vanadium localization on three independent crystallographic sites enabling their electric behavior by electron hopping.

  15. How Slow Can We Go? 4 Frames Per Second (fps) Versus 7.5 fps Fluoroscopy for Atrial Septal Defects (ASDs) Device Closure.

    PubMed

    Hiremath, Gurumurthy; Meadows, Jeffery; Moore, Phillip

    2015-06-01

    Radiation exposure remains a significant concern for ASD device closure. In an effort to reduce radiation exposure, the default fluoroscopy frame rate in our Siemens biplane pediatric catheterization laboratory was reduced to 4 fps in November 2013 from an earlier 7.5 fps fluoro rate. This study aims to evaluate the components contributing to total radiation exposure and compare the procedural success and radiation exposure during ASD device closure using 4 versus 7.5 fps fluoroscopy rates. Twenty ASD device closures performed using 4 fps fluoro rate were weight-matched to 20 ASD closure procedures using 7.5 fps fluoro rate. Baseline characteristics, procedure times and case times were similar in the two groups. Device closure was successful in all but one case in the 4 fps group. The dose area product (DAP), normalized DAP to body weight, total radiation time and fluoro time were lower in the 4 fps group but not statistically different than the 7.5 fps. The number of cine images and cine times were identical in both groups. Fluoroscopy and cineangiography contributed equally to radiation exposure. Fluoroscopy at 4 fps can be safe and effective for ASD device closure in children and adults. There was no increase in procedure time, cine time, fluoro time or complications at this slow fluoro rate. There was a trend toward decreased radiation exposure as measured by indexed DAP although not statistically significant in this small study. Further study with multiple operators using 4 fps fluoroscopy for simple interventional procedures is recommended.

  16. Two New Crystals in Li(m)Cs(n)B(m+n)O2(m+n) (m + n = 5, 7; m > n) Series: Noncentrosymmetric Li5Cs2B7O14 and Centrosymmetric Li4CsB5O10.

    PubMed

    Li, Lin; Han, Shujuan; Lei, Binghua; Dong, Xiaoyu; Wu, Hongping; Zhou, Zhongxiang; Yang, Zhihua; Pan, Shilie

    2015-08-03

    With the introduction of an alkali metal into the B-O framework, two new alkali metal borate crystals, Li5Cs2B7O14 and Li4CsB5O10, have been obtained for the first time. Both compounds obey a general formula of Li(m)Cs(n)B(m+n)O2(m+n) (m + n = 5, 7; m > n). The two crystals have different three-dimensional (3D) framework structures composed by LiOn (n = 4, 5), CsO10, BO3, and BO4 units. Li5Cs2B7O14 crystallizes into the polar and noncentrosymmetric space group Ama2, while Li4CsB5O10 belongs to the nonpolar and centrosymmetric space group P21/c. Detailed structure comparison analysis indicates that the different arrangements of the anionic groups in Li(m)Cs(7-m)B7O14 (m = 4, 5) and Li(m)Cs(5-m)B5O10 (m = 3, 4) may arise from the cation size effects, bond-valence requirements, and differences of coordination environment. In addition, in order to get better understandings of electronic structures and linear optical properties, we also carried out first-principle theoretical studies.

  17. The Ultra-Red Color of Kuiper Belt Objects in the 5:3 and 7:4 Mean Motion Neptune Resonances

    NASA Astrophysics Data System (ADS)

    Sheppard, Scott S.

    2012-10-01

    New optical colors of objects in mean motion resonances with Neptune show the various resonant populations have significantly different color distributions. The 5:3 and 7:4 resonances have semi-major axes near the middle of the main Kuiper Belt and both are dominated by ultra-red material. The 5:3 and 7:4 resonances have statistically the same color distribution as the low inclination ``cold'' classical belt. The inner 4:3 and distant 5:2 resonances have objects with mostly moderately red colors, similar to the scattered and detached disk populations. The 2:1 resonance, which is near the outer edge of the main Kuiper Belt, has a large range of colors with similar numbers of moderately red and ultra-red objects at all inclinations. The inner 3:2 resonance, like the outer 2:1, has a large range of objects from neutral to ultra-red. The Neptune Trojans (1:1 resonance) are only slightly red, similar to the Jupiter Trojans. The inner 5:4 resonance only has four objects with measured colors but shows equal numbers of ultra-red and moderately red objects. The 9:5, 12:5, 7:3, 3:1 and 11:3 resonances do not have reliable color distribution statistics, though it appears noteworthy that all three of the measured 3:1 objects have only moderately red colors, similar to the 4:3 and 5:2 resonances. The different color distributions are likely a result from the disruption of the primordial Kuiper Belt from the scattering and migration of the giant planets. The few low inclination objects known in the outer 2:1 and 5:2 resonances are mostly only moderately red. This suggests if the 2:1 and 5:2 have a cold low inclination component, the objects likely had a significantly different origin than the ultra-red dominated cold components of the cold classical belt and 5:3 and 7:4 resonances. This work has been accepted for publication in the Astronomical Journal.

  18. 7 CFR 254.5 - Household eligibility.

    Code of Federal Regulations, 2014 CFR

    2014-01-01

    ... 7 Agriculture 4 2014-01-01 2014-01-01 false Household eligibility. 254.5 Section 254.5 Agriculture Regulations of the Department of Agriculture (Continued) FOOD AND NUTRITION SERVICE, DEPARTMENT OF AGRICULTURE... 253.7. (b) Urban places. No household living in an urban place in Oklahoma shall be eligible for...

  19. 7 CFR 254.5 - Household eligibility.

    Code of Federal Regulations, 2013 CFR

    2013-01-01

    ... 7 Agriculture 4 2013-01-01 2013-01-01 false Household eligibility. 254.5 Section 254.5 Agriculture Regulations of the Department of Agriculture (Continued) FOOD AND NUTRITION SERVICE, DEPARTMENT OF AGRICULTURE... 253.7. (b) Urban places. No household living in an urban place in Oklahoma shall be eligible for...

  20. 7 CFR 254.5 - Household eligibility.

    Code of Federal Regulations, 2010 CFR

    2010-01-01

    ... 7 Agriculture 4 2010-01-01 2010-01-01 false Household eligibility. 254.5 Section 254.5 Agriculture Regulations of the Department of Agriculture (Continued) FOOD AND NUTRITION SERVICE, DEPARTMENT OF AGRICULTURE... 253.7. (b) Urban places. No household living in an urban place in Oklahoma shall be eligible for...

  1. 7 CFR 254.5 - Household eligibility.

    Code of Federal Regulations, 2011 CFR

    2011-01-01

    ... 7 Agriculture 4 2011-01-01 2011-01-01 false Household eligibility. 254.5 Section 254.5 Agriculture Regulations of the Department of Agriculture (Continued) FOOD AND NUTRITION SERVICE, DEPARTMENT OF AGRICULTURE... 253.7. (b) Urban places. No household living in an urban place in Oklahoma shall be eligible for...

  2. A novel synthesis and pharmacological evaluation of a potential dopamine D1/D2 agonist: 1-propyl-1,2,3,4,4a,5,10,10a-octahydrobenzo[g]quinoline-6,7-diol.

    PubMed

    Liu, Danyang; Dijkstra, Durk; de Vries, Jan B; Wikström, Håkan V

    2008-03-15

    Previously, we have demonstrated that enone prodrugs of dopaminergic catecholamines represent a new type of dopamine (DA) agonist. Trans-1-propyl-1,2,3,4,4a,5,10,10a-octahydrobenzo[g]quinoline-6,7-diol (TL-334), the active form of trans-1-propyl-2,3,4,4a,5,7,8,9,10,10a-decahydro-1H-benzo[g]quinolin-6-one (GMC-6650), in vivo showed an extremely potent dopaminergic activity. Here, we report a novel synthesis and a pharmacological evaluation of TL-334 by means of microdialysis.

  3. Photophysical properties of ESIPT inspired fluorescent 2-(2-hydroxyphenyl)-6-methylimidazo[4,5-f]isoindole-5,7(1H,6H)-dione and its derivative: Experimental and DFT based approach

    NASA Astrophysics Data System (ADS)

    Deshmukh, Mininath S.; Sekar, Nagaiyan

    2015-01-01

    The excited-state intramolecular proton transfer chromophores 2-(2-hydroxyphenyl)-6-methylimidazo[4,5-f]isoindole-5,7(1H,6H)-dione and 2-(4-(diethylamino)-2-hydroxyphenyl)-6-methylimidazo[4,5-f]isoindole-5,7(1H,6H)-dione are synthesized from 4,5-diamino-N-methylphthalimide. The photophysical behavior of the synthesized chromophores was studied using UV-visible and fluorescence spectroscopy in the polar and non-polar solvents. The synthesized o-hydroxyphenyl benzimidazole derivatives are fluorescent and very sensitive to the solvent polarity. These dyes are thermally stable up to 317 °C. Density Functional Theory computations have been used to understand the structural, molecular, electronic and photophysical properties of the chromophores. The experimental absorption and emission wavelengths are in good agreement with the computed vertical excitation and theoretical emission obtained by Density Functional Theory and Time Dependant Density Functional Theory.

  4. Photoabsorption of the ground state of Ne and of Ne-like Na+, Mg2+, Al3+, Si4+, P5+, S6+, and Cl7+ ions

    NASA Astrophysics Data System (ADS)

    Sakho, I.

    2016-03-01

    Photoabsorption of the 1s2 2s2 2p6 (1S0) ground state of Ne-like ions is presented in this paper. Resonance energies and width of the 2 s 2p6 n p1P1 series of Ne and Ne-like Na+, Mg2+, Al3+, Si4+, P5+, S6+, and Cl7+ ions are reported. Wavelengths of the 2s2 2p6 (1S0) → 2s2 2p5(2P 3 / 2 , 1 / 2) n d transitions in neon-like Na+ ion and of the 2s2 2p6(1S0) → 2 s 2p6 n p1P1 transitions in Ne and in Ne-like Na+, Mg2+, Al3+, Si4+, P5+, S6+, and Cl7+ ions are tabulated. Analysis of the resonances investigated is done in the framework of the LS, jj and JK coupling schemes. All the calculations are made using the Screening constant by unit nuclear charge (SCUNC) formalism. Very good agreement is found between the SCUNC results and various experimental and theoretical literature values and new data for the Ne-like Si4+, P5+, S6+, and Cl7+ ions are listed.

  5. Molecular analysis of the VP7, VP4, VP6, NSP4, and NSP5/6 genes of a buffalo rotavirus strain: identification of the rare P[3] rhesus rotavirus-like VP4 gene allele.

    PubMed

    Martella, V; Ciarlet, M; Pratelli, A; Arista, S; Terio, V; Elia, G; Cavalli, A; Gentile, M; Decaro, N; Greco, G; Cafiero, M A; Tempesta, M; Buonavoglia, C

    2003-12-01

    We report the detection and molecular characterization of a rotavirus strain, 10733, isolated from the feces of a buffalo calf affected with diarrhea in Italy. Strain 10733 was classified as a P[3] rotavirus, as the VP8* trypsin cleavage product of the VP4 protein revealed a high amino acid identity (96.2%) with that of rhesus rotavirus strain RRV (P5B[3]), used as the recipient virus in the human-simian reassortant vaccine. Analysis of the VP7 gene product revealed that strain 10733 possessed G6 serotype specificity, a type common in ruminants, with an amino acid identity to G6 rotavirus strains ranging from 88 to 98%, to Venezuelan bovine strain BRV033, and Hungarian human strain Hun4. Phylogenetic analysis based on the VP7 gene of G6 rotaviruses identified at least four lineages and an apparent linkage between each lineage and the VP4 specificity, suggesting the occurrence of repeated interspecies transmissions and genetic reassortment events between ruminant and human rotaviruses. Moreover, strain 10733 displayed a bovine-like NSP4 and NSP5/6 and a subgroup I VP6 specificity, as well as a long electropherotype pattern. The detection of the rare P[3] genotype in ruminants provides additional evidence for the wide genetic and antigenic diversity of group A rotaviruses.

  6. Global emission estimates and radiative impact of C4F10, C5F12, C6F14, C7F16 and C8F18

    NASA Astrophysics Data System (ADS)

    Ivy, D. J.; Rigby, M.; Baasandorj, M.; Burkholder, J. B.; Prinn, R. G.

    2012-08-01

    Global emission estimates based on new atmospheric observations are presented for the acylic high molecular weight perfluorocarbons (PFCs): decafluorobutane (C4F10), dodecafluoropentane (C5F12), tetradecafluorohexane (C6F14), hexadecafluoroheptane (C7F16) and octadecafluorooctane (C8F18). Emissions are estimated using a 3-dimensional chemical transport model and an inverse method that includes a growth constraint on emissions. The observations used in the inversion are based on newly measured archived air samples that cover a 39-yr period, from 1973 to 2011, and include 36 Northern Hemispheric and 46 Southern Hemispheric samples. The derived emission estimates show that global emission rates were largest in the 1980s and 1990s for C4F10 and C5F12, and in the 1990s for C6F14, C7F16 and C8F18. After a subsequent decline, emissions have remained relatively stable, within 20%, for the last 5 yr. Bottom-up emission estimates are available from the Emission Database for Global Atmospheric Research version 4.2 (EDGARv4.2) for C4F10, C5F12, C6F14 and C7F16, and inventories of C4F10, C5F12 and C6F14 are reported to the United Nations' Framework Convention on Climate Change (UNFCCC) by Annex 1 countries that have ratified the Kyoto Protocol. The atmospheric measurement-based emission estimates are 20 times larger than EDGARv4.2 for C4F10 and over three orders of magnitude larger for C5F12 (with 2008 EDGARv4.2 estimates for C5F12 at 9.6 kg yr-1, as compared to 67±53 t yr-1 as derived in this study). The derived emission estimates for C6F14 largely agree with the bottom-up estimates from EDGARv4.2. Moreover, the C7F16 emission estimates are comparable to those of EDGARv4.2 at their peak in the 1990s, albeit significant underestimation for the other time periods. There are no bottom-up emission estimates for C8F18, thus the emission rates reported here are the first for C8F18. The reported inventories for C4F10, C5F12 and C6F14 to UNFCCC are five to ten times lower than those

  7. Synthesis and antiparasitic and antitumor activity of 2, 4-diamino-6-(arylmethyl)-5,6,7,8-tetrahydroquinazoline analogues of piritrexim.

    PubMed

    Rosowsky, A; Papoulis, A T; Forsch, R A; Queener, S F

    1999-03-25

    Nineteen previously undescribed 2,4-diamino-6-(arylmethyl)-5,6,7, 8-tetrahydroquinazolines (5a-m, 10-12) were synthesized as part of a larger effort to assess the therapeutic potential of lipophilic dihydrofolate reductase (DHFR) inhibitors against opportunistic infections of AIDS. Condensation of appropriately substituted (arylmethyl)triphenylphosphoranes with 4, 4-ethylenedioxycyclohexanone, followed by hydrogenation (H2/Pd-C) and acidolysis, yielded the corresponding 4-(arylmethyl)cyclohexanones, which were then condensed with cyanoguanidine to form the tetrahydroquinazolines. Three simple 2, 4-diamino-6-alkyl-5,6,7,8-tetrahydroquinazoline model compounds (9a-c) were also prepared in one step from commercially available 4-alkylcyclohexanones by this method. Enzyme inhibition assays against rat liver DHFR, Pneumocystis carinii DHFR, and the bifunctional DHFR-TS enzyme from Toxoplasma gondii were carried out, and the selectivity ratios IC50(rat)/IC50(P. carinii) and IC50(rat)/IC50(T. gondii) were compared. The three most potent inhibitors of P. carinii DHFR were the 2,5-dimethoxybenzyl (5j), 3, 4-dimethoxybenzyl (5k), and 3,4,5-trimethoxybenzyl (5l) analogues, with IC50 values of 0.057, 0.10, and 0.091 microM, respectively. The remaining compounds generally had IC50 values in the 0.1-1.0 microM range. However all the compounds were more potent against the rat liver enzyme than the P. carinii enzyme and thus were nonselective. The T. gondii enzyme was always more sensitive than the P. carinii enzyme, with most of the analogues giving IC50 values of 0.01-0.1 microM. Moderate 5-10-fold selectivity for T. gondii versus rat liver DHFR was observed with five compounds, the best combination of potency and selectivity being achieved with the 2-methoxybenzyl analogue 5d, which had an IC50 of 0.014 microM and a selectivity ratio of 8.6. One compound (5l) was tested for antiproliferative activity against P. carinii trophozoites in culture at a concentration of 10 microgram

  8. Lanthanide complexes containing 5-methyl-1,2,4-triazolo[1,5-a] pyrimidin-7(4H)-one and their therapeutic potential to fight leishmaniasis and Chagas disease.

    PubMed

    Caballero, Ana B; Rodríguez-Diéguez, Antonio; Salas, Juan M; Sánchez-Moreno, Manuel; Marín, Clotilde; Ramírez-Macías, Inmaculada; Santamaría-Díaz, Noelia; Gutiérrez-Sánchez, Ramón

    2014-09-01

    In the last years, numerous and significant advances in lanthanide coordination chemistry have been achieved. The unique chemical nature of these metal ions which is conferred by their f-electrons has led to a wide range of coordination compounds with interesting structural, physical and also biological properties. Consequently, lanthanide complexes have found applications mainly in catalysis, gas adsorption, photochemistry and as diagnostic tools. However, research on their therapeutic potential and the understanding of their mechanism of action is still taking its first steps, and there is a distinct lack of research in the parasitology field. In the present work, we describe the synthesis and physical properties of seven new lanthanide complexes with the anionic form of the bioactive ligand 5-methyl-1,2,4-triazolo[1,5-a]pyrimidin-7(4H)-one (HmtpO), namely [Ln(mtpO)3(H2O)6]·9H2O (Ln=La(III), Nd(III), Eu(III), Gd(III), Tb(III), Dy(III) and Er(III)). In addition, results on the in vitro antiproliferative activity against Leishmania spp. and Trypanosoma cruzi are described. The high activity of the new compounds against parasite proliferation and their low cytotoxicity against reference host cell lines show a great potential of this type of compounds to become a new generation of highly effective and non-toxic antiparasitic agents to fight the so considered neglected diseases leishmaniasis and Chagas disease.

  9. Diethyl 2,3-dihydro-thieno[3,4-b]-1,4-dioxine-5,7-dicarboxyl-ate.

    PubMed

    Ono, Katsuhiko; Tomura, Masaaki; Saito, Katsuhiro

    2008-01-18

    The title compound, C(12)H(14)O(6)S, is a dicarboxylic acid diethyl ester of 3,4-ethyl-enedioxy-thio-phene, which is a component of electrically conductive poly(3,4-ethyl-enedioxy-thio-phene) (PEDOT). The ethyl-ene group is disordered over two sites with occupancy factors 0.64 and 0.36. Both the carbonyl groups are coplanar with the thio-phene ring. The mol-ecules form centrosymmetric dimers with an R(2) (2)(12) coupling by inter-molecular C-H⋯O hydrogen bonds [3.333 (5) Å] at the ethoxy-carbonyl groups. The dimer units are arranged to form a ribbon-like mol-ecular sheet.

  10. Cargo-selective apical exocytosis in epithelial cells is conducted by Myo5B, Slp4a, Vamp7, and Syntaxin 3

    PubMed Central

    Vogel, Georg F.; Klee, Katharina M.C.; Janecke, Andreas R.; Müller, Thomas

    2015-01-01

    Mutations in the motor protein Myosin Vb (Myo5B) or the soluble NSF attachment protein receptor Syntaxin 3 (Stx3) disturb epithelial polarity and cause microvillus inclusion disease (MVID), a lethal hereditary enteropathy affecting neonates. To understand the molecular mechanism of Myo5B and Stx3 interplay, we used genome editing to introduce a defined Myo5B patient mutation in a human epithelial cell line. Our results demonstrate a selective role of Myo5B and Stx3 for apical cargo exocytosis in polarized epithelial cells. Apical exocytosis of NHE3, CFTR (cystic fibrosis transmembrane conductance regulator), and GLUT5 required an interaction cascade of Rab11, Myo5B, Slp4a, Munc18-2, and Vamp7 with Stx3, which cooperate in the final steps of this selective apical traffic pathway. The brush border enzymes DPPIV and sucrase-isomaltase still correctly localize at the apical plasma membrane independent of this pathway. Hence, our work demonstrates how Myo5B, Stx3, Slp4a, Vamp7, Munc18-2, and Rab8/11 cooperate during selective apical cargo trafficking and exocytosis in epithelial cells and thereby provides further insight into MVID pathophysiology. PMID:26553929

  11. A simple isocratic HPLC method for the simultaneous determination of sinensetin, eupatorin, and 3'-hydroxy-5,6,7,4'-tetramethoxyflavone in Orthosiphon stamineus extracts.

    PubMed

    Yam, Mun Fei; Mohamed, Elsnoussi Ali Hussin; Ang, Lee Fung; Pei, Li; Darwis, Yusrida; Mahmud, Roziahanim; Asmawi, Mohd Zaini; Basir, Rusliza; Ahmad, Mariam

    2012-08-01

    Orthosiphon stamineus extracts contain three flavonoids (3'-hydroxy-5,6,7,4'-tetramethoxyflavone, sinensetin, and eupatorin) as bioactive substances. Previous reported high performance liquid chromatography- ultraviolet (HPLC-UV) methods for the determination of these flavonoids have several disadvantages, including unsatisfactory separation times and not being well validated according to International Conference on Harmonisation of Technical Requirements for Registration of Pharmaceuticals for Human Use (ICH) standard guidelines. A rapid, specific reversed-phase HPLC method with isocratic elution of acetonitrile: isopropyl alcohol: 20mM phosphate buffer (NaH(2)PO(4)) (30:15:55, v/v) (pH 3.5) at a flow-rate of 1ml/minute, a column temperature of 25°C, and ultraviolet (UV) detection at 340 nm was developed. The method was validated and applied for quantification of different types of O stamineus extracts and fractions. The method allowed simultaneous determination of 3'-hydroxy-5,6,7,4'-tetramethoxyflavone, sinensetin, and eupatorin in the concentration range of 0.03052-250 μg/ml. The limits of detection and quantification, respectively, were 0.0076 and 0.061 μg/ml for 3'-hydroxy-5,6,7,4'-tetramethoxyflavone, 0.0153 and 0.122 μg/ml for sinensetin and 0.0305 and 0.122 μg/ml for eupatorin. The percent relative standard deviation (% RSD) values for intraday were 0.048-0.368, 0.025-0.135, and 0.05-0.476 for 3'-hydroxy-5,6,7,4'-tetramethoxyflavone, sinensetin, and eupatorin, respectively, and those for intraday precision were 0.333-1.688, 0.722-1.055, and 0.548-1.819, respectively. The accuracy for intraday were 91.25%-103.38%, 94.32%-109.56%, and 92.85%-109.70% for 3'-hydroxy-5,6,7,4'-tetramethoxyflavone, sinensetin, and eupatorin, respectively, and those for interday accuracy were 97.49%-103.92%, 103.58%-104.57%, and 103.9%-105.33%, respectively. The method was found to be simple, accurate and precise and is recommended for routine quality control analysis of O

  12. Red long-lasting phosphorescence (LLP) in β-TCP type Ca 9.5Mn(PO 4) 7 compounds

    NASA Astrophysics Data System (ADS)

    Lecointre, A.; Ait Benhamou, R.; Bessiére, A.; Wallez, G.; Elaatmani, M.; Viana, B.

    2011-12-01

    Mn-ion doped calcium phosphates namely Ca 5(PO 4) 3(OH) hydroxyapatite (HAP), β-Ca 3(PO 4) 2 (β-TCP) as well as Ca 9.5Mn(PO 4) 7 whitlockite were synthesized and the optical properties of the Mn 2+ cations were investigated. Annealing under reducing atmosphere enhances the emission of the divalent manganese species. Electron paramagnetic resonance (EPR) and optical spectroscopies confirm that Mn 2+ ions are the active species. Orange and red emissions occur respectively for the Mn:HAP and Mn:TCP. For this latter, long-lasting phosphorescence (LLP) coming from the Mn 2+ emission ( 4T 1 → 6A 1 transition) is observed at 640 nm but it appears that the traps depths are either two shallow or too deep to lead to an efficient long-lasting emission.

  13. Deposition of calcium phosphate coatings using condensed phosphates (P2O7(4-) and P3O10(5-)) as phosphate source through induction heating.

    PubMed

    Zhou, Huan; Hou, Saisai; Zhang, Mingjie; Yang, Mengmeng; Deng, Linhong; Xiong, Xinbo; Ni, Xinye

    2016-12-01

    In present work condensed phosphates (P2O7(4-) and P3O10(5-)) were used as phosphate source in induction heating to deposit calcium phosphate coatings. The phase, morphology, and composition of different phosphate-related coatings were characterized and compared using XRD, FTIR, and SEM analyses. Results showed that P2O7(4-)formed calcium pyrophosphate hydrate coatings with interconnected cuboid-like particles. The as-deposited calcium tripolyphosphate hydrate coating with P3O10(5-) was mainly composed of flower-like particles assembled by plate-like crystals. The bioactivity and cytocompatibility of the coatings were also studied. Moreover, the feasibility of using hybrid phosphate sources for preparing and depositing coatings onto magnesium alloy was investigated.

  14. Hydrogen-bonded and π-interaction assembly in two 8-alkoxycarbonyl-1,8-diazabicyclo[5.4.0]undec-7-enium chloride salts.

    PubMed

    Mesto, E; Quaranta, E

    2013-04-01

    The crystal structures of 8-phenoxycarbonyl-1,8-diazabicyclo[5.4.0]undec-7-enium chloride, C16H21N2O2(+)·Cl(-), (I), and 8-methoxycarbonyl-1,8-diazabicyclo[5.4.0]undec-7-enium chloride monohydrate, C11H19N2O2(+)·Cl(-)·H2O, (II), recently reported by Carafa, Mesto & Quaranta [Eur. J. Org. Chem. (2011), pp. 2458-2465], are analysed and discussed with a focus on crystal interaction assembly. Both compounds crystallize in the space group P2(1)/c. The crystal packings are characterized by dimers linked through π-π stacking interactions and intermolecular nonclassical hydrogen bonds, respectively. Additional intermolecular C-H···Cl interactions [in (I) and (II)] and classical O-H···Cl hydrogen bonds [in (II)] are also evident and contribute to generating three-dimensional hydrogen-bonded networks.

  15. Novel 2-phenyl-4,5,6,7-tetrahydro[b]benzothiophene analogues as selective COX-2 inhibitors: Design, synthesis, anti-inflammatory evaluation, and molecular docking studies.

    PubMed

    Khatri, Chetan K; Indalkar, Krishna S; Patil, Chandragouda R; Goyal, Sameer N; Chaturbhuj, Ganesh U

    2017-04-15

    A series of 2-phenyl-4,5,6,7-tetrahydro[b]benzothiophene derivatives were synthesized and evaluated for in vitro COX inhibitory potential. Within the series, compounds 4a, 4j, 4k, and 4q were identified as potential and selective COX-2 inhibitors with COX-2 IC50 in 0.31-1.40µM range; COX-2 selectivity index (SI)=48.8-183.8 range and they showed percent PGE-2 inhibitory activity in the range of 25.4-46.9. Further, compounds 4a, 4j, 4k and 4q displayed potent anti-inflammatory activity with percentage rise in paw volume ranging from 21.1-30.5 at 180min, while celecoxib demonstrated 19.6 percentage rise at the same dose at 180min in carrageenan-induced rat paw edema assay. Cell viability via MTT assay showed no cytotoxicity up to 80µM concentrations. Molecular docking study of potent compounds in the series showed Gscore comparable to celecoxib with similar binding orientation for the COX-2 active site which also corroborates the observed in vitro COX-2 inhibition.

  16. Synthesis and pharmacological evaluation of pyrazolo[1,5-a]pyrimidin-7(4H)-one derivatives as potential GABAA-R ligands.

    PubMed

    Guerrini, Gabriella; Ciciani, Giovanna; Daniele, Simona; Di Cesare Mannelli, Lorenzo; Ghelardini, Carla; Martini, Claudia; Selleri, Silvia

    2017-03-15

    The synthesis of a new series of 6-phenyl- and 6-benzylpyrazolo[1,5-a]pyrimidin-7(4H)-ones 2a-g and 3a-g, strictly related to derivatives with pyrazolobenzotriazine (PBT) and pyrazoloquinazoline (PQ) scaffold, was realized. The in vitro GABAA-receptor subtype affinity was evaluated and from preliminary pharmacological studies, compound 3g shows anxiolytic-like effect at 10-30mg/kg.

  17. Theoretical vibrations of carbon chains C3, C4, C5, C6, C7, C8, and C9

    NASA Technical Reports Server (NTRS)

    Kurtz, Joe; Adamowicz, Ludwik

    1991-01-01

    The MBPT (2) procedure with the 6-31g (asterisk) basis set was used to study nearly linear carbon chains. The theoretical vibrational frequencies of the molecules C3 through C9 are presented and, for C3 through C6, compared to experimental stretching frequencies and their (C-13)/(C-12) isotopomers. Predictions for C7, C8, and C9 stretching frequencies are calculated by directly scaling the theoretical frequencies with factors derived from experimental-to-theoretical ratios known for the smaller molecules.

  18. Synthesis and acetylcholinesterase/butyrylcholinesterase inhibition activity of 4-amino-2, 3-diaryl-5, 6, 7, 8-tetrahydrofuro(and thieno)[2, 3-b]-quinolines, and 4-amino-5, 6, 7, 8, 9-pentahydro-2, 3-diphenylcyclohepta[e]furo(and thieno)-[2, 3-b]pyridines.

    PubMed

    Marco, José L; De Los Ríos, Cristóbal; Carreiras, María C; Baños, Josep E; Badia, Albert; Vivas, Nuria M

    2002-07-01

    The acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) inhibition activities of a series of 4-amino-2, 3-diaryl-5, 6, 7, 8-tetrahydrofuro[2, 3-b]quinolines (10-12)/4-amino-5, 6, 7, 8-tetrahydro-2, 3-diphenylthieno[2, 3-b]quinoline (14) and 4-amino-5, 6, 7, 8, 9-pentahydro-2, 3-diphenylcyclohepta[e]furo[2, 3-b]pyridine (13)/4-amino-5, 6, 7, 8, 9-pentahydro-2, 3-phenylcyclohepta[e]thieno[2, 3-b]pyridine (15) are described. These compounds are tacrine (THA) analogues which have been prepared either from readily available 2-amino-3-cyano-4, 5-diarylfurans (16-18) or from 2-amino-3-cyano-4, 5-diphenylthiophene (19), via Friedländer condensation with cyclohexanone or cycloheptanone. These compounds are competitive inhibitors for acetylcholinesterase, the more potent being compound (13) which is three-fold less active than tacrine. The butyrylcholinesterase inhibition activity is significant only in compounds 10 and133, which are ten-fold less active than tacrine. It is found that the products 11 and 12 strongly inhibit acetylcholinesterase, and show excellent selectivity regarding butyrylcholinesterase.

  19. Diversity oriented synthesis of a vinblastine-templated library of 7-aryl-octahydroazonino[5,4-b]indoles via a three-component reaction.

    PubMed

    Fokas, Demosthenes; Kaselj, Mira; Isome, Yuko; Wang, Zhimin

    2013-01-14

    A vinblastine-templated library of 7-aryl-octahydroazonino[5,4-b]indoles was prepared by a three-component reaction from indolizino[8,7-b]indoles, chloroformates, and activated arenes via a chloroformate mediated fragmentation of the indolizinoindole nucleus followed by insertion of an activated arene. In addition to N3-carbamoyl-7-aryl-octahydroazonino[5,4-b]indoles prepared in one step, a wide range of N3-substituted substrates were synthesized in one pot via the derivatization of a versatile N3-H-azonino[5,4-b]indole intermediate generated in situ by application of the same strategy. A subset of 308 compounds out of a virtual library of 3216, representing 13 different chemotypes, was prepared by high throughput solution-phase synthesis and subsequently purified by mass-triggered high performance liquid chromatography (HPLC). A total of 188 compounds with a minimum purity of 80% by UV214 nm and 85% by evaporative light scattering detection (ELSD) was isolated for primary screening.

  20. Global emission estimates and radiative impact of C4F10, C5F12, C6F14, C7F16 and C8F18

    NASA Astrophysics Data System (ADS)

    Ivy, D. J.; Rigby, M.; Baasandorj, M.; Burkholder, J. B.; Prinn, R. G.

    2012-05-01

    Global emission estimates based on new atmospheric observations are presented for the acylic high molecular weight perfluorocarbons (PFCs): decafluorobutane (C4F10), dodecafluoropentane (C5F12), tetradecafluorohexane (C6F14), hexadecafluoroheptane (C7F16) and octadecafluorooctane (C8F18). Emissions are estimated using a 3-dimensional chemical transport model and an inverse method that includes a growth constraint on emissions. The observations used in the inversion are based on newly measured archived air samples that cover a 39-yr period, from 1973 to 2011, and include 36 Northern Hemispheric and 46 Southern Hemispheric samples (Ivy et al., 2012). The derived emission estimates show that global emission rates were largest in the 1980s and 1990s for C4F10 and C5F12, and in the 1990s for C6F14,C7F16 and C8F18. After a subsequent decline, emissions have remained relatively stable, within 20%, for the last 5 yr. Bottom-up emission estimates are available from the Emission Database for Global Atmospheric Research version 4.2 (EDGARv4.2) for C4F10, C5F12, C6F14 and C7F16, and inventories of C4F10, C5F12 andC6F14 are reported to the United Nations' Framework Convention on Climate Change (UNFCCC) by Annex 1 countries that have ratified the Kyoto Protocol. The atmospheric measurement based emission estimates are 20 times larger than EDGARv4.2 for C4F10 and over three orders of magnitude for C5F12. The derived emission estimates for C6F14 largely agree with the bottom-up estimates from EDGARv4.2. Moreover, the C7F16 emission estimates are comparable to those of EDGARv4.2 at their peak in the 1990s, albeit significant underestimation for the other time periods. There are no bottom-up emission estimates for C8F18, thus the emission rates reported here are the first for C8F18. The reported inventories for C4F10, C5F12 and C6F14 to UNFCCC are five to ten times lower than those estimated in this study. In addition, we present measured infrared absorption spectra for C7F16 and C8

  1. Discovery and optimization of 5-(2-((1-(phenylsulfonyl)-1,2,3,4-tetrahydroquinolin-7-yl)oxy)pyridin-4-yl)-1,2,4-oxadiazoles as novel gpr119 agonists.

    PubMed

    Wang, Yingcai; Yu, Ming; Zhu, Jiang; Zhang, Jian Ken; Kayser, Frank; Medina, Julio C; Siegler, Karen; Conn, Marion; Shan, Bei; Grillo, Mark P; Liu, Jiwen Jim; Coward, Peter

    2014-02-15

    We describe the discovery and optimization of 5-(2-((1-(phenylsulfonyl)-1,2,3,4-tetrahydroquinolin-7-yl)oxy)pyridin-4-yl)-1,2,4-oxadiazoles as novel agonists of GPR119. Previously described aniline 2 had suboptimal efficacy in signaling assays using cynomolgus monkey (cyno) GPR119 making evaluation of the target in preclinical models difficult. Replacement of the aniline ring with a tetrahydroquinoline ring constrained the rotation of the aniline C-N bond and gave compounds with increased efficacy on human and cyno receptors. Additional optimization led to the discovery of 10, which possesses higher free fraction in plasma and improved pharmacokinetic properties in rat and cyno compared to 2.

  2. 4,5-Dibromo-2,7-di-tert-butyl-9,9-dimethyl-9H-thioxanthene

    PubMed Central

    Rubio, Omayra H.; Fuentes de Arriba, Angel L.; Sanz, Francisca; Muniz, Francisco M.; Morán, Joaquín R.

    2012-01-01

    In the title compound, C23H28Br2S, the thioxanthene unit is twisted, showing a dihedral angle of 29.3 (5)° between the benzene rings. When projected along [001], the packing shows two types of channels. The crystal studied was a racemic twin. PMID:22719586

  3. Digital Group Multiplexers (DGM). Volume 2. Section 3.0, 5.0, 7.0, 15.4

    DTIC Science & Technology

    1980-02-01

    ELECTRONICS COMMAND FORT MONMOUTH, NEW JERSEY PREPARED BY: RAYTHEON COMPANY EQUIPMENT DIVISION COMMUNICATIONS SYSTEM LABORATORY SUDBURY, MASSACHUSETTS...COMPANY EQUIPMENT DIVISION COMMUNICATIONS SYSTEM LABORATORY/9 UDBURY, MASSACHUSETTS 01776 19, ti4"IftE I documt has " pproy for Pub.o -e and ads: itsdI... communications shelters and vans. Its primary function is the time division multiplexing of up to sixteen (16) conditioned diphase loops into a loop group

  4. Discovery of [7-(2,6-dichlorophenyl)-5-methylbenzo [1,2,4]triazin-3-yl]-[4-(2-pyrrolidin-1-ylethoxy)phenyl]amine--a potent, orally active Src kinase inhibitor with anti-tumor activity in preclinical assays.

    PubMed

    Noronha, Glenn; Barrett, Kathy; Boccia, Antonio; Brodhag, Tessa; Cao, Jianguo; Chow, Chun P; Dneprovskaia, Elena; Doukas, John; Fine, Richard; Gong, Xianchang; Gritzen, Colleen; Gu, Hong; Hanna, Ehab; Hood, John D; Hu, Steven; Kang, Xinshan; Key, Jann; Klebansky, Boris; Kousba, Ahmed; Li, Ge; Lohse, Dan; Mak, Chi Ching; McPherson, Andrew; Palanki, Moorthy S S; Pathak, Ved P; Renick, Joel; Shi, Feng; Soll, Richard; Splittgerber, Ute; Stoughton, Silva; Tang, Suhan; Yee, Shiyin; Zeng, Binqi; Zhao, Ningning; Zhu, Hong

    2007-02-01

    We describe the identification of [7-(2,6-dichlorophenyl)-5-methylbenzo [1,2,4]triazin-3-yl]-[4-(2-pyrrolidin-1-ylethoxy)phenyl]amine (3), a potent, orally active Src inhibitor with desirable PK properties, demonstrated activity in human tumor cell lines and in animal models of tumor growth.

  5. 1-[4-[4[(4R,5R)-3,3-Dibutyl-7-(dimethylamino)-2,3,4,5-tetrahydro-4-hydroxy-1,1-dioxido-1-benzothiepin-5-yl]phenoxy]butyl]-4-aza-1-azoniabicyclo[2.2.2]octane methanesulfonate (SC-435), an ileal apical sodium-codependent bile acid transporter inhibitor alters hepatic cholesterol metabolism and lowers plasma low-density lipoprotein-cholesterol concentrations in guinea pigs.

    PubMed

    West, Kristy L; Ramjiganesh, Tripurasundari; Roy, Suheeta; Keller, Bradley T; Fernandez, Maria Luz

    2002-10-01

    Male Hartley guinea pigs (10/group) were assigned either to a control diet (no drug treatment) or to diets containing 0.4, 2.2, or 7.3 mg/day of an ileal apical sodium-codependent bile acid transporter (ASBT) inhibitor, 1-[4-[4[(4R,5R)-3,3-dibutyl-7-(dimethylamino)-2,3,4,5-tetrahydro-4-hydroxy-1,1-dioxido-1-benzothiepin-5-yl]phenoxy]butyl]-4-aza-1-azoniabicyclo[2.2.2] octane methanesulfonate (SC-435). Based on food consumption, guinea pigs received 0, 0.8, 3.7, or 13.4 mg/kg/day of the ASBT inhibitor. The amount of cholesterol in the four diets was maintained at 0.17%, equivalent to 1200 mg/day in the human situation. Guinea pigs treated with 13.4 mg/kg/day SC-435 had 41% lower total cholesterol and 44% lower low-density lipoprotein (LDL)-cholesterol concentrations compared with control (P < 0.01), whereas no significant differences were observed with either of the lower doses of SC-435. Hepatic cholesterol esters were significantly reduced by 43, 56, and 70% in guinea pigs fed 0.8, 3.7, and 13.4 mg/kg/day of the ASBT inhibitor, respectively (P < 0.01). In addition, the highest dose of the inhibitor resulted in a 42% increase in the number of very low-density lipoprotein (VLDL) triacylglycerol molecules and a larger VLDL diameter compared with controls (P < 0.05). Acyl-CoA cholesterol/acyltransferase activity was 30% lower with the highest dose treatment, whereas cholesterol 7alpha-hydroxylase, the regulatory enzyme of bile acid synthesis, was 30% higher with the highest ASBT inhibitor dose (P < 0.05). Furthermore, bile acid excretion increased 2-fold with the highest dose of SC-435 compared with the control group (P < 0.05). These results suggest that the reduction in total and LDL-cholesterol concentrations by the ASBT inhibitor is a result of alterations in hepatic cholesterol metabolism due to modifications in the enterohepatic circulation of bile acids.

  6. A novel technique for measurement of thermal rate constants and temperature dependences of dissociative recombination: CO2+, CF3+, N2O+, C7H8+, C7H7+, C6H6+, C6H5+, C5H6+, C4H4+, and C3H3+

    NASA Astrophysics Data System (ADS)

    Fournier, Joseph A.; Shuman, Nicholas S.; Melko, Joshua J.; Ard, Shaun G.; Viggiano, Albert A.

    2013-04-01

    A novel technique using a flowing afterglow-Langmuir probe apparatus for measurement of temperature dependences of rate constants for dissociative recombination (DR) is presented. Low (˜1011 cm-3) concentrations of a neutral precursor are added to a noble gas/electron afterglow plasma thermalized at 300-500 K. Charge exchange yields one or many cation species, each of which may undergo DR. Relative ion concentrations are monitored at a fixed reaction time while the initial plasma density is varied between 109 and 1010 cm-3. Modeling of the decrease in concentration of each cation relative to the non-recombining noble gas cation yields the rate constant for DR. The technique is applied to several species (O2+, CO2+, CF3+, N2O+) with previously determined 300 K values, showing excellent agreement. The measurements of those species are extended to 500 K, with good agreement to literature values where they exist. Measurements are also made for a range of CnHm+ (C7H7+, C7H8+, C5H6+, C4H4+, C6H5+, C3H3+, and C6H6+) derived from benzene and toluene neutral precursors. CnHm+ DR rate constants vary from 8-12 × 10-7 cm3 s-1 at 300 K with temperature dependences of approximately T-0.7. Where prior measurements exist these results are in agreement, with the exception of C3H3+ where the present results disagree with a previously reported flat temperature dependence.

  7. A novel technique for measurement of thermal rate constants and temperature dependences of dissociative recombination: CO2(+), CF3(+), N2O(+), C7H8(+), C7H7(+), C6H6(+), C6H5(+), C5H6(+), C4H4(+), and C3H3(+).

    PubMed

    Fournier, Joseph A; Shuman, Nicholas S; Melko, Joshua J; Ard, Shaun G; Viggiano, Albert A

    2013-04-21

    A novel technique using a flowing afterglow-Langmuir probe apparatus for measurement of temperature dependences of rate constants for dissociative recombination (DR) is presented. Low (~10(11) cm(-3)) concentrations of a neutral precursor are added to a noble gas∕electron afterglow plasma thermalized at 300-500 K. Charge exchange yields one or many cation species, each of which may undergo DR. Relative ion concentrations are monitored at a fixed reaction time while the initial plasma density is varied between 10(9) and 10(10) cm(-3). Modeling of the decrease in concentration of each cation relative to the non-recombining noble gas cation yields the rate constant for DR. The technique is applied to several species (O2(+), CO2(+), CF3(+), N2O(+)) with previously determined 300 K values, showing excellent agreement. The measurements of those species are extended to 500 K, with good agreement to literature values where they exist. Measurements are also made for a range of CnHm(+) (C7H7(+), C7H8(+), C5H6(+), C4H4(+), C6H5(+), C3H3(+), and C6H6(+)) derived from benzene and toluene neutral precursors. CnHm(+) DR rate constants vary from 8-12 × 10(-7) cm(3) s(-1) at 300 K with temperature dependences of approximately T(-0.7). Where prior measurements exist these results are in agreement, with the exception of C3H3(+) where the present results disagree with a previously reported flat temperature dependence.

  8. 7 CFR 273.5 - Students.

    Code of Federal Regulations, 2011 CFR

    2011-01-01

    ... 7 Agriculture 4 2011-01-01 2011-01-01 false Students. 273.5 Section 273.5 Agriculture Regulations... § 273.5 Students. (a) Applicability. An individual who is enrolled at least half-time in an institution.... (b) Student Exemptions. To be eligible for the program, a student as defined in paragraph (a) of...

  9. 7 CFR 273.5 - Students.

    Code of Federal Regulations, 2013 CFR

    2013-01-01

    ... 7 Agriculture 4 2013-01-01 2013-01-01 false Students. 273.5 Section 273.5 Agriculture Regulations... § 273.5 Students. (a) Applicability. An individual who is enrolled at least half-time in an institution.... (b) Student Exemptions. To be eligible for the program, a student as defined in paragraph (a) of...

  10. 7 CFR 273.5 - Students.

    Code of Federal Regulations, 2012 CFR

    2012-01-01

    ... 7 Agriculture 4 2012-01-01 2012-01-01 false Students. 273.5 Section 273.5 Agriculture Regulations... § 273.5 Students. (a) Applicability. An individual who is enrolled at least half-time in an institution.... (b) Student Exemptions. To be eligible for the program, a student as defined in paragraph (a) of...

  11. 7 CFR 273.5 - Students.

    Code of Federal Regulations, 2014 CFR

    2014-01-01

    ... 7 Agriculture 4 2014-01-01 2014-01-01 false Students. 273.5 Section 273.5 Agriculture Regulations... § 273.5 Students. (a) Applicability. An individual who is enrolled at least half-time in an institution.... (b) Student Exemptions. To be eligible for the program, a student as defined in paragraph (a) of...

  12. 7 CFR 273.5 - Students.

    Code of Federal Regulations, 2010 CFR

    2010-01-01

    ... 7 Agriculture 4 2010-01-01 2010-01-01 false Students. 273.5 Section 273.5 Agriculture Regulations... FOOD STAMP AND FOOD DISTRIBUTION PROGRAM CERTIFICATION OF ELIGIBLE HOUSEHOLDS § 273.5 Students. (a... the individual is enrolled in a regular curriculum at a college or university that offers...

  13. Synthesis and X-ray structural studies of the dextro-rotatory enantiomer of methyl α-5(4,5,6,7-tetrahydro(3,2- c)thieno pyridyl) (2-chlorophenyl)-acetate isopropylsulfate

    NASA Astrophysics Data System (ADS)

    Renou, Ludovic; Coste, Servane; Coquerel, Gerard

    2007-02-01

    This study resolves conflicting data on a particular salt of the enantiomer of methyl α-5(4,5,6,7-tetrahydro(3,2- c)thieno pyridyl) (2-chlorophenyl)-acetate (S(+)clopidogrel). The title compound, (C 16H 17ClNO 2S) + (C 3H 7O 4S) -, was obtained and successfully characterized by X-ray diffraction, NMR, TG/DSC/MS. This salt previously reported in the literature as a 2-propanol solvate of the hydrogensulfate salt appears to be actually an isopropylsulfate salt.

  14. Yb{sub 5}Ni{sub 4}Sn{sub 10} and Yb{sub 7}Ni{sub 4}Sn{sub 13}: New polar intermetallics with 3D framework structures

    SciTech Connect

    Lei Xiaowu; Sun Zhongming; Li Longhua; Zhong Guohua; Hu Chunli; Mao Jianggao

    2010-04-15

    The title compounds have been obtained by solid state reactions of the corresponding pure elements at high temperature, and structurally characterized by single-crystal X-ray diffraction studies. Yb{sub 5}Ni{sub 4}Sn{sub 10} adopts the Sc{sub 5}Co{sub 4}Si{sub 10} structure type and crystallizes in the tetragonal space group P4/mbm (No. 127) with cell parameters of a=13.785(4) A, c=4.492 (2) A, V=853.7(5) A{sup 3}, and Z=2. Yb{sub 7}Ni{sub 4}Sn{sub 13} is isostructural with Yb{sub 7}Co{sub 4}InGe{sub 12} and crystallizes in the tetragonal space group P4/m (No. 83) with cell parameters of a=11.1429(6) A, c=4.5318(4) A, V=562.69(7) A{sup 3}, and Z=1. Both structures feature three-dimensional (3D) frameworks based on three different types of one-dimensional (1D) channels, which are occupied by the Yb atoms. Electronic structure calculations based on density functional theory (DFT) indicate that both compounds are metallic. These results are in agreement with those from temperature-dependent resistivity and magnetic susceptibility measurements. - Graphical abstract: Two new ytterbium nickel stannides, namely, Yb{sub 5}Ni{sub 4}Sn{sub 10} and Yb{sub 7}Ni{sub 4}Sn{sub 13}, have been synthesized and structurally characterized by single-crystal X-ray diffraction studies. Both their structures feature three-dimensional (3D) frameworks based on three different types of one-dimensional (1D) channels, which are situated by all the Yb atoms. Electronic structure calculations based on density functional theory (DFT) indicate that both compounds are metallic, which are in accordance with the results from temperature-dependent resistivity and magnetic susceptibility measurements.

  15. Synthesis of 7-oxo-dihydrospiro[indazole-5,4'-piperidine] acetyl-CoA carboxylase inhibitors.

    PubMed

    Bagley, Scott W; Southers, James A; Cabral, Shawn; Rose, Colin R; Bernhardson, David J; Edmonds, David J; Polivkova, Jana; Yang, Xiaojing; Kung, Daniel W; Griffith, David A; Bader, Scott J

    2012-02-03

    Synthesis of oxo-dihydrospiroindazole-based acetyl-CoA carboxylase (ACC) inhibitors is reported. The dihydrospiroindazoles were assembled in a regioselective manner in six steps from substituted hydrazines and protected 4-formylpiperidine. Enhanced regioselectivity in the condensation between a keto enamine and substituted hydrazines was observed when using toluene as the solvent, leading to selective formation of 1-substituted spiroindazoles. The 2-substituted spiroindazoles were formed selectively from alkyl hydrazones by ring closure with Vilsmeier reagent. The key step in the elaboration to the final products is the conversion of an intermediate olefin to the desired ketone through elimination of HBr from an O-methyl bromohydrin. This methodology enabled the synthesis of each desired regioisomer on 50-75 g scale with minimal purification. Acylation of the resultant spirocyclic amines provided potent ACC inhibitors.

  16. Engineering substrate specificity of succinic semialdehyde reductase (AKR7A5) for efficient conversion of levulinic acid to 4-hydroxyvaleric acid.

    PubMed

    Yeon, Young Joo; Park, Hyung-Yeon; Yoo, Young Je

    2015-09-20

    Engineering enzyme substrate specificity is a promising approach that can expand the applicability of enzymes for the biocatalytic production of industrial chemicals and fuels. In this study, succinic semialdehyde reductase (AKR7A5) was engineered for the conversion of levulinic acid to 4-hydroxyvaleric acid. Levulinic acid is a derivative of cellulosic biomass, and 4-hydroxyvaleric acid is a potential precursor to bio-polymers and fuels. Therefore, the enzymatic conversion of levulinic acid to 4-hydroxyvaleric acid is of special significance in that this conversion could provide a meaningful basis for the bio-production of useful chemicals from cellulosic biomass. In engineering the substrate specificity of the AKR7A5, a rational design approach with the aid of enzyme-substrate interatomic contact analysis was applied. The Met13 residue was selected as a key mutation site, and substitutions of the residue with six hydrophobic amino acids were applied. As a result, four mutants with enhanced catalytic activity toward levulinic acid were obtained, and the most improved mutant, Met13Trp, exhibited a 7.0-fold increase in catalytic efficiency. Additionally, the structural effects of the positive mutations were investigated to analyze the structural basis for the enzyme substrate specificity with the target substrate.

  17. Design, synthesis, and preclinical evaluation of new 5,6- (or 6,7-) disubstituted-2-(fluorophenyl)quinolin-4-one derivatives as potent antitumor agents.

    PubMed

    Chou, Li-Chen; Tsai, Meng-Tung; Hsu, Mei-Hua; Wang, Sheng-Hung; Way, Tzong-Der; Huang, Chi-Hung; Lin, Hui-Yi; Qian, Keduo; Dong, Yizhou; Lee, Kuo-Hsiung; Huang, Li-Jiau; Kuo, Sheng-Chu

    2010-11-25

    Our previous exploration of 2-phenylquinolin-4-ones (2-PQs) has led to an anticancer drug candidate 2-(2-fluorophenyl)-6,7-methylenedioxyquinolin-4-one monosodium phosphate (CHM-1-P-Na). In order to develop additional new drug candidates, novel 2-PQs were designed, synthesized, and evaluated for cytotoxic activity. Most analogues, including 1b, 2a,b, 3a,b, 4a,b, and 5a,b, exhibited significant inhibitory activity (IC(50) of 0.03-8.2 μM) against all tested tumor cell lines. As one of the most potent analogue, 2-(3-fluorophenyl)-5-hydroxy-6-methoxyquinolin-4-one (3b) selectively inhibited 14 out of 60 cancer cell lines in a National Cancer Institute (NCI) evaluation. Preliminary mechanism of action study suggested that 3b had a significant effect on the tyrosine autophosphorylation of insulin-like growth factor-1 receptor (IGF-1R). Safety pharmacology profiling of 3b showed no significant effect on normal biological functions of most enzymes tested. Furthermore, sodium 2-(3-fluorophenyl)-6-methoxy-4-oxo-1,4-dihydroquinolin-5-yl phosphate (15), the monophosphate of 3b, exceeded the activity of doxorubicin and was comparable to CHM-1-P-Na in a Hep3B xenograft nude mice model. In summary, 15 is a promising clinical candidate and is currently under preclinical study.

  18. H2 genotypes of G4P[6], G5P[7], and G9[23] porcine rotaviruses show super-short RNA electropherotypes.

    PubMed

    Nagai, Makoto; Shimada, Saya; Fujii, Yoshiki; Moriyama, Hiromitsu; Oba, Mami; Katayama, Yukie; Tsuchiaka, Shinobu; Okazaki, Sachiko; Omatsu, Tsutomu; Furuya, Tetsuya; Koyama, Satoshi; Shirai, Junsuke; Katayama, Kazuhiko; Mizutani, Tetsuya

    2015-04-17

    During group A rotavirus (RVA) surveillance of pig farms in Japan, we detected three RVA strains (G4P[6], G5P[7], and G9P[23] genotypes), which showed super-short RNA patterns by polyacrylamide gel electrophoresis, in samples from a healthy eight-day-old pig and two pigs of seven and eight days old with diarrhea from three farms. Reverse transcription PCR and sequencing revealed that the full-length NSP5 gene of these strains contained 952 or 945 nucleotides, which is consistent with their super-short electropherotypes. Due to a lack of whole genome data on Japanese porcine RVAs, we performed whole genomic analyses of the three strains. The genomic segments of these RVA strains showed typical porcine RVA constellations, except for H2 NSP5 genotype, (G4,5,9-P[6,7,23]-I5-R1-C1-M1-A8-N1-T1-E1-H2 representing VP7-VP4-VP6-VP1-VP2-VP3-NSP1-NSP2-NSP3-NSP4-NSP5 genes). In phylogenetic analyses, these porcine RVA strains clustered with porcine and porcine-like human RVA strains and showed a typical porcine RVA backbone, except for the NSP5 gene; however, intra-genotype reassortment events among porcine and porcine-like human RVA strains were observed. The NSP5 gene segments of these strains were clustered within the H2b genotype with super-short human RVA strains. The H2 genotype has to date only been identified in human and lapine RVA strains. Thus, to our knowledge, this report presents the first case of H2 NSP5 genotype showing a super-short RNA pattern in porcine RVA. These data suggest the possibility of interspecies transmission between pigs and humans and imply that super-short porcine RVA strains possessing H2 genotype are circulating among both asymptomatic and diarrheic porcine populations in Japan.

  19. Environmentally relevant concentrations of arsenite and monomethylarsonous acid inhibit IL-7/STAT5 cytokine signaling pathways in mouse CD3+CD4-CD8- double negative thymus cells.

    PubMed

    Xu, Huan; Lauer, Fredine T; Liu, Ke Jian; Hudson, Laurie G; Burchiel, Scott W

    2016-04-15

    Environmental arsenic exposure is a public health issue. Immunotoxicity induced by arsenic has been reported in humans and animal models. The purpose of this study was to evaluate mechanisms of As(+3) and MMA(+3) toxicity in mouse thymus cells. Because we know that MMA(+3) inhibits IL-7 signaling in mouse bone marrow pre-B cells, we studied the influence of As(+3) and MMA(+3) on T cell development in the thymus at the earliest stage of T cell development (CD4-CD8-, double negative, DN) which requires IL-7 dependent signaling. We found in a DN thymus cell line (D1) that a low concentration of MMA(+3) (50 nM) suppressed IL-7 dependent JAK1, 3 and STAT5 signaling. As(+3) suppressed STAT5 and JAK3 at higher concentrations (500 nM). Cell surface expression of the IL-7 receptor (CD127) was also suppressed by 50 nM MMA(+)3, but was increased by 500 NM As(+3), indicating possible differences in the mechanisms of action of these agents. A decrease in cyclin D1 protein expression was observed in D1 cells exposed to As(+3) at 500 nM and MMA(+3) starting at 50 nM, suggesting that arsenic at these environmentally-relevant doses suppresses early T cell development through the inhibition of IL-7 signaling pathway.

  20. (4bS,8aS)-1-Isopropyl-4b,8,8-trimethyl-4b,5,6,7,8,8a,9,10-octa­hydro­phenan­thren-2-yl acetate

    PubMed Central

    Oubabi, Radouane; Auhmani, Aziz; Ait Itto, My Youssef; Auhmani, Abdelwahed; Daran, Jean-Claude

    2014-01-01

    The hemisynthesis of the title compound, C22H32O2, was carried out through direct acetyl­ation reaction of the naturally occurring diterpene totarol [systematic name: (4bS,8aS)-4b,8,8-trimethyl-1-propan-2-yl-5,6,7,8a,9,10-hexa­hydro­phen­an­thren-2-ol]. The mol­ecule is built up from three fused six membered rings, one saturated and two unsaturated. The central unsaturated ring has a half-chair conformation, whereas the other unsaturated ring displays a chair conformation. The absolute configuration is deduced from the chemical pathway. The value of the Hooft parameter [−0.10 (6)] allowed this absolute configuration to be confirmed. PMID:24765017

  1. Antileishmanial Effect of 5,3′-Hydroxy-7,4′-dimethoxyflavanone of Picramnia gracilis Tul. (Picramniaceae) Fruit: In Vitro and In Vivo Studies

    PubMed Central

    Robledo, Sara M.; Cardona, Wilson; Ligardo, Karen; Henao, Jéssica; Arbeláez, Natalia; Montoya, Andrés; Alzate, Fernando; Pérez, Juan M.; Arango, Victor; Vélez, Iván D.; Sáez, Jairo

    2015-01-01

    Species of Picramnia genus are used in folk medicine to treat or prevent skin disorders, but only few species have been studied for biological activity and chemical composition. P. gracilis Tul. is a native species from Central and South America and although its fruits are edible, phytochemical analysis or medicinal uses of this species are not known. In the search of candidates to antileishmanial drugs, this work aimed to evaluate the antileishmanial activity of P. gracilis Tul. in in vitro and in vivo studies. Only ethanolic extract of fruits showed leishmanicidal activity. The majoritarian metabolite was 5,3′-hydroxy-7,4′-dimethoxyflavanone ether that exhibited high activity against L. (V.) panamensis (EC50 17.0 + 2.8 mg/mL, 53.7 μM) and low toxicity on mammalian U-937 cells, with an index of selectivity >11.8. In vivo studies showed that the flavanone administered in solution (2 mg/kg/day) or cream (2%) induces clinical improvement and no toxicity in hamsters with CL. In conclusion, this is the first report about isolation of 5,3′-hydroxy-7,4′-dimethoxyflavanone of P. gracilis Tul. The leishmanicidal activity attributed to this flavanone is also reported for the first time. Finally, the in vitro and in vivo leishmanicidal activity reported here for 5,3′-hydroxy-7,4′-dimethoxyflavanone offers a greater prospect towards antileishmanial drug discovery and development. PMID:26064104

  2. Metabolite generation via microbial biotransformations with Actinomycetes: rapid screening for active strains and biosynthesis of important human metabolites of two development-stage compounds, 5-[(5S,9R)-9-(4-cyanophenyl)-3-(3,5-dichlorophenyl)-1-methyl-2,4-dioxo-1,3,7-triazaspiro[4.4]non7-yl-methyl]-3-thiophenecarboxylic acid (BMS-587101) and dasatinib.

    PubMed

    Li, Wenying; Josephs, Jonathan L; Skiles, Gary L; Humphreys, W Griffith

    2008-04-01

    The enzymes present in many microbial strains are capable of carrying out a variety of biotransformations when presented with drug-like molecules. Although the enzymes responsible for the biotransformations are not well characterized, microbial strains can often be found that produce metabolites identical to those found in mammalian systems. However, traditional screening for microbial strains that produce metabolites of interest is done with many labor intensive steps that include multiple shake flasks and many manual manipulations, which hinder the application of these techniques in drug metabolite preparation. A 24-well microtiter plate screening system was developed for rapid screening of actinomycetes strains for their ability to selectively produce metabolites of interest. The utility of this system was first demonstrated with the well characterized cytochrome P450 substrate diclofenac. Subsequently, the use of this system allowed the rapid identification of several actinomycetes strains that were capable of converting two drug candidates under development, 5-[(5S,9R)-9-(4-cyanophenyl)-3-(3,5-dichlorophenyl)-1-methyl-2,4-dioxo-1,3,7-triazaspiro[4.4]non7-yl-methyl]-3-thiophenecarboxylic acid and N-(2-chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-1-piperazinyl)]-2-methyl-4-pyrimidinyl]amino)]-1,3-thiazole-5-carboxamide (dasatinib, Sprycel, BMS-345825), to mammalian metabolites of interest. Milligram quantities of the metabolites were then prepared by scaling-up the microbial biotransformation reactions. These quantities were sufficient for initial characterization, such as testing for pharmacological activity and use as analytical standards, prior to the availability of authentic chemically synthesized compounds.

  3. Three closely related 4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridines: synthesis, molecular conformations and hydrogen bonding in zero, one and two dimensions.

    PubMed

    Sagar, Belakavadi K; Harsha, Kachigere B; Yathirajan, Hemmige S; Rangappa, Kanchugarakoppal S; Rathore, Ravindranath S; Glidewell, Christopher

    2017-03-01

    In each of 1-(4-fluorophenyl)-5-methylsulfonyl-3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine, C21H19F4N3O2S, (I), 1-(4-chlorophenyl)-5-methylsulfonyl-3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine, C21H19ClF3N3O2S, (II), and 1-(3-methylphenyl)-5-methylsulfonyl-3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine, C22H22F3N3O2S, (III), the reduced pyridine ring adopts a half-chair conformation with the methylsulfonyl substituent occupying an equatorial site. Although compounds (I) and (II) are not isostructural, having the space groups Pbca and P212121, respectively, their molecular conformations are very similar, but the conformation of compound (III) differs from those of (I) and (II) in the relative orientation of the N-benzyl and methylsulfonyl substituents. In compounds (II) and (III), but not in (I), the trifluoromethyl groups are disordered over two sets of atomic sites. Molecules of (I) are linked into centrosymmetric dimers by C-H...π(arene) hydrogen bonds, molecules of (II) are linked by two C-H...O hydrogen bonds to form ribbons of R3(3)(18) rings, which are themselves further linked by a C-Cl...π(arene) interaction, and a combination of C-H...O and C-H...π(arene) hydrogen bonds links the molecules of (III) into sheets. Comparisons are made with the structures of some related compounds.

  4. Discovery of methyl 4'-methyl-5-(7-nitrobenzo[c][1,2,5]oxadiazol-4-yl)-[1,1'-biphenyl]-3-carboxylate, an improved small-molecule inhibitor of c-Myc-max dimerization.

    PubMed

    Chauhan, Jay; Wang, Huabo; Yap, Jeremy L; Sabato, Philip E; Hu, Angela; Prochownik, Edward V; Fletcher, Steven

    2014-10-01

    c-Myc is a basic helix-loop-helix-leucine zipper (bHLH-ZIP) transcription factor that is responsible for the transcription of a wide range of target genes involved in many cancer-related cellular processes. Over-expression of c-Myc has been observed in, and directly contributes to, a variety of human cancers including those of the hematopoietic system, lung, prostate and colon. To become transcriptionally active, c-Myc must first dimerize with Myc-associated factor X (Max) via its own bHLH-ZIP domain. A proven strategy towards the inhibition of c-Myc oncogenic activity is to interfere with the structural integrity of the c-Myc-Max heterodimer. The small molecule 10074-G5 is an inhibitor of c-Myc-Max dimerization (IC50 =146 μM) that operates by binding and stabilizing c-Myc in its monomeric form. We have identified a congener of 10074-G5, termed 3jc48-3 (methyl 4'-methyl-5-(7-nitrobenzo[c][1,2,5]oxadiazol-4-yl)-[1,1'-biphenyl]-3-carboxylate), that is about five times as potent (IC50 =34 μM) at inhibiting c-Myc-Max dimerization as the parent compound. 3jc48-3 exhibited an approximate twofold selectivity for c-Myc-Max heterodimers over Max-Max homodimers, suggesting that its mode of action is through binding c-Myc. 3jc48-3 inhibited the proliferation of c-Myc-over-expressing HL60 and Daudi cells with single-digit micromolar IC50 values by causing growth arrest at the G0 /G1 phase. Co-immunoprecipitation studies indicated that 3jc48-3 inhibits c-Myc-Max dimerization in cells, which was further substantiated by the specific silencing of a c-Myc-driven luciferase reporter gene. Finally, 3jc48-3's intracellular half-life was >17 h. Collectively, these data demonstrate 3jc48-3 to be one of the most potent, cellularly active and stable c-Myc inhibitors reported to date.

  5. On the occurrence of dynamic strain aging in near-alpha alloy Ti-5.8Al-4Sn-3.5Zr-0.7Nb-0.5Mo-0.35Si

    SciTech Connect

    Singh, N.; Prasad, N.; Singh, V.

    1999-09-01

    Alloy Ti-5.8Al-4Sn-3.5Zr-0.7Nb-0.5Mo-0.35Si (IMI 834) is the most recently developed near-alpha type titanium alloy for high-temperature application up to 873 K, as discs and blades in the high pressure part of compressors, in advanced jet engines. It possesses a good combination of creep and fatigue resistance at elevated temperature, in properly heat-treated condition, and has a fine bimodal microstructure, consisting of a small volume fraction of equiaxed alpha in a fine-grained matrix of transformed beta. Some investigations have already been done on the tensile behavior of this alloy, in different heat-treated conditions, over a wide range of temperature from 293 to 923 K. However, no report has been made on the occurrence of dynamic strain aging (DSA) in this alloy. The purpose of this article is to present the observation on the occurrence of DSA in the titanium alloy IMI 834, in the as-received (hot-rolled and mill-annealed) condition, over the temperature range 623 to 823 K.

  6. Synthesis, crystal structure, NMR study and AC conductivity of [(C3H7)4N]2Cd2ClF5 compound

    NASA Astrophysics Data System (ADS)

    Hajji, Rachid; Oueslati, Abderrazak; Body, Monique; Hlel, Faouzi

    2015-08-01

    The [(C3H7)4N]2Cd2ClF5 compound was crystallized in the triclinic system with space group P1. The crystal structure consists of organic-inorganic layers, stacked along direction. The organic part consists of two cations types. The inorganic layer is made up of Cd2ClF5 dimmers composed of two in-equivalent irregular tetrahedra sharing one edge (Cl-F). The MAS NMR spectra showed two, three and five isotropic resonances relative to 111Cd, 13C and 19F nuclei, respectively. DSC measurement disclosed a phase transition at around 380 K. The impedance spectroscopy and AC electrical conductivity measurements of our compound were taken from 209 Hz to 5 MHz over the temperature range of 350-381 K. Nyquist plots ( Z″ vs Z') show semicircle arcs at different temperatures, and an electrical equivalent circuit has been proposed to explain the impedance results. The circuits consist of the parallel combination of bulk resistance ( R), capacitance ( C) and fractal capacitance (CPE). The conductivity σ p follows the Arrhenius relation. The near value of activation energies obtained from the conductivity data and circuit equivalent confirms that the transport is through hopping mechanism. The analysis of the experimental data shows that the reorientation motion of [N(C3H7)4]+ cations and/or [Cd2ClF5]2- anions is probably responsible for the observed conductivity.

  7. CryoEM structure of the yeast U4/U6.U5 tri-snRNP at 3.7 Å resolution

    PubMed Central

    Bai, Xiao-chen; Oubridge, Chris; Newman, Andrew J.; Scheres, Sjors H. W.; Nagai, Kiyoshi

    2016-01-01

    U4/U6.U5 tri-snRNP represents a substantial part of the spliceosome before activation. A cryoEM structure of Saccharomyces cerevisiae U4/U6.U5 tri-snRNP at 3.7Å resolution led to an essentially complete atomic model comprising 30 proteins plus U4/U6 and U5 snRNAs. The structure reveals striking interweaving interactions of the protein and RNA components including extended polypeptides penetrating into subunit interfaces. The invariant ACAGAGA sequence of U6 snRNA, which base-pairs with the 5′-splice site during catalytic activation, forms a hairpin stabilised by Dib1 and Prp8 while the adjacent nucleotides interact with the exon binding loop 1 of U5 snRNA. Snu114 harbours GTP but its putative catalytic histidine is held away from the γ-phosphate by hydrogen bonding to a tyrosine in Prp8’s N-terminal domain. Mutation of this histidine to alanine has no detectable effect on yeast growth. The structure provides important new insights into the spliceosome activation process leading to the formation of the catalytic centre. PMID:26829225

  8. Crystal structure of britvinite [Pb7(OH)3F(BO3)2(CO3)][Mg4.5(OH)3(Si5O14)]: A new layered silicate with an original type of silicon-oxygen networks

    NASA Astrophysics Data System (ADS)

    Yakubovich, O. V.; Massa, W.; Chukanov, N. V.

    2008-03-01

    The crystal structure of a new mineral britvinite Pb7.1Mg4.5(Si4.8Al0.2O14)(BO3)(CO3)[(BO3)0.7(SiO4)0.3](OH, F)6.7 from the Lángban iron-manganese skarn deposit (Värmland, Sweden) is determined at T = 173 K using X-ray diffraction (Stoe IPDS diffractometer, λMo Kα, graphite monochromator, 2θmax = 58.43°, R = 0.052 for 6262 reflections). The main crystal data are as follows: a = 9.3409(8) Å, b = 9.3579(7) Å, c = 18.8333(14) Å, α = 80.365(6)°, β = 75.816(6)°, γ = 59.870(5)°, V = 1378.7(2) Å3, space group P1, Z = 2, and ρcalcd = 5.42 g/cm3. The idealized structural formula of the mineral is represented as [Pb7(OH)3F(BO3)2(CO3)][Mg4.5(OH)3(Si5O14)]. It is demonstrated that the mineral britvinite is a new representative of the group of mica-like layered silicates with structures in which three-layer (2: 1) "sandwiches" composed of tetrahedra and octahedra alternate with blocks of other compositions, such as oxide, oxide-carbonate, oxide-carbonate-sulfate, and other blocks. The tetrahedral networks (Si5O14)∞∞ consisting of twelve-membered rings are fragments of the britvinite structure. Similar networks also form crystal structures of the mineral zeophyllite and the synthetic phase Rb6Si10O23. In the crystal structures under consideration, the tetrahedral networks differ in the rotation of tetrahedra with respect to the layer plane.

  9. A sequential injection method for the fluorimetric determination of aluminum in drinking water using 8-hydroxy-7-(4-sulfo-1-naphthylazo)-5-quinoline sulfonic acid.

    PubMed

    Al-Kindy, Salma M Z; Al-Ghamari, Salwa S; Suliman, Fakhr Eldin O

    2007-12-31

    A robust and simple sequential injection (SI) method for the assay of aluminum ions in drinking water is described. The method is based on the complex formation between aluminum and 8-hydroxy-7-(4-sulfo-1-naphthylazo)-5-quinoline sulfonic acid (HSNQ). The fluorescence of the complex is monitored at an emission wavelength of 492 nm with excitation at 357 nm. The HSNQ concentration, aspirated reagent and sample volumes were optimized simultaneously using 3(3) full factorial design. The optimum operating conditions are aspirated sample and reagent volumes of 90 and 70 microL, respectively, and HSNQ concentration of 20 microM. With these conditions linear calibration curves were obtained from 100 to 800 ppb. The detection limit was 4 ppb. The maximum relative standard deviation of the method was 1.43% (n=5). The method was successfully applied for the determination of aluminum in drinking water samples.

  10. PIP2-dependent coupling is prominent in Kv7.1 due to weakened interactions between S4-S5 and S6

    NASA Astrophysics Data System (ADS)

    Kasimova, Marina A.; Zaydman, Mark A.; Cui, Jianmin; Tarek, Mounir

    2015-01-01

    Among critical aspects of voltage-gated potassium (Kv) channels' functioning is the effective communication between their two composing domains, the voltage sensor (VSD) and the pore. This communication, called coupling, might be transmitted directly through interactions between these domains and, as recently proposed, indirectly through interactions with phosphatidylinositol-4,5-bisphosphate (PIP2), a minor lipid of the inner plasma membrane leaflet. Here, we show how the two components of coupling, mediated by protein-protein or protein-lipid interactions, both contribute in the Kv7.1 functioning. On the one hand, using molecular dynamics simulations, we identified a Kv7.1 PIP2 binding site that involves residues playing a key role in PIP2-dependent coupling. On the other hand, combined theoretical and experimental approaches have shown that the direct interaction between the segments of the VSD (S4-S5) and the pore (S6) is weakened by electrostatic repulsion. Finally, we conclude that due to weakened protein-protein interactions, the PIP2-dependent coupling is especially prominent in Kv7.1.

  11. Interaction of helix D of elongation factor Tu with helices 4 and 5 of protein L7/12 on the ribosome.

    PubMed

    Kothe, Ute; Wieden, Hans-Joachim; Mohr, Dagmar; Rodnina, Marina V

    2004-03-05

    Elongation factor Tu (EF-Tu) promotes binding of aminoacyl-tRNA to the A site of the ribosome. Here, we report the effects of mutations in helix D of EF-Tu and in the C-terminal domain of L7/12 on the kinetics of A-site binding. Reaction rates were measured by stopped-flow and quench-flow techniques. The rates of A-site binding were decreased by mutations at positions 144, 145, 148, and 152 in helix D of EF-Tu as well as at positions 65, 66, 69, 70, 73, and 84 in helices 4 and 5 of L7/12. The effect was due primarily to the lower association rate constant of ternary complex binding to the ribosome. These results suggest that helix D of EF-Tu is involved in an initial transient contact with helices 4 and 5 of L7/12 that promotes ternary complex binding to the ribosome. By analogy to the interaction of helix D of EF-Tu with the N-terminal domain of EF-Ts, the contact area is likely to consist of a hydrophobic patch flanked by two salt-bridges.

  12. Non-additive hepatic gene expression elicited by 2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD) and 2,2',4,4',5,5'-hexachlorobiphenyl (PCB153) co-treatment in C57BL/6 mice

    SciTech Connect

    Kopec, Anna K.; D'Souza, Michelle L.; Mets, Bryan D.; Burgoon, Lyle D.; Reese, Sarah E.; Archer, Kellie J.; Potter, Dave; Tashiro, Colleen; Sharratt, Bonnie; Harkema, Jack R.; Zacharewski, Timothy R.

    2011-10-15

    Interactions between environmental contaminants can lead to non-additive effects that may affect the toxicity and risk assessment of a mixture. Comprehensive time course and dose-response studies with 2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD), non-dioxin-like 2,2',4,4',5,5'-hexachlorobiphenyl (PCB153) and their mixture were performed in immature, ovariectomized C57BL/6 mice. Mice were gavaged once with 30 {mu}g/kg TCDD, 300 mg/kg PCB153, a mixture of 30 {mu}g/kg TCDD with 300 mg/kg PCB153 (MIX) or sesame oil vehicle for 4,12, 24,72 or 168 h. In the 24 h dose-response study, animals were gavaged with TCDD (0.3,1, 3, 6, 10, 15, 30, 45 {mu}g/kg), PCB153 (3,10, 30, 60, 100, 150, 300, 450 mg/kg), MIX (0.3 + 3, 1 + 10, 3 + 30, 6 + 60, 10 + 100, 15 + 150, 30 + 300, 45 {mu}g/kg TCDD + 450 mg/kg PCB153, respectively) or vehicle. All three treatments significantly increased relative liver weights (RLW), with MIX eliciting significantly greater increases compared to TCDD and PCB153 alone. Histologically, MIX induced hepatocellular hypertrophy, vacuolization, inflammation, hyperplasia and necrosis, a combination of TCDD and PCB153 responses. Complementary lipid analyses identified significant increases in hepatic triglycerides in MIX and TCDD samples, while PCB153 had no effect on lipids. Hepatic PCB153 levels were also significantly increased with TCDD co-treatment. Microarray analysis identified 167 TCDD, 185 PCB153 and 388 MIX unique differentially expressed genes. Statistical modeling of quantitative real-time PCR analysis of Pla2g12a, Serpinb6a, Nqo1, Srxn1, and Dysf verified non-additive expression following MIX treatment compared to TCDD and PCB153 alone. In summary, TCDD and PCB153 co-treatment elicited specific non-additive gene expression effects that are consistent with RLW increases, histopathology, and hepatic lipid accumulation. - Graphical abstract: Display Omitted Highlights: > MIX (TCDD:PCB153 at 1:10,000 ratio) exposure leads to non-additive gene expression

  13. 3.6 and 4.5 μm Spitzer Phase Curves of the Highly Irradiated Hot Jupiters WASP-19b and HAT-P-7b

    NASA Astrophysics Data System (ADS)

    Wong, Ian; Knutson, Heather A.; Kataria, Tiffany; Lewis, Nikole K.; Burrows, Adam; Fortney, Jonathan J.; Schwartz, Joel; Shporer, Avi; Agol, Eric; Cowan, Nicolas B.; Deming, Drake; Désert, Jean-Michel; Fulton, Benjamin J.; Howard, Andrew W.; Langton, Jonathan; Laughlin, Gregory; Showman, Adam P.; Todorov, Kamen

    2016-06-01

    We analyze full-orbit phase curve observations of the transiting hot Jupiters WASP-19b and HAT-P-7b at 3.6 and 4.5 μm, obtained using the Spitzer Space Telescope. For WASP-19b, we measure secondary eclipse depths of 0.485%+/- 0.024% and 0.584%+/- 0.029% at 3.6 and 4.5 μm, which are consistent with a single blackbody with effective temperature 2372 ± 60 K. The measured 3.6 and 4.5 μm secondary eclipse depths for HAT-P-7b are 0.156%+/- 0.009% and 0.190%+/- 0.006%, which are well described by a single blackbody with effective temperature 2667 ± 57 K. Comparing the phase curves to the predictions of one-dimensional and three-dimensional atmospheric models, we find that WASP-19b’s dayside emission is consistent with a model atmosphere with no dayside thermal inversion and moderately efficient day-night circulation. We also detect an eastward-shifted hotspot, which suggests the presence of a superrotating equatorial jet. In contrast, HAT-P-7b’s dayside emission suggests a dayside thermal inversion and relatively inefficient day-night circulation; no hotspot shift is detected. For both planets, these same models do not agree with the measured nightside emission. The discrepancies in the model-data comparisons for WASP-19b might be explained by high-altitude silicate clouds on the nightside and/or high atmospheric metallicity, while the very low 3.6 μm nightside planetary brightness for HAT-P-7b may be indicative of an enhanced global C/O ratio. We compute Bond albedos of 0.38 ± 0.06 and 0 (\\lt 0.08 at 1σ ) for WASP-19b and HAT-P-7b, respectively. In the context of other planets with thermal phase curve measurements, we show that WASP-19b and HAT-P-7b fit the general trend of decreasing day-night heat recirculation with increasing irradiation.

  14. Phosphorylation regulates the sensitivity of voltage‐gated Kv7.2 channels towards phosphatidylinositol‐4,5‐bisphosphate

    PubMed Central

    Salzer, Isabella; Erdem, Fatma Asli; Chen, Wei‐Qiang; Heo, Seok; Koenig, Xaver; Schicker, Klaus W.; Kubista, Helmut; Lubec, Gert; Boehm, Stefan

    2016-01-01

    Key points Phosphatidylinositol‐4,5‐bisphosphate (PIP2) is a key regulator of many membrane proteins, including voltage‐gated Kv7.2 channels.In this study, we identified the residues in five phosphorylation sites and their corresponding protein kinases, the former being clustered within one of four putative PIP2‐binding domains in Kv7.2.Dephosphorylation of these residues reduced the sensitivity of Kv7.2 channels towards PIP2.Dephosphorylation of Kv7.2 affected channel inhibition via M1 muscarinic receptors, but not via bradykinin receptors.Our data indicated that phosphorylation of the Kv7.2 channel was necessary to maintain its low affinity for PIP2, thereby ensuring the tight regulation of the channel via G protein‐coupled receptors. Abstract The function of numerous ion channels is tightly controlled by G protein‐coupled receptors (GPCRs). The underlying signalling mechanisms may involve phosphorylation of channel proteins and participation of phosphatidylinositol‐4,5‐bisphosphate (PIP2). Although the roles of both mechanisms have been investigated extensively, thus far only little has been reported on their interaction in channel modulation. GPCRs govern Kv7 channels, the latter playing a major role in the regulation of neuronal excitability by determining the levels of PIP2 and through phosphorylation. Using liquid chromatography‐coupled mass spectrometry for Kv7.2 immunoprecipitates of rat brain membranes and transfected cells, we mapped a cluster of five phosphorylation sites in one of the PIP2‐binding domains. To evaluate the effect of phosphorylation on PIP2‐mediated Kv7.2 channel regulation, a quintuple alanine mutant of these serines (S427/S436/S438/S446/S455; A5 mutant) was generated to mimic the dephosphorylated state. Currents passing through these mutated channels were less sensitive towards PIP2 depletion via the voltage‐sensitive phosphatase Dr‐VSP than were wild‐type channels. In vitro phosphorylation assays with the

  15. Novel ligands for the opioid receptors: synthesis and structure-activity relationships among 5'-aryl and 5'-heteroaryl 17-cyclopropylmethyl-4,5 alpha-epoxypyrido[2',3':6,7]morphinans.

    PubMed

    Ananthan, Subramaniam; Khare, Naveen K; Saini, Surendra K; Davis, Peg; Dersch, Christina M; Porreca, Frank; Rothman, Richard B

    2003-09-01

    A series of pyridomorphinans possessing an aryl (10a-s) or heteroaryl (11a-h) substituent at the 5'-position of the pyridine ring of 17-cyclopropylmethyl-4,5 alpha-epoxypyrido[2',3':6,7]morphinan was synthesized and evaluated for binding and functional activity at the opioid delta, mu, and kappa receptors. All of these pyridomorphinans bound with higher affinity at the delta site than at mu or kappa sites. The binding data on isomeric compounds revealed that there exists greater bulk tolerance for substituents placed at the o-position of the phenyl ring than at m- or p-positions. Among the ligands examined, the 2-chlorophenyl (10l), 2-nitrophenyl (10n), 2-pyridyl (11a), and 4-quinolinyl (11g) compounds bound to the delta receptor with subnanomolar affinity. Compound 10c with the p-tolyl substituent displayed the highest mu/delta selectivity (ratio=42) whereas compound 10l with the 2-chlorophenyl substituent displayed the highest kappa/delta selectivity (ratio=23). At 10 microM concentration, the in vitro functional activity determined using [(35)S]GTP-gamma-S binding assays showed that all of the compounds were antagonists devoid of any significant agonist activity at the delta, mu, and kappa receptors. Antagonist potency determinations of three selected ligands revealed that the p-tolyl compound 10c is a potent delta selective antagonist. In the [(35)S]GTP-gamma-S assays this compound had a functional antagonist K(i) value of 0.2, 4.52, and 7.62 nM at the delta, mu, and kappa receptors, respectively. In the smooth muscle assays 10c displayed delta antagonist potency with a K(e) value of 0.88 nM. As an antagonist, it was 70-fold more potent at the delta receptors in the MVD than at the mu receptors in the GPI. The in vitro delta antagonist profile of this pyridomorphinan 10c resembles that of the widely used delta selective antagonist ligand naltrindole.

  16. 2,4-Diamino-6,7-dihydro-5H-cyclopenta[d]pyrimidine analogues of trimethoprim as inhibitors of Pneumocystis carinii and Toxoplasma gondii dihydrofolate reductase.

    PubMed

    Rosowsky, A; Papoulis, A T; Queener, S F

    1998-03-12

    Three previously unreported (R,S)-2,4-diamino-5-[(3,4,5-trimethoxyphenyl) alkyl]-6,7-dihydro-5H-cyclopenta[d]pyrimidines 15a-c were synthesized as analogues of trimethoprim (TMP) and were tested as inhibitors of Pneumocystis carinii, Toxoplasma gondii, and rat liver dihydrofolate reductase (DHFR). The length of the alkyl bridge between the cyclopenta[d]pyrimidine and trimethoxyphenyl moiety ranged from one in 15a to three carbons in 15c. The products were tested as competitive inhibitors of the reduction of dihydrofolate by Pneumocystis carinii, Toxoplasma gondii, and rat liver DHFR. Compounds 15a-c had IC50 values of > 32, 1.8 and 1.3 microM, respectively, against P. carinii DHFR, as compared to 12 microM for TMP. Against the T. gondii enzyme, 15a-c had IC50 values of 21, 0.14 and 0.14 microM, respectively, as compared to 2.7 microM for TMP. Inhibitors 15b and 15c with two- and three-carbon bridges were significantly more potent than 15a against all three enzymes. Unlike TMP, 15b and 15c were better inhibitors of the rat liver enzyme than of the microbial enzymes. The potency of 15b and 15c against rat liver DHFR was less than has been reported for the corresponding 6,7-dihydro-5H-cyclopenta[d]pyrimidines with a classical p-aminobenzoyl-L-glutamate side chain as inhibitors of bovine, murine, and human DHFR.

  17. Facile synthesis of 4,5,6a,7-tetrahydrodibenzo[de,g]chromene heterocycles and their transformation to phenanthrene alkaloids

    PubMed Central

    Kapadia, Nirav; Harding, Wayne

    2013-01-01

    Oxa-Pictet-Spengler cyclization and microwave-assisted C-H arylation have been implemented as key steps in the synthesis of new isochroman heterocycles containing a 4,5,6a,7-tetrahydrodibenzo[de,g]chromene motif. These isochromans may be easily transformed to phenanthrene alkaloids via acidic cleavage of the isochroman ring and standard synthetic manipulations thereafter. The route described is attractive in that it provides access to two biologically interesting scaffolds in simple and high yielding synthetic steps. PMID:24187388

  18. Generation and intermolecular trapping of 1,2-diaza-4-silacyclopentane-3,5-diyls in the denitrogenation of 2,3,5,6-tetraaza-7-silabicyclo[2.2.1]hept-2-ene: an experimental and computational study.

    PubMed

    Nakamura, Takeshi; Takegami, Akinobu; Abe, Manabu

    2010-03-19

    In our previous computational study, we found that silicon and nitrogen atoms have a notable effect on the reactivity of 1,2-diaza-4-silacyclopentane-3,5-diyls. Thus, the singlet state of the diradical was calculated to be much more stable than the corresponding ring-closing product, i.e., 2,3-diaza-5-silabicyclo[2.1.0]pentane, and the triplet state of the diradical. In the present study, derivatives of the diradical were generated experimentally in the denitrogenation of precursor azoalkanes, i.e., 2,3,5,6-tetraaza-7-silabicyclo[2.2.1]hept-2-enes, which can be prepared by cycloaddition of a diazasilole with 4-phenyl-1,2,4-triazole-3,5-dione (PTAD) or 4-methyl-1,2,4-triazole-3,5-dione (MTAD). The diradicals were trapped intermolecularly to afford polycyclic compounds. The computational studies (UB3LYP/6-31G*) of the denitrogenation of a model azoalkane suggested that stepwise denitrogenation with an activation energy of ca. 22 kcal/mol is the thermodynamically favored pathway for generation of the singlet diradical 1,2-diaza-4-silacyclopentane-3,5-diyl derivative via a 1,4-diazenyldiradical intermediate. The low activation energy of the denitrogenation reaction was consistent with the experimental observation that the azoalkane was labile under the preparation conditions used in this study.

  19. C3H7NO2S effect on concrete steel-rebar corrosion in 0.5 M H2SO4 simulating industrial/microbial environment

    NASA Astrophysics Data System (ADS)

    Okeniyi, Joshua Olusegun; Nwadialo, Christopher Chukwuweike; Olu-Steven, Folusho Emmanuel; Ebinne, Samaru Smart; Coker, Taiwo Ebenezer; Okeniyi, Elizabeth Toyin; Ogbiye, Adebanji Samuel; Durotoye, Taiwo Omowunmi; Badmus, Emmanuel Omotunde Oluwasogo

    2017-02-01

    This paper investigates C3H7NO2S (Cysteine) effect on the inhibition of reinforcing steel corrosion in concrete immersed in 0.5 M H2SO4, for simulating industrial/microbial environment. Different C3H7NO2S concentrations were admixed, in duplicates, in steel-reinforced concrete samples that were partially immersed in the acidic sulphate environment. Electrochemical monitoring techniques of open circuit potential, as per ASTM C876-91 R99, and corrosion rate, by linear polarization resistance, were then employed for studying anticorrosion effect in steel-reinforced concrete samples by the organic hydrocarbon admixture. Analyses of electrochemical test-data followed ASTM G16-95 R04 prescriptions including probability distribution modeling with significant testing by Kolmogorov-Smirnov and student's t-tests statistics. Results established that all datasets of corrosion potential distributed like the Normal, the Gumbel and the Weibull distributions but that only the Weibull model described all the corrosion rate datasets in the study, as per the Kolmogorov-Smirnov test-statistics. Results of the student's t-test showed that differences of corrosion test-data between duplicated samples with the same C3H7NO2S concentrations were not statistically significant. These results indicated that 0.06878 M C3H7NO2S exhibited optimal inhibition efficiency η = 90.52±1.29% on reinforcing steel corrosion in the concrete samples immersed in 0.5 M H2SO4, simulating industrial/microbial service-environment.

  20. 5-(3,4-Dimethoxybenzyl)-7-isopropyl-1,3,5-triazepane-2,6-dione acetonitrile solvate refined using a multipolar atom model.

    PubMed

    Ejsmont, Krzysztof; Boeglin, Joel; Didierjean, Claude; Guichard, Gilles; Jelsch, Christian

    2010-06-01

    The crystal structure of the title compound, C(16)H(23)N(3)O(4).CH(3)CN, was refined using a multipolar atom model transferred from an experimental electron-density database. The refinement showed some improvement in crystallographic statistical indices compared with the independent atom model. The triazepane ring adopts a twist-boat conformation. In the crystal structure, the molecule forms intermolecular contacts with 14 different neighbours. There are two N-H...O and one C-H...O intermolecular hydrogen bond.

  1. Synthesis of 4-((1E, 6E)-7-(4-hydroxy-3-methoxyphenyl)-3, 5-dioxohepta-1, 6-dienyl)-2-methoxyphenyl 4-fluorobenzoate, a novel monoester derivative of curcumin, its experimental and theoretical (DFT) studies

    NASA Astrophysics Data System (ADS)

    Srivastava, Sangeeta; Gupta, Preeti; Amandeep; Singh, Ranvijay Pratap

    2016-04-01

    Curcumin (1), isolated as a major component from the chloroform extract of Curcuma longa was converted to its ester derivative 4-((1E, 6E)-7-(4-hydroxy-3-methoxyphenyl)-3,5-dioxohepta-1,6-dienyl)-2-methoxyphenyl 4-fluorobenzoate (2). The compound has been characterized with the help of 1H, 13C NMR, UV, IR and mass spectrometry. The molecular geometry of synthesized compound was calculated in ground state by Density functional theory (DFT/B3LYP) using 6-31G (d,p) basis set. 1H and 13C NMR chemical shifts were calculated in ground state by using Gauge-Including Atomic Orbital (GIAO) approach and these values were correlated with experimental observations. The electronic properties such as HOMO and LUMO energies were calculated using time dependent Density Functional Theory (TD-DFT). Stability of the molecule as a result of hyper conjugative interactions and electron delocalization were analysed using Natural bond orbital (NBO) analysis. Intramolecular interactions were analysed by AIM (Atom in molecule) approach. Global reactivity descriptors were calculated to study the reactive site within molecule. The vibrational wavenumbers were calculated using DFT method and assigned with the help of potential energy distribution (PED). First hyperpolarizability values have been calculated to describe the nonlinear optical (NLO) property of the synthesized compounds. Molecular electrostatic potential (MEP) analysis has also been carried out.

  2. Solid state structure by X-ray and 13C CP/MAS NMR of new 5-[2-(N,N-dimethylamino)ethoxy]-4,7-dimethylcoumarins

    NASA Astrophysics Data System (ADS)

    Ostrowska, Kinga; Maciejewska, Dorota; Dobrzycki, Łukasz; Socha, Pawel

    2016-05-01

    5-[2-(N,N-dimethylamino)ethoxy]-4,7-dimethylcoumarin (1) and 6-acetyl-5-[2-(N,N-dimethylamino)ethoxy]-4,7-dimethylcoumarin (2), structurally related, were synthesized using both conventional and microwave-assisted approach. An impact of acetyl groups on the molecular structure of coumarin derivatives has been examined. Crystals of 2 were investigated using single crystal and powder X-ray diffraction techniques. Compound 2 crystallizes forming two polymorphs (denoted as 2_1 and 2_2), both belonging to P21/c space group. Both polymorphs are comparably stable and can be formed simultaneously during crystallization process. The solid state structure was also analysed using the fully resolved 13C CP/MAS NMR. The double signals with the intensity ratio of about 1:1 which were observed in the 13C CP/MAS NMR spectrum of compound 1 must arise due to the presence of two conformers of 1. In contrast, NMR spectrum recorded for powder mixture of two polymorphs of compound 2 displays no signal splitting. This is related to structural similarities of molecules in both polymorphs.

  3. Quantification of ultra-trace molybdenum using 4-amino-5-hydroxynaphthalene-2,7-disulfonic acid monosodium salt as a chromogenic probe.

    PubMed

    Nagaraja, Padmarajaiah; Krishna, Honnur; Shivakumar, Anantharaman; Paulas, Anthonydas Robert; Rangappa, Dinesh

    2011-04-15

    A simple, ultrasensitive, nonextractive spectrophotometric method has been developed for the assay of Mo(VI), which involves Mo-catalyzed oxidation of 4-amino-5-hydroxynaphthalene-2,7-disulfonic acid monosodium salt (AHNDSA) by H(2)O(2) in acetic acid/sodium acetate buffer yielding an intense pink colored product with λ(max) of 540 nm. Beer's law is obeyed in the range of 10-240 ng/ml with molar absorptivity of 3.0137×10(5)L mol(-1)cm(-1). The LOD and LOQ were found to be 0.7696 and 2.565 ng/ml, respectively. The applicability of the method toward water and biological samples was tested and statistically compared with a reference method.

  4. Discovery of 1-(4-Methoxyphenyl)-7-oxo-6-(4-(2-oxopiperidin-1-yl)phenyl)-4,5,6,7-tetrahydro- 1H-pyrazolo[3,4-c]pyridine-3-carboxamide (Apixaban, BMS-562247), a Highly Potent, Selective, Efficacious, and Orally Bioavailable Inhibitor of Blood Coagulation Factor Xa

    SciTech Connect

    Pinto, Donald J.P.; Orwat, Michael J.; Koch, Stephanie; Rossi, Karen A.; Alexander, Richard S.; Smallwood, Angela; Wong, Pancras C.; Rendina, Alan R.; Luettgen, Joseph M.; Knabb, Robert M.; He, Kan; Xin, Baomin; Wexler, Ruth R.; Lam, Patrick Y.S.

    2010-03-08

    Efforts to identify a suitable follow-on compound to razaxaban (compound 4) focused on modification of the carboxamido linker to eliminate potential in vivo hydrolysis to a primary aniline. Cyclization of the carboxamido linker to the novel bicyclic tetrahydropyrazolopyridinone scaffold retained the potent fXa binding activity. Exceptional potency of the series prompted an investigation of the neutral P{sub 1} moieties that resulted in the identification of the p-methoxyphenyl P{sub 1}, which retained factor Xa binding affinity and good oral bioavailability. Further optimization of the C-3 pyrazole position and replacement of the terminal P{sub 4} ring with a neutral heterocycle culminated in the discovery of 1-(4-methoxyphenyl)-7-oxo-6-(4-(2-oxopiperidin-1-yl)phenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-carboxamide (apixaban, compound 40). Compound 40 exhibits a high degree of fXa potency, selectivity, and efficacy and has an improved pharmacokinetic profile relative to 4.

  5. On the Fine Structure Splitting of the 3p43d 4D5/2 and 3p43d 4D7/2 Levels of Fe X

    NASA Astrophysics Data System (ADS)

    Judge, Philip G.; Hutton, Roger; Li, Wenxian; Brage, Tomas

    2016-12-01

    We study UV spectra obtained with the SO82-B slit spectrograph on board SKYLAB to estimate the fine structure (FS) splitting of the Cl-like 3{{{p}}}43{{d}}{}4{{{D}}}5/2 and 3{{{p}}}43{{d}}{}4{{{D}}}7/2 levels of Fe x. The splitting is of interest because the Zeeman effect mixes these levels, producing a “magnetically induced transition” (MIT) from 3{{{p}}}43{{d}}{}4{{{D}}}7/2 to 3{{{p}}}5{}2{{{P}}}3/2{{o}} for modest magnetic field strengths characteristic of the active solar corona. We estimate the splitting using the Ritz combination formula applied to two lines in the UV region of the spectrum close to 1603.2 Å, which decay from the level 3{{{p}}}4{(}1{{D}})3{{d}}{}2{{{G}}}7/2 to these two lower levels. The MIT and accompanying spin-forbidden transition lie near 257 Å. By careful inspection of a deep exposure obtained with the S082B instrument, we derive a splitting of ≲ 7+/- 3 cm-1. The upper limit arises because of a degeneracy between the effects of non-thermal line broadening and FS splitting for small values of the latter parameter. Although the data were recorded on photographic film, we solved for optimal values of line width and splitting of 8.3 ± 0.9 and 3.6 ± 2.7 cm-1.

  6. 7-(Pyrazol-4-yl)-3H-imidazo[4,5-b]pyridine-based derivatives for kinase inhibition: Co-crystallisation studies with Aurora-A reveal distinct differences in the orientation of the pyrazole N1-substituent.

    PubMed

    Bavetsias, Vassilios; Pérez-Fuertes, Yolanda; McIntyre, Patrick J; Atrash, Butrus; Kosmopoulou, Magda; O'Fee, Lisa; Burke, Rosemary; Sun, Chongbo; Faisal, Amir; Bush, Katherine; Avery, Sian; Henley, Alan; Raynaud, Florence I; Linardopoulos, Spiros; Bayliss, Richard; Blagg, Julian

    2015-10-01

    Introduction of a 1-benzyl-1H-pyrazol-4-yl moiety at C7 of the imidazo[4,5-b]pyridine scaffold provided 7a which inhibited a range of kinases including Aurora-A. Modification of the benzyl group in 7a, and subsequent co-crystallisation of the resulting analogues with Aurora-A indicated distinct differences in binding mode dependent upon the pyrazole N-substituent. Compounds 7a and 14d interact with the P-loop whereas 14a and 14b engage with Thr217 in the post-hinge region. These crystallographic insights provide options for the design of compounds interacting with the DFG motif or with Thr217.

  7. Synthesis and Application of 1,3,4,5,7,8-Hexafluorotetracyanonaphthoquinodimethane (F6-TNAP): A Conductivity Dopant for Organic Light-Emitting Devices

    SciTech Connect

    Koech, Phillip K.; Padmaperuma, Asanga B.; Wang, Liang; Swensen, James S.; Polikarpov, Evgueni; Darsell, Jens T.; Rainbolt, James E.; Gaspar, Daniel J.

    2010-07-13

    We report the synthesis, photophysical and organic light-emitting device (OLED) properties of an organic molecular p-dopant 1,3,4,5,7,8-hexafluorotetracyanonaphthoquinodimethane (F6-TNAP). F6-TNAP was obtained in a three step 2 pot synthesis from commercially available octafluoronaphthalene. Doping effect of F6-TNAP was evaluated using films of 1-5% F6-TNAP with N,N'-di-1-naphthyl-N,N'-diphenyl-1,1'-biphenyl-4,4'diamineα-NPD) co-evaporated on quartz. UV-vis analysis of these films showed an absorption peak at 950 nm corresponding to the charge transfer complex resulting from electron transfer from α-NPD to F6-TNAP. Hole only devices using α-NPD as the hole transport layer (HTL) doped with F6-TNAP show greater than 2V decrease in operating voltage compared to the undoped device. A decrease in operating voltage was also demonstrated in blue OLED devices using F6-TNAP doped HTL, with a slight decrease in external quantum efficiency (EQE), thus resulting in a net improvement in power efficiency.

  8. 7 CFR 371.4 - Veterinary Services.

    Code of Federal Regulations, 2010 CFR

    2010-01-01

    ... 7 Agriculture 5 2010-01-01 2010-01-01 false Veterinary Services. 371.4 Section 371.4 Agriculture..., DEPARTMENT OF AGRICULTURE ORGANIZATION, FUNCTIONS, AND DELEGATIONS OF AUTHORITY § 371.4 Veterinary Services. (a) General statement. Veterinary Services (VS) protects and safeguards the Nation's livestock...

  9. 7 CFR 319.73-4 - Costs.

    Code of Federal Regulations, 2010 CFR

    2010-01-01

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  10. 7 CFR 319.73-4 - Costs.

    Code of Federal Regulations, 2011 CFR

    2011-01-01

    ... 7 Agriculture 5 2011-01-01 2011-01-01 false Costs. 319.73-4 Section 319.73-4 Agriculture..., DEPARTMENT OF AGRICULTURE FOREIGN QUARANTINE NOTICES Coffee § 319.73-4 Costs. All costs of inspection... duty will be furnished without cost to the importer....

  11. 7 CFR 353.4 - Products covered.

    Code of Federal Regulations, 2011 CFR

    2011-01-01

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  12. 7 CFR 353.4 - Products covered.

    Code of Federal Regulations, 2012 CFR

    2012-01-01

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  13. 7 CFR 319.73-4 - Costs.

    Code of Federal Regulations, 2014 CFR

    2014-01-01

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  14. 7 CFR 319.73-4 - Costs.

    Code of Federal Regulations, 2012 CFR

    2012-01-01

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  15. 7 CFR 319.73-4 - Costs.

    Code of Federal Regulations, 2013 CFR

    2013-01-01

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  16. 7 CFR 351.4 - Records.

    Code of Federal Regulations, 2011 CFR

    2011-01-01

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  17. 7 CFR 331.4 - [Reserved

    Code of Federal Regulations, 2014 CFR

    2014-01-01

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  18. 7 CFR 331.4 - [Reserved

    Code of Federal Regulations, 2012 CFR

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  19. 7 CFR 331.4 - [Reserved

    Code of Federal Regulations, 2011 CFR

    2011-01-01

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  20. 7 CFR 331.4 - [Reserved

    Code of Federal Regulations, 2010 CFR

    2010-01-01

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  1. 7 CFR 331.4 - [Reserved

    Code of Federal Regulations, 2013 CFR

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  2. 7 CFR 319.75-4 - Treatments.

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    2010-01-01

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  3. 7 CFR 352.4 - Documentation.

    Code of Federal Regulations, 2010 CFR

    2010-01-01

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  4. 7 CFR 305.4 - [Reserved

    Code of Federal Regulations, 2010 CFR

    2010-01-01

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  5. 40 CFR 721.5540 - 1H,3H,5H-oxazolo [3,4-c] oxazole, dihydro-7a-methyl-.

    Code of Federal Regulations, 2014 CFR

    2014-07-01

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  6. 40 CFR 721.5540 - 1H,3H,5H-oxazolo [3,4-c] oxazole, dihydro-7a-methyl-.

    Code of Federal Regulations, 2013 CFR

    2013-07-01

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  7. 40 CFR 721.5540 - 1H,3H,5H-oxazolo [3,4-c] oxazole, dihydro-7a-methyl-.

    Code of Federal Regulations, 2011 CFR

    2011-07-01

    ... 40 Protection of Environment 31 2011-07-01 2011-07-01 false 1H,3H,5H-oxazolo oxazole, dihydro-7a... Specific Chemical Substances § 721.5540 1H,3H,5H-oxazolo oxazole, dihydro-7a-methyl-. (a) Chemical...-oxazolo oxazole, dihydro-7a-methyl- (PMN P-91-1324) is subject to reporting under this section for...

  8. 40 CFR 721.5540 - 1H,3H,5H-oxazolo [3,4-c] oxazole, dihydro-7a-methyl-.

    Code of Federal Regulations, 2012 CFR

    2012-07-01

    ... 40 Protection of Environment 32 2012-07-01 2012-07-01 false 1H,3H,5H-oxazolo oxazole, dihydro-7a... Specific Chemical Substances § 721.5540 1H,3H,5H-oxazolo oxazole, dihydro-7a-methyl-. (a) Chemical...-oxazolo oxazole, dihydro-7a-methyl- (PMN P-91-1324) is subject to reporting under this section for...

  9. Molecular cloning, characterization and expression analysis of Wnt4, Wnt5, Wnt6, Wnt7, Wnt10 and Wnt16 from Litopenaeus vannamei.

    PubMed

    Zhang, Shuang; Li, Chao-Zheng; Yang, Qi-Hui; Dong, Xiao-Hui; Chi, Shu-Yan; Liu, Hong-Yu; Shi, Li-Li; Tan, Bei-Ping

    2016-07-01

    The Wnt (Wg-type MMTV integration site) signaling represents as the negative regulator of virus-induced innate immune responses. Wnt genes act as ligands to activate the Wnt signaling. To know more about the information of Wnt genes in invertebrates, Litopenaeus vannamei Wnt genes (LvWnts) were identified and characterized. In this study, Six Wnt genes (LvWnt4, LvWnt5, LvWnt6, LvWnt7, LvWnt10 and LvWnt16) were obtained in L. vannamei. The complete cDNAs open reading frames (ORF) of LvWnt4, LvWnt5, LvWnt6, LvWnt7, LvWnt10 and LvWnt16 were 1077 bp, 1107 bp, 1350 bp, 1047 bp, 1509 bp and 1158 bp (GenBank accession no. KU169896, KU169897, KU169898, KU169899, KU169900 and KU169901), encoding 358, 368, 449, 348, 502 and 385 amino acid (aa) residues respectively. All the six members of LvWnts contain a Wnt1 domain, which is considered as an important feature of Wnt gene family. ClustalW analysis with amino acid sequences revealed that the proportion of identity with other species was more than 48% for all the LvWnts except LvWnt10 (36-41%). The phylogenetic relationship analysis illustrated that different subtype of Wnts formed their own separate branches and were placed in branch of invertebrates respectively with strong bootstrap support. The constitutive expressions of LvWnts were confirmed by RT-PCR in all the examined five developmental stages and eleven tissues of L. vannamei with different express patterns. LvWnt4, LvWnt5 and LvWnt10 were expressed highest in nerve while LvWnt6, LvWnt7 and LvWnt16 were expressed highest in intestine, stomach and gill, respectively. In addition, all the LvWnts were regulated by white spot syndrome virus (WSSV) challenges at different levels in hepatopancreas, gill and hemocytes, suggesting that Wnt genes may play a role in the defense against pathogenic virus infection in innate immune of L. vannamei.

  10. Discovery of 4,5,6,7-Tetrahydrobenzo[1,2-d]thiazoles as Novel DNA Gyrase Inhibitors Targeting the ATP-Binding Site.

    PubMed

    Tomašič, Tihomir; Katsamakas, Sotirios; Hodnik, Žiga; Ilaš, Janez; Brvar, Matjaž; Solmajer, Tom; Montalvão, Sofia; Tammela, Päivi; Banjanac, Mihailo; Ergović, Gabrijela; Anderluh, Marko; Peterlin Mašič, Lucija; Kikelj, Danijel

    2015-07-23

    Bacterial DNA gyrase and topoisomerase IV are essential enzymes that control the topological state of DNA during replication and validated antibacterial drug targets. Starting from a library of marine alkaloid oroidin analogues, we identified low micromolar inhibitors of Escherichia coli DNA gyrase based on the 5,6,7,8-tetrahydroquinazoline and 4,5,6,7-tetrahydrobenzo[1,2-d]thiazole scaffolds. Structure-based optimization of the initial hits resulted in low nanomolar E. coli DNA gyrase inhibitors, some of which exhibited micromolar inhibition of E. coli topoisomerase IV and of Staphylococcus aureus homologues. Some of the compounds possessed modest antibacterial activity against Gram positive bacterial strains, while their evaluation against wild-type, impA and ΔtolC E. coli strains suggests that they are efflux pump substrates and/or do not possess the physicochemical properties necessary for cell wall penetration. Our study provides a rationale for optimization of this class of compounds toward balanced dual DNA gyrase and topoisomerase IV inhibitors with antibacterial activity.

  11. Aftershock relocation and frequency-size distribution, stress inversion and seismotectonic setting of the 7 August 2013 M = 5.4 earthquake in Kallidromon Mountain, central Greece

    NASA Astrophysics Data System (ADS)

    Ganas, Athanassios; Karastathis, Vassilios; Moshou, Alexandra; Valkaniotis, Sotirios; Mouzakiotis, Evangelos; Papathanassiou, George

    2014-03-01

    On August 7, 2013 a moderate earthquake (NOA ML = 5.1, NOA Mw = 5.4) occurred in central Kallidromon Mountain, in the Pthiotis region of central Greece. 2270 aftershocks were relocated using a modified 1-D velocity model for this area. The b-value of the aftershock sequence was b = 0.85 for a completeness magnitude of Mc = 1.7. The rate of aftershock decay was determined at p = 0.63. The spatial distribution of the aftershock sequence points towards the reactivation of a N70° ± 10°E striking normal fault at crustal depths between 8 and 13 km. A NNW-SSE cross-section imaged the activation of a steep, south dipping normal fault. A stress inversion analysis of 12 focal mechanisms showed that the minimum horizontal stress is extensional at N173°E. No primary surface ruptures were observed in the field; however, the earthquake caused severe damage in the villages of the Kallidromon area. The imaged fault strike and the orientation of the long-axis of the aftershock sequence distribution are both at a high-angle to the strike of known active faults in this area of central Greece. We interpret the Kallidromon seismic sequence as release of extensional seismic strain on secondary, steep faults inside the Fokida-Viotia crustal block.

  12. Effects of 3,3',4,4',5-pentachlorobiphenyl and 2,3,7,8-tetrachlorodibenzo-p-dioxin injected into the yolks of double-crested cormorant (Phalacrocorax auritus) eggs prior to incubation

    USGS Publications Warehouse

    Powell, D.C.; Aulerich, R.J.; Meadows, J.C.; Tillitt, D.E.; Kelly, M.E.; Stromborg, K.L.; Melancon, M.J.; Fitzgerald, S.D.; Bursian, S.J.

    1998-01-01

    Double-crested cormorant (Phalacrocorax auritus) eggs were injected with either 3,3',4,4',5-pentachlorobiphenyl (polychlorinated biphenyl [PCB] 126; 70-698 ?g/kg egg) or 2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD; 1.3-11.7 ?g/kg egg) prior to incubation. These compounds were injected into the yolks of cormorant eggs collected from incomplete clutches at isolated colonies on Lake Winnipegosis, Manitoba, Canada. Eggs were incubated for approximately 26 to 28 d. After hatching the brain, bursa, heart, liver, and spleen were dissected and weighed. Torsos were preserved in formalin for examination of the gonads. Median lethal doses (LD50s) calculated from mortality data at hatching were 177 and 4.0 ?g/kg egg for PCB 126 and TCDD, respectively. No significant differences were found in the incidence of developmental abnormalities in any of the treatment groups. Bursa weights were significantly less in the greatest (11.7 ?g/kg egg) TCDD group compared to the vehicle control group. Spleen weights were significantly less in the 349 ?g PCB 126/kg egg and the 5.4 and 11.7 ?g TCDD/kg egg groups when compared to the vehicle control group. No histological alterations of the gonads were found. Hepatic ethoxyresorufin-O-deethylase activity in all PCB 126 and TCDD dose groups was significantly greater compared to the control activity. The toxic equivalency factor for PCB 126 was 0.02

  13. The role of 5-arylalkylamino- and 5-piperazino- moieties on the 7-aminopyrazolo[4,3-d]pyrimidine core in affecting adenosine A1 and A2A receptor affinity and selectivity profiles.

    PubMed

    Squarcialupi, Lucia; Betti, Marco; Catarzi, Daniela; Varano, Flavia; Falsini, Matteo; Ravani, Annalisa; Pasquini, Silvia; Vincenzi, Fabrizio; Salmaso, Veronica; Sturlese, Mattia; Varani, Katia; Moro, Stefano; Colotta, Vittoria

    2017-12-01

    New 7-amino-2-phenylpyrazolo[4,3-d]pyrimidine derivatives, substituted at the 5-position with aryl(alkyl)amino- and 4-substituted-piperazin-1-yl- moieties, were synthesized with the aim of targeting human (h) adenosine A1 and/or A2A receptor subtypes. On the whole, the novel derivatives 1-24 shared scarce or no affinities for the off-target hA2B and hA3 ARs. The 5-(4-hydroxyphenethylamino)- derivative 12 showed both good affinity (Ki = 150 nM) and the best selectivity for the hA2A AR while the 5-benzylamino-substituted 5 displayed the best combined hA2A (Ki = 123 nM) and A1 AR affinity (Ki = 25 nM). The 5-phenethylamino moiety (compound 6) achieved nanomolar affinity (Ki = 11 nM) and good selectivity for the hA1 AR. The 5-(N(4)-substituted-piperazin-1-yl) derivatives 15-24 bind the hA1 AR subtype with affinities falling in the high nanomolar range. A structure-based molecular modeling study was conducted to rationalize the experimental binding data from a molecular point of view using both molecular docking studies and Interaction Energy Fingerprints (IEFs) analysis.[Formula: see text].

  14. A vibrational spectroscopic study of the silicate mineral lomonosovite Na5Ti2(Si2O7)(PO4)O2

    NASA Astrophysics Data System (ADS)

    Frost, Ray L.; López, Andrés; Theiss, Frederick L.; Graça, Leonardo M.; Scholz, Ricardo

    2015-01-01

    The mineral lomonosovite has been studied using a combination of scanning electron microscopy with energy dispersive X-ray analysis and vibrational spectroscopy. Qualitative chemical analysis gave Si, P, Na and Ti as the as major elements with small amounts of Mn, Ca, Fe and Al. The mineral lomonosovite has a formula Na5Ti2(Si2O7)(PO4)O2. Raman bands observed at 909, 925 and 939 cm-1 are associated with phosphate units. Raman bands found at 975, 999, 1070, 1080 and 1084 cm-1 are attributed to siloxane stretching vibrations. The observation of multiple bands in both the phosphate stretching and bending regions supports the concept that the symmetry of the phosphate anion in the structure of lomonosovite is significantly reduced. Infrared spectroscopy identifies bands in the water stretching and bending regions, thus suggesting that water is involved with the structure of lomonosovite either through adsorption on the surface or by bonding to the phosphate units.

  15. Vesicular PtdIns(3,4,5)P3 and Rab7 are key effectors of sea urchin zygote nuclear membrane fusion.

    PubMed

    Lete, Marta G; Byrne, Richard D; Alonso, Alicia; Poccia, Dominic; Larijani, Banafshé

    2017-01-15

    Regulation of nuclear envelope dynamics is an important example of the universal phenomena of membrane fusion. The signalling molecules involved in nuclear membrane fusion might also be conserved during the formation of both pronuclear and zygote nuclear envelopes in the fertilised egg. Here, we determine that class-I phosphoinositide 3-kinases (PI3Ks) are needed for in vitro nuclear envelope formation. We show that, in vivo, PtdIns(3,4,5)P3 is transiently located in vesicles around the male pronucleus at the time of nuclear envelope formation, and around male and female pronuclei before membrane fusion. We illustrate that class-I PI3K activity is also necessary for fusion of the female and male pronuclear membranes. We demonstrate, using coincidence amplified Förster resonance energy transfer (FRET) monitored using fluorescence lifetime imaging microscopy (FLIM), a protein-lipid interaction of Rab7 GTPase and PtdIns(3,4,5)P3 that occurs during pronuclear membrane fusion to create the zygote nuclear envelope. We present a working model, which includes several molecular steps in the pathways controlling fusion of nuclear envelope membranes.

  16. The molecular structure of the borate mineral inderite Mg(H4B3O7)(OH)ṡ5H2O - A vibrational spectroscopic study

    NASA Astrophysics Data System (ADS)

    Frost, Ray L.; López, Andrés; Xi, Yunfei; Lima, Rosa Malena Fernandes; Scholz, Ricardo; Granja, Amanda

    2013-12-01

    We have undertaken a study of the mineral inderite Mg(H4B3O7)(OH)ṡ5H2O a hydrated hydroxy borate mineral of magnesium using scanning electron microscopy, thermogravimetry and vibrational spectroscopic techniques. The structure consists of [ soroborate groups and Mg(OH)2(H2O)4 octahedra interconnected into discrete molecules by the sharing of two OH groups. Thermogravimetry shows a mass loss of 47.2% at 137.5 °C, proving the mineral is thermally unstable. Raman bands at 954, 1047 and 1116 cm-1 are assigned to the trigonal symmetric stretching mode. The two bands at 880 and 916 cm-1 are attributed to the symmetric stretching mode of the tetrahedral boron. Both the Raman and infrared spectra of inderite show complexity. Raman bands are observed at 3052, 3233, 3330, 3392 attributed to water stretching vibrations and 3459 cm-1 with sharper bands at 3459, 3530 and 3562 cm-1 assigned to OH stretching vibrations. Vibrational spectroscopy is used to assess the molecular structure of inderite.

  17. Synthesis and Photoelectrochemistry Characterization of Polymer based on 4,7-Di(thiophen-2-yl)-benzo[c][1,2,5]thiadiazole, (DTBT)

    NASA Astrophysics Data System (ADS)

    Lazo Jimenez, Luz Maria; Frontana-Uribe, Bernardo Antonio

    Poly[4,7-di-(thiophen-2-yl)-benzo[c]-[1,2,5] thiadiazole], P(DTBT), is used in polymer:PCMB blends as active layer on organic photovoltaic devices, (OPV); DTBT-based copolymers show well-reversible oxidation and reduction electrochemical processes. These processes indicate their hig electrochemical stability suitable for n- and p-doping. This is a typical feature benzothiadiazole containing molecules. In the present study the synthesis conditions of the monomer, 4,7-di-(thiophen-2-yl)-benzo[c]-[1,2,5]-thiadiazole based on Stille coupling reactions has been investigated and its respectively polymer P(DTBT) was prepared by repetitive potential-sweep anodic oxidation of the corresponding monomer DTBT onto Pt disk or indium tin oxide (ITO) electrodes. Electrochemical cyclic voltammetry (CV) was performed to determine the HOMO and the LUMO energy levels of the conjugated DTBT and P(DTBT), both exhibit amphoteric redox properties, n- and p- doping process. The optical gap estimated from electrochemical measurements of the polymer P(DTBT) was found to be 1.77 eV, which is close to the reported band gap (1.1-1.2eV) determined by optical absorption technique . Photoelectrochemical characterization of P(DTBT) was realized from UV-Vis-NIR spectra recorded at different applied potentials. These result are correlated with the charge-transfer phenomena in the polymers applied as active layer on OPV`s. Av. Universidad 3000. Coyoacán.C.P. 04510. México. D.F. MEXICO.

  18. Molecular Engineering of Liquid Crystalline Polymers by Living Polymerization. 9. Living Cationic Polymerization of 5-((4-Cyano-4’-Biphenyl) oxy)pentyl Vinyl Ethers and 7-((4-Cyano-4’-Biphenyl)oxy)heptyl Vinyl Ether, and the Mesomorphic Behavior of the Resulting Polymers

    DTIC Science & Technology

    1990-10-16

    REPRODUCEDO A"? GOVERPNME14T EXPENSE AD 2979 T.pOCUMENTATION PiA,4j -* L E is RkEPoRT SC-R-Y CLA i.ATiO It lb RESTRiCTovE MARKiNGS 26 SECURITYr C...PROCuREMENT INSTRUMENT IDENTIFICATION NUMBER OGN IZAT7ION If picb & L . AZORE SS (Ciay, Sr, arad ZIP Coot) 10 SOURCE OF ’UNDING NUMBERS office of Naval...mesomorphic behavior of poly( L .-.) and poly(6-_7) is discussed and compared to that of 5-[(4-cyano-4’- biphenyl)oxy]pentyl ethyl ether (8)and 7-f (4-cyano

  19. Second order phase transition temperature of single crystals of Gd5Si1.3Ge2.7 and Gd5Si1.4Ge2.6

    DOE PAGES

    Hadimani, R. L.; Melikhov, Y.; Schlagel, D. L.; ...

    2015-01-30

    Gd5(SixGe1–x)4 has mixed phases in the composition range 0.32 < x < 0.41, which have not been widely studied. In this paper, we have synthesized and indexed single crystal samples of Gd5Si1.3Ge2.7 and Gd5Si1.4Ge2.6. In this study, we have investigated the first order and second order phase transition temperatures of these samples using magnetic moment vs. temperature and magnetic moment vs. magnetic field at different temperatures. We have used a modified Arrott plot technique that was developed and reported by us previously to determine the “hidden” second order phase transition temperature of the orthorhombic II phase.

  20. Lead optimization of a pyrazolo[1,5-a]pyrimidin-7(4H)-one scaffold to identify potent, selective and orally bioavailable KDM5 inhibitors suitable for in vivo biological studies.

    PubMed

    Liang, Jun; Zhang, Birong; Labadie, Sharada; Ortwine, Daniel F; Vinogradova, Maia; Kiefer, James R; Gehling, Victor S; Harmange, Jean-Christophe; Cummings, Richard; Lai, Tommy; Liao, Jiangpeng; Zheng, Xiaoping; Liu, Yichin; Gustafson, Amy; Van der Porten, Erica; Mao, Weifeng; Liederer, Bianca M; Deshmukh, Gauri; Classon, Marie; Trojer, Patrick; Dragovich, Peter S; Murray, Lesley

    2016-08-15

    Starting with a lead [1,5-a]pyrimidin-7(4H)-one-containing molecule (1), we generated potent, selective and orally bioavailable KDM5 inhibitors. Using structure- and property-based approaches, we designed 48 with improved cell potency (PC9 H3K4Me3 EC50=0.34μM). Furthermore, 48 maintained suitable physiochemical properties and displayed an excellent pharmacokinetic (PK) profile in mice. When dosed orally in mice at 50mg/kg twice a day (BID), 48 showed an unbound maximal plasma concentration (Cmax) >15-fold over its cell EC50, thereby providing a robust chemical probe for studying KDM5 biological functions in vivo.

  1. Characterization and cross calibration of Agfa D4, D7, and D8 and Kodak SR45 x-ray films against direct exposure film at 4.0-5.5 keV

    SciTech Connect

    Lanier, N.E.; Cowan, J.S.; Workman, J.

    2006-04-15

    Kodak direct exposure film (DEF) [B. L. Henke et al., J. Opt. Soc. Am. B 3, 1540 (1986)] has been the standard for moderate energy (1-10 keV) x-ray diagnostic applications among the high-energy-density and inertial confinement fusion research communities. However, market forces have prompted Kodak to discontinue production of DEF, leaving these specialized communities searching for a replacement. We have conducted cross-calibration experiments and film characterizations on five possible substitutes for Kodak DEF. The film types studied were Kodak's Biomax MR (BMR) and SR45 along with Agfa's D8, D7, and D4sc. None of the films tested matched the speed of DEF. BMR and D8 were closest but D8 exhibited lower noise, with superior resolution and dynamic range. Agfa D7, Agfa D4sc, and Kodak SR45 were significantly less sensitive than BMR and D8, however, the improvements they yielded in resolution and dynamic range warrant their use if experimental constraints allow.

  2. Characterization and cross calibration of Agfa D4, D7, and D8 and Kodak SR45 x-ray films against direct exposure film at 4.0-5.5 keV

    NASA Astrophysics Data System (ADS)

    Lanier, N. E.; Cowan, J. S.; Workman, J.

    2006-04-01

    Kodak direct exposure film (DEF) [B. L. Henke et al., J. Opt. Soc. Am. B 3, 1540 (1986)] has been the standard for moderate energy (1-10keV) x-ray diagnostic applications among the high-energy-density and inertial confinement fusion research communities. However, market forces have prompted Kodak to discontinue production of DEF, leaving these specialized communities searching for a replacement. We have conducted cross-calibration experiments and film characterizations on five possible substitutes for Kodak DEF. The film types studied were Kodak's Biomax MR (BMR) and SR45 along with Agfa's D8, D7, and D4sc. None of the films tested matched the speed of DEF. BMR and D8 were closest but D8 exhibited lower noise, with superior resolution and dynamic range. Agfa D7, Agfa D4sc, and Kodak SR45 were significantly less sensitive than BMR and D8, however, the improvements they yielded in resolution and dynamic range warrant their use if experimental constraints allow.

  3. Synthesis and crystal structure of N-(4-chloro­phen­yl)-5,7-dimethyl-1,2,4-triazolo[1,5-a]pyrimidin-2-amine

    PubMed Central

    Repich, Hlib; Orysyk, Svitlana; Savytskyi, Pavlo; Pekhnyo, Vasyl

    2017-01-01

    The title compound, C13H12ClN5, was synthesized by the cyclization of 1-(4,6-di­methyl­pyrimidin-2-yl)-4-phenyl­thio­semicarbazide in the presence of Ni(NO3)2. The mol­ecular structure of the compound is essentially planar. In the crystal, mol­ecules form dimers via pairs of N—H⋯N hydrogen bonds between the H atom of the exocyclic amino group and the N atom at the 4-position of the triazole ring. The resulting dimers are packed into layers which are connected by π-stacking inter­actions between the aromatic systems of the pyrimidine and benzene nuclei, and between the triazole cores. PMID:28083130

  4. Protective effects of 5,7,4'-trihydroxy-6,3'dimethoxy-flavone 5-O-α-l-rhamnopyranoside, isolated from Annona squamosa leaves in thyrotoxicosis and in hepatic lipid peroxidation in rats.

    PubMed

    Panda, Sunanda; Kar, Anand

    2015-12-15

    Hitherto unknown protective effects of 5,7,4'-trihydroxy-6,3'dimethoxy-flavone 5-O-α-l-rhamnopyranoside (THDMF-Rha); isolated from Annona squamosa leaves were evaluated in l-thyroxine (l-T4)-induced thyrotoxicosis in rats. Administration of l-T4 at 500μg/kg body weight for 12days increased the levels of serum thyroid hormones, the activity of 5'-monodeiodinase-I (5'DI) and hepatic glucose-6-phosphatase (G-6Pase) as well as lipid peroxidation (LPO); with a parallel decrease in the levels of cellular antioxidants and serum lipids. However, administration of the isolated THDMF-Rha at a pre-standardized dose for 15days ameliorated the l-T4-induced alterations in the levels of thyroid hormones, hepatic LPO, G-6-Pase, 5'DI activity, and cellular levels of antioxidants and improved the status of different serum lipids, suggesting its antithyroidal and antioxidative potential. As compared to standard antithyroid drug, propylthiouracil, THDMF-Rha appeared to be more promising.

  5. 4,7-Dimethoxy-5-methyl-1,3-benzodioxole from Antrodia camphorata inhibits LPS-induced inflammation via suppression of NF-κB and induction HO-1 in RAW264.7 cells.

    PubMed

    Shie, Pei-Hsin; Wang, Sheng-Yang; Lay, Horng-Liang; Huang, Guan-Jhong

    2016-02-01

    Several benzenoid compounds have been isolated from Antrodia camphorata are known to have excellent anti-inflammatory activity. In this study, we investigated the anti-inflammatory potential of 4,7-dimethoxy-5-methyl-1,3-benzodioxole (DMB), one of the major benzenoid compounds isolated from the mycelia of A. camphorata. DMB significantly decreased the LPS-induced production of pro-inflammatory molecules, such as nitric oxide (NO), interleukin-1β (IL-1β), and tumor necrosis factor-α (TNF-α) in RAW264.7 cells. In addition, DMB suppressed the protein levels of inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2) in a dose dependent manner. Moreover, DMB significantly suppressed LPS-induced nuclear translocation of nuclear factor-κB (NF-κB), and this inhibition was found to be associated with decreases in the phosphorylation and degradation of its inhibitor, inhibitory κB-α (IκB-α). Moreover, we found that DMB markedly inhibited the protein expression level of Toll-like receptor 4 (TLR4). Furthermore, treatment with DMB significantly increased hemoxygenase-1 (HO-1) expression in RAW264.7 cells, which is further confirmed by hemin, a HO-1 enhancer, significantly attenuated the LPS-induced pro-inflammatory molecules and iNOS and TLR4 protein levels. Taken together, the present study suggests that DMB may have therapeutic potential for the treatment of inflammatory diseases.

  6. We are Family: the Conformations of 1-FLUOROALKANES, C_nH2n+1F (n = 2,3,4,5,6,7,8)

    NASA Astrophysics Data System (ADS)

    Obenchain, Daniel A.; Orellana, W.; Cooke, S. A.

    2016-06-01

    he pure rotational spectra of the n = 5, 6, 7, and 8 members of the 1-fluoroalkane family have been recorded between 7 GHz and 14 GHz using chirped pulse Fourier transform microwave spectroscopy. The spectra have been analyzed and results will be presented and compared with previous work on the n= 2, 3, and 4 members. The lowest energy conformer for all family members has the common feature that the fluorine is in a gauche position relative to the alkyl tail for which all other heavy atom dihedral angles, where appropriate, are 180 degrees. For the n = 3 and higher family members the second lowest energy conformer has all heavy atom dihedral angles equal to 180 degrees. For each family member transitions carried by both low energy conformers were observed in the collected rotational spectra. Quantum chemical calculations were performed and trends in the energy separations between these two common conformers will be presented as a function of chain length. Furthermore, longer chain lengths have been examined using only quantum chemical calculations and results will be presented. M. Hayashi, M. Fujitake, T. Inagusa, S. Miyazaki, J.Mol.Struct., 216, 9-26, 1990 W. Caminati, A. C. Fantoni, F. Manescalchi, F. Scappini, Mol.Phys., 64, 1089 ,1988 L. B. Favero, A. Maris, A. Degli Esposti, P. G. Favero, W. Caminati, G. Pawelke, Chem.Eur.J., 6(16), 3018-3025, 2000

  7. Structural characterization, vibrational study, NLO and DFT calculations of a novel organic sulfate monohydrate templated with (S)-(-)-2,6-diammonium-4,5,6,7-tetrahydrobenzothiazole

    NASA Astrophysics Data System (ADS)

    Barhoumi, Abir; Mhiri, Tahar; Dammak, Thameur; Suñol, Joan Josep; Belhouchet, Mohamed

    2017-01-01

    A single crystal of (S)-(-)-2,6-diammonium-4,5,6,7-tetrahydrobenzothiazole sulfate monohydrate has been synthesized and grown at room temperature by slow evaporation of aqueous solution. The studied compound crystallizes in the space group P212121 of the orthorhombic system with cell parameters a = 7.0014(12), b = 8.7631(15), c = 19.773(3) Å. We report the molecular structure and the theoretical and experimental vibrational spectra of the synthesized compound. The atomic arrangement, which is an alternation of organic inorganic layers linked together through hydrogen bonds, gives rise to three types of rings formed by the interconnection of organic-inorganic entities. The experimental FT-IR and the Raman spectra the synthesized compound were recorded and analyzed. The peaks assignment has been made unambiguously from the literature. To confirm the assignment, the experimental spectra were compared with theoretical spectra obtained with the Gaussian 98 program by the Density Functional Theory (DFT) method using B3LYP function with the LanL2DZ basis set. Moreover, to study the nonlinear optical (NLO) property of this compound, the hyperpolarizability βtot, the electric dipole μtot and the polarizability αtot were calculated using the DFT. Based on our calculation the synthesized compound has a non-zero hyperpolarizability suggesting that it may be used in some NLO applications.

  8. (meso-5,7,7,12,14,14-Hexamethyl-1,4,8,11-tetra­azacyclo­tetra­deca-4,11-diene)copper(II) bis­[O,O′-bis­(4-methyl­phen­yl) dithio­phosphate

    PubMed Central

    He, Lin-Xin; Zou, Li-Ke; Xie, Bin; Xiang, Yang-Guang; Feng, Jian-Shen

    2010-01-01

    The title compound, [Cu(C16H32N4)](C14H14O2PS2)2 or [Cu(trans[14]dien)][S2P(OC6H4Me-4)2]2, where trans[14]dien is meso-5,7,7,12,14,14-hexa­methyl-1,4,8,11-tetra­azacyclo­tetra­deca-4,11-diene, was obtained by the reaction of [Cu(trans[14]dien)](ClO4)2 and [(C2H5)2NH]2 [S2P(OC6H4Me-4)2]2. The CuII atom lies on a centre of inversion and possesses a relatively undistorted square-planar coordination arrangement with four N atoms of the macrocyclic tetra­mine trans[14]dien [Cu—N = 1.9716 (19) and 2.0075 (19) Å]. The two uncoordinated [(4-MeC6H4O)2PS2]− groups act as counter-ions to balance the charge and inter­act with the [Cu(trans[14]dien)]2+ complex cation through N—H⋯S hydrogen bonds. PMID:21580524

  9. The arylpiperazine derivatives N-(4-cyanophenylmethyl)-4-(2-diphenyl)-1-piperazinehexanamide and N-benzyl-4-(2-diphenyl)-1-piperazinehexanamide exert a long-lasting inhibition of human serotonin 5-HT7 receptor binding and cAMP signaling.

    PubMed

    Atanes, Patricio; Lacivita, Enza; Rodríguez, Javier; Brea, José; Burgueño, Javier; Vela, José Miguel; Cadavid, María Isabel; Loza, María Isabel; Leopoldo, Marcello; Castro, Marián

    2013-12-01

    We performed a detailed in vitro pharmacological characterization of two arylpiperazine derivatives, compound N-(4-cyanophenylmethyl)-4-(2-diphenyl)-1-piperazinehexanamide (LP-211) previously identified as a high-affinity brain penetrant ligand for 5-hydroxytryptamine (serotonin) type 7 (5-HT7) receptors, and its analog N-benzyl-4-(2-diphenyl)-1-piperazinehexanamide (MEL-9). Both ligands exhibited competitive displacement of [(3)H]-(2R)-1-[(3-hydroxyphenyl)sulfonyl]-2-[2-(4-methyl-1-piperidinyl)ethyl]pyrrolidine ([(3)H]-SB-269970) radioligand binding and insurmountable antagonism of 5-carboxamidotryptamine (5-CT)-stimulated cyclic adenosine monophosphate (cAMP) signaling in human embryonic kidney (HEK293) cells stably expressing human 5-HT7 receptors. They also inhibited forskolin-stimulated adenylate cyclase activity in 5-HT7-expressing HEK293 cells but not in the parental cell line. The compounds elicited long-lasting (at least 24 h) concentration-dependent inhibition of radioligand binding at 5-HT7-binding sites in whole-cell radioligand binding assays, after pretreatment of the cells with the compounds and subsequent compound removal. In cAMP assays, pretreatment of cells with the compounds rendered 5-HT7 receptors unresponsive to 5-CT and also rendered 5-HT7-expressing HEK293 cells unresponsive to forskolin. Compound 1-(2-biphenyl)piperazine (RA-7), a known active metabolite of LP-211 present in vivo, was able to partially inhibit 5-HT7 radioligand binding in a long-lasting irreversible manner. Hence, LP-211 and MEL-9 were identified as high-affinity long-acting inhibitors of human 5-HT7 receptor binding and function in cell lines. The detailed in vitro characterization of these two pharmacological tools targeting 5-HT7 receptors may benefit the study of 5-HT7 receptor function and it may lead to the development of novel selective pharmacological tools with defined functional properties at 5-HT7 receptors.

  10. LC-UV-Guided Isolation and Structure Determination of Lancolide E: A Nortriterpenoid with a Tetracyclo[5.4.0.0(2,4).0(3,7)]undecane-Bridged System from a "Talented" Schisandra Plant.

    PubMed

    Shi, Yi-Ming; Cai, Song-Liang; Li, Xiao-Nian; Liu, Miao; Shang, Shan-Zhai; Du, Xue; Xiao, Wei-Lie; Pu, Jian-Xin; Sun, Han-Dong

    2016-01-04

    Lancolide E (1) featuring a complex tetracyclo[5.4.0.0(2,4).0(3,7)]undecane-bridged system that is constructed by an eight-, a three-, and two five-membered carbon rings in a sterically congested region was obtained in trace amounts from a "talented" schinortriterpenoid producer Schisandra lancifolia. Its structure was fully characterized by combining 2D NMR spectroscopy, theoretical calculations, and X-ray diffraction analysis. The biogenetic pathway of 1 was proposed to involve a Prins cyclization.

  11. Phthalocyanines functionalized with 2-methyl-5-nitro-1H-imidazolylethoxy and 1,4,7-trioxanonyl moieties and the effect of metronidazole substitution on photocytotoxicity.

    PubMed

    Wierzchowski, Marcin; Sobotta, Lukasz; Skupin-Mrugalska, Paulina; Kruk, Justyna; Jusiak, Weronika; Yee, Michael; Konopka, Krystyna; Düzgüneş, Nejat; Tykarska, Ewa; Gdaniec, Maria; Mielcarek, Jadwiga; Goslinski, Tomasz

    2013-10-01

    Four novel magnesium(II) and zinc(II) phthalocyanines bearing 1,4,7-trioxanonyl, polyether and/or (2-methyl-5-nitro-1H-imidazol-1-yl)ethoxy, heterocyclic substituents at their non-peripheral positions were synthesized and assessed in terms of physicochemical and biological properties. Magnesium phthalocyanine derivatives bearing polyether substituents (Pc-1), a mixed system of polyether and heterocyclic substituents (Pc-3), and four heterocyclic substituents (Pc-4), respectively, were synthesized following the Linstead macrocyclization reaction procedure. Zinc phthalocyanine (Pc-2) bearing polyether substituents at non-peripheral positions was synthesized following the procedure in n-pentanol with the zinc acetate, and DBU. Novel phthalocyanines were purified by flash column chromatography and characterized using NMR, MS, UV-Vis and HPLC. Moreover, two precursors in macrocyclization reaction phthalonitriles were characterized using X-ray. Photophysical properties of the novel macrocycles were evaluated, including UV-Vis spectra analysis and aggregation study. All macrocycles subjected to singlet oxygen generation and the oxidation rate constant measurements exhibited lower quantum yields of singlet oxygen generation in DMSO than in DMF. In addition, the Pc-2 molecule was found to be the most efficient singlet oxygen generator from the group of macrocycles studied. The photocytotoxicity evaluated on the human oral squamous cell carcinoma cell line, HSC-3, for Pc-3 was significantly higher than that for Pc-1, Pc-2, and Pc-4. Interestingly, Pc-3 was found to be the most active macrocycle in vitro although its ability to generate singlet oxygen was significantly lower than those of Pc-1 and Pc-2. However, attempts to encapsulate phthalocyanines Pc-1-Pc-3 in liposomal membranes were unsuccessful. The phthalocyanine-nitroimidazole conjugate, Pc-4 was encapsulated in phosphatidylglycerol:phosphatidylcholine unilamellar liposomes and subjected to photocytotoxicity study.

  12. Association of Brain DNA Methylation in SORL1, ABCA7, HLA-DRB5, SLC24A4, and BIN1 With Pathological Diagnosis of Alzheimer Disease

    PubMed Central

    Yu, Lei; Chibnik, Lori B.; Srivastava, Gyan P.; Pochet, Nathalie; Yang, Jingyun; Xu, Jishu; Kozubek, James; Obholzer, Nikolaus; Leurgans, Sue E.; Schneider, Julie A.; Meissner, Alexander; De Jager, Philip L.; Bennett, David A.

    2015-01-01

    IMPORTANCE Recent large-scale genome-wide association studies have discovered several genetic variants associated with Alzheimer disease (AD); however, the extent to which DNA methylation in these AD loci contributes to the disease susceptibility remains unknown. OBJECTIVE To examine the association of brain DNA methylation in 28 reported AD loci with AD pathologies. DESIGN, SETTING, AND PARTICIPANTS Ongoing community-based clinical pathological cohort studies of aging and dementia (the Religious Orders Study and the Rush Memory and Aging Project) among 740 autopsied participants 66.0 to 108.3 years old. EXPOSURES DNA methylation levels at individual CpG sites generated from dorsolateral prefrontal cortex tissue using a bead assay. MAIN OUTCOMES AND MEASURES Pathological diagnosis of AD by National Institute on Aging–Reagan criteria following a standard postmortem examination. RESULTS Overall, 447 participants (60.4%) met the criteria for pathological diagnosis of AD. Brain DNA methylation in SORL1, ABCA7, HLA-DRB5, SLC24A4, and BIN1 was associated with pathological AD. The association was robustly retained after replacing the binary trait of pathological AD with 2 quantitative and molecular specific hallmarks of AD, namely, Aβ load and paired helical filament tau tangle density. Furthermore, RNA expression of transcripts of SORL1 and ABCA7 was associated with paired helical filament tau tangle density, and the expression of BIN1 was associated with Aβ load. CONCLUSIONS AND RELEVANCE Brain DNA methylation in multiple AD loci is associated with AD pathologies. The results provide further evidence that disruption of DNA methylation is involved in the pathological process of AD. PMID:25365775

  13. Consistency of land surface reflectance data: presentation of a new tool and case study with Formosat-2, SPOT-4 and Landsat-5/7/8 data

    NASA Astrophysics Data System (ADS)

    Claverie, M.; Vermote, E.; Franch, B.; Huc, M.; Hagolle, O.; Masek, J.

    2013-12-01

    Maintaining consistent dataset of Surface Reflectance (SR) data derived from the large panel of in-orbit sensors is an important challenge to ensure long term analysis of earth observation data. Continuous validation of such SR products through comparison with a reference dataset is thus an important challenge. Validating with in situ or airborne SR data is not easy since the sensors rarely match completely the same spectral, spatial and directional characteristics of the satellite measurement. Inter-comparison between satellites sensors data appears as a valuable tool to maintain a long term consistency of the data. However, satellite data are acquired at various times of the day (i.e., variation of the atmosphere content) and within a relative large range of geometry (view and sun angles). Also, even if band-to-band spectral characteristics of optical sensors are closed, they rarely have identical spectral responses. As the results, direct comparisons without consideration of these differences are poorly suitable. In this study, we suggest a new systematic method to assess land optical SR data from high to medium resolution sensors. We used MODIS SR products (MO/YD09CMG) which benefit from a long term calibration/validation process, to assess SR from 3 sensors data: Formosat-2 (280 scenes 24x24km - 5 sites), SPOT-4 (62 scenes 120x60km - 1 site) and Landsat-5/7 (104 180x180km scenes - 50 sites). The main issue concerns the difference in term of geometry acquisition between MODIS and compared sensors data. We used the VJB model (Vermote et al. 2009, TGRS) to correct MODIS SR from BRDF effects and to simulate SR at the corresponding geometry (view and sun angles) of each pixel of the compared sensor data. The comparison is done at the CMG spatial resolution (0.05°) which ensures a constant field-of-view and negligible geometrical errors. Figure 1 displays the summary of the NIR results through APU graphs where metrics A, P and U stands for Accuracy, Precision and

  14. Electroexcitation of the Roper resonance for 1.7 < Q**2 < 4.5 -GeV2 in vec-ep ---> en pi+

    SciTech Connect

    Aznauryan, Inna; Burkert, Volker; Kim, Wooyoung; Park, Kil; Adams, Gary; Amaryan, Moscov; Amaryan, Moskov; Ambrozewicz, Pawel; Anghinolfi, Marco; Asryan, Gegham; Avagyan, Harutyun; Bagdasaryan, H.; Baillie, Nathan; Ball, J.P.; Ball, Jacques; Baltzell, Nathan; Barrow, Steve; Batourine, V.; Battaglieri, Marco; Bedlinskiy, Ivan; Bektasoglu, Mehmet; Bellis, Matthew; Benmouna, Nawal; Berman, Barry; Biselli, Angela; Blaszczyk, Lukasz; Bonner, Billy; Bookwalter, Craig; Bouchigny, Sylvain; Boyarinov, Sergey; Bradford, Robert; Branford, Derek; Briscoe, Wilbert; Brooks, William; Bultmann, S.; Bueltmann, Stephen; Butuceanu, Cornel; Calarco, John; Careccia, Sharon; Carman, Daniel; Casey, Liam; Cazes, Antoine; Chen, Shifeng; Cheng, Lu; Cole, Philip; Collins, Patrick; Coltharp, Philip; Cords, Dieter; Corvisiero, Pietro; Crabb, Donald; Crede, Volker; Cummings, John; Dale, Daniel; Dashyan, Natalya; De Masi, Rita; De Vita, Raffaella; De Sanctis, Enzo; Degtiarenko, Pavel; Denizli, Haluk; Dennis, Lawrence; Deur, Alexandre; Dhamija, Seema; Dharmawardane, Kahanawita; Dhuga, Kalvir; Dickson, Richard; Djalali, Chaden; Dodge, Gail; Donnelly, J.; Doughty, David; Dugger, Michael; Dytman, Steven; Dzyubak, Oleksandr; Egiyan, Hovanes; Egiyan, Kim; Elfassi, Lamiaa; Elouadrhiri, Latifa; Eugenio, Paul; Fatemi, Renee; Fedotov, Gleb; Feldman, Gerald; Feuerbach, Robert; Forest, Tony; Fradi, Ahmed; Funsten, Herbert; Gabrielyan, Marianna; Garcon, Michel; Gavalian, Gagik; Gevorgyan, Nerses; Gilfoyle, Gerard; Giovanetti, Kevin; Girod, Francois-Xavier; Goetz, John; Gohn, Wesley; Golovach, Evgeny; Gonenc, Atilla; Gordon, Christopher; Gothe, Ralf; Graham, L.; Griffioen, Keith; Guidal, Michel; Guillo, Matthieu; Guler, Nevzat; Guo, Lei; Gyurjyan, Vardan; Hadjidakis, Cynthia; Hafidi, Kawtar; Hafnaoui, Khadija; Hakobyan, Hayk; Hakobyan, Rafael; Hanretty, Charles; Hardie, John; Hassall, Neil; Heddle, David; Hersman, F.; Hicks, Kenneth; Hleiqawi, Ishaq; Holtrop, Maurik; Hyde, Charles; Ilieva, Yordanka; Ireland, David; Ishkhanov, Boris; Isupov, Evgeny; Ito, Mark; Jenkins, David; Jo, Hyon-Suk; Johnstone, John; Joo, Kyungseon; Juengst, Henry; Kalantarians, Narbe; Keller, Dustin; Kellie, James; Khandaker, Mahbubul; Kim, Kui; Klein, Andreas; Klein, Andreas; Klimenko, Alexei; Kossov, Mikhail; Krahn, Zebulun; Kramer, Laird; Kubarovsky, Valery; Kuhn, Joachim; Kuhn, Sebastian; Kuleshov, Sergey; Kuznetsov, Viacheslav; Lachniet, Jeff; Laget, Jean; Langheinrich, Jorn; Lawrence, Dave; Lee, T.; Lima, Ana; Livingston, Kenneth; Lu, Haiyun; Lukashin, Konstantin; MacCormick, Marion; Markov, Nikolai; Mattione, Paul; McAleer, Simeon; McKinnon, Bryan; McNabb, John; Mecking, Bernhard; Mehrabyan, Surik; Melone, Joseph; Mestayer, Mac; Meyer, Curtis; Mibe, Tsutomu; Mikhaylov, Konstantin; Minehart, Ralph; Mirazita, Marco; Miskimen, Rory; Mokeev, Viktor; Morand, Ludyvine; Moreno, Brahim; Moriya, Kei; Morrow, Steven; Moteabbed, Maryam; Mueller, James; Munevar Espitia, Edwin; Mutchler, Gordon; Nadel-Turonski, Pawel; Nasseripour, Rakhsha; Niccolai, Silvia; Niculescu, Gabriel; Niculescu, Maria-Ioana; Niczyporuk, Bogdan; Niroula, Megh; Niyazov, Rustam; Nozar, Mina; O'Rielly, Grant; Osipenko, Mikhail; Ostrovidov, Alexander; Park, S.; Pasyuk, Evgueni; Paterson, Craig; Anefalos Pereira, S.; Philips, Sasha; Pierce, Jerome; Pivnyuk, Nikolay; Pocanic, Dinko; Pogorelko, Oleg; Polli, Ermanno; Popa, Iulian; Pozdnyakov, Sergey; Preedom, Barry; Price, John; Prok, Yelena; Protopopescu, Dan; Qin, Liming; Raue, Brian; Riccardi, Gregory; Ricco, Giovanni; Ripani, Marco; Ritchie, Barry; Rosner, Guenther; Rossi, Patrizia; Rowntree, David; Rubin, Philip; Sabatie, Franck; Saini, Mukesh; Salamanca, Julian; Salgado, Carlos; Santoro, Joseph; Sapunenko, Vladimir; Schott, Diane; Schumacher, Reinhard; Serov, Vladimir; Sharabian, Youri; Sharov, Dmitri; Shaw, J.; Shvedunov, Nikolay; Skabelin, Alexander; Smith, Elton; Smith, Lee; Sober, Daniel; Sokhan, Daria; Stavinskiy, Aleksey; Stepanyan, Samuel; Stepanyan, Stepan; Stokes, Burnham

    2008-10-01

    DOI: http://dx.doi.org/10.1103/PhysRevC.78.045209
    The helicity amplitudes of the electroexcitation of the Roper resonance are extracted for 1.7 < Q2 < 4.5 GeV2 from recent high precision JLab-CLAS cross section and longitudinally polarized beam asymmetry data for pi+ electroproduction on protons at W=1.15-1.69 GeV. The analysis is made using two approaches, dispersion relations and a unitary isobar model, which give consistent results. It is found that the transverse helicity amplitude A_{1/2} for the gamma* p -> N(1440)P11 transition, which is large and negative at Q2=0, becomes large and positive at Q2 ~ 2 GeV2, and then drops slowly with Q2. The longitudinal helicity amplitude S_{1/2}, which was previously found from CLAS ep -> eppi0,enpi+ data to be large and positive at Q2=0.4,0.65 GeV2, drops with Q2. Available model predictions for gamma* p -> N(1440)P11 allow us to conclude that these results provide strong evidence in favor of N(1440)P11 as a first radial excitation of

  15. Anti-inflammatory effect of the 5,7,4'-trihydroxy-6-geranylflavanone isolated from the fruit of Artocarpus communis in S100B-induced human monocytes.

    PubMed

    Lin, Jer-An; Fang, Song-Chwan; Wu, Chi-Hao; Huang, Shang-Ming; Yen, Gow-Chin

    2011-01-12

    The fruit of Artocarpus communis Moraceae, a traditional starch crop, is a rich source of phytochemicals, such as flavonoids and their derivatives. The aim of this study was to investigate whether 5,7,4'-trihydroxy-6-geranylflavanone (AC-GF), a geranyl flavonoid derivative isolated from the fruits of A. communis, could decrease the activation of inflammatory mediators induced by S100B (ligand of receptor for advanced glycation end products, RAGE) in THP-1 monocytes. According to the results, low levels of AC-GF (≤2.5 μM) showed a great inhibitory effect on gene expression of RAGE and down-regulated both TNF-α and IL-1β secretion and gene expression (p < 0.05). AC-GF also decreased reactive oxygen species (ROS) production in response to S100B (p < 0.05). Additionally, Western blotting revealed that AC-GF could effectively attenuate RAGE-dependent signaling, including expression of protein kinase C (PKC) and p47phox, phosphorylation of extracellular signal-regulated kinase (ERK) and p38 mitogen-activated protein kinase (MAPK), and particularly NF-κB activation (p < 0.05). In conclusion, this is the first report that AC-GF possesses great antioxidant and anti-inflammatory properties in vitro. This finding may contribute to increased implication and utilization of the fruit of A. communis Moraceae in functional foods.

  16. Discovery and Preclinical Characterization of 3-((4-(4-Chlorophenyl)-7-fluoroquinoline-3-yl)sulfonyl)benzonitrile, a Novel Non-acetylenic Metabotropic Glutamate Receptor 5 (mGluR5) Negative Allosteric Modulator for Psychiatric Indications.

    PubMed

    Galambos, János; Bielik, Attila; Krasavin, Mikhail; Orgován, Zoltán; Domány, György; Nógrádi, Katalin; Wágner, Gábor; Balogh, György T; Béni, Zoltán; Kóti, János; Szakács, Zoltán; Bobok, Amrita; Kolok, Sándor; Mikó-Bakk, Mónika L; Vastag, Mónika; Sághy, Katalin; Laszy, Judit; Halász, Attila Sándor; Balázs, Ottilia; Gál, Krisztina; Greiner, István; Szombathelyi, Zsolt; Keserű, György M

    2017-03-23

    Negative allosteric modulators (NAM) of metabotropic glutamate receptor 5 (mGluR5) have been implicated as a potential pharmacotherapy for a number of psychiatric diseases, including anxiety and depression. Most of the mGluR5 NAM clinical candidates can be characterized by the central acetylenic moiety that connects the terminal pharmacophores. Identification of a sulfoquinoline hit via high throughput screening (HTS) followed by optimization provided a 4-phenyl-3-aryl-sulfoquinoline lead compound with the minimal pharmacophore. Optimization of the core and aryl appendages was performed by scanning and matrix libraries synthesized by the multiple parallel synthesis approach. Biological evaluation of matrix libraries provided a number of potent, metabolically stable, and in vivo active compounds. One of these compounds, 25 showed high efficacy and safety in preclinical in vivo models; this allowed its nomination as a novel, nonacetylenic mGluR5 NAM clinical candidate. Compound 25 was advanced to first-in-man trials for the treatment of psychiatric conditions.

  17. 7 CFR 1779.5-1779.7 - [Reserved

    Code of Federal Regulations, 2010 CFR

    2010-01-01

    ... 7 Agriculture 12 2010-01-01 2010-01-01 false 1779.5-1779.7 Section 1779.5-1779.7 Agriculture Regulations of the Department of Agriculture (Continued) RURAL UTILITIES SERVICE, DEPARTMENT OF AGRICULTURE (CONTINUED) WATER AND WASTE DISPOSAL PROGRAMS GUARANTEED LOANS §§ 1779.5-1779.7...

  18. Cardiotonic agents. 7. Prodrug derivatives of 4-ethyl-1,3-dihydro- 5-[4-(2-methyl-1H-imidazol-1-yl)benzoyl]-2H-imidazol-2-one.

    PubMed

    Shaw, K J; Erhardt, P W; Hagedorn, A A; Pease, C A; Ingebretsen, W R; Wiggins, J R

    1992-04-03

    The cardiotonic agent 4-ethyl-1,3-dihydro-5-4-(2-methyl-1H-imidazol-1-yl)benzoyl]-2H- imidazol-2-one (1) was found to have low bioavailability when administered orally to rats and dogs. A series of N-acyl derivatives, an underutilized prodrug of acidic NH compounds, has been synthesized and tested for their ability to improve the oral bioavailability of 1. Reaction of the monosodium salt of 1 with various anhydrides afforded the N-1 monoacylimidazolones with surprisingly high regioselectivity. In addition to the prodrugs, acylation of 1 with propionic or phenylacetic anhydride led to the novel 3H-pyrrolo[1,2-c]imidazole-3,5(2H)-diones 6. The prodrugs showed a significant increase in the partition coefficients with a minor decrease in the aqueous solubility. The benzoyl derivative 4b exhibited the highest stability in both pH 1.5 and 7.4 buffer solutions. Further evaluation of 4b showed rapid conversion to 1 in canine plasma (t1/2 = 38 min), and human plasma (t1/2 = 10 min). Oral studies indicated that the bioavailability of 4b was increased to greater than 75% (compared to less than 20% for 1), and hemodynamic studies demonstrated that the selective inotropic profile of 1 was retained.

  19. [μ-2,8-Dimethyl-1,4,5,6,7,10,11,12-octa­hydro­diimidazo[4,5-h;4′,5′-c][1,6]diaze­cine-5,11-diacetato]bis­[diaqua­nitrato­copper(II)] trihydrate

    PubMed Central

    Luna-Ramírez, Karen S.; Bernès, Sylvain; Gasque, Laura

    2008-01-01

    The title compound, [Cu2(C16H20N6O4)(NO3)2(H2O)4]·3H2O, crystallizes with two dinuclear CuII complex mol­ecules, each lying on an inversion center, and six solvent water mol­ecules per unit cell. The central 1,6-diazecine ring adopts the common chair conformation invariably found in the family of complexes bearing such ligands. The CuII atoms have an octa­hedral geometry, with a very strong tetra­gonal distortion due to the Jahn–Teller effect. Axial sites are occupied by a nitrate ion and a water mol­ecule. The Cu⋯Cu separations [7.3580 (9) and 7.3341 (9) Å] are compatible with a potential catecholase activity. Neighboring mol­ecules in the crystal structure are connected via O—H⋯O hydrogen bonds formed by water mol­ecules and carboxyl­ate O atoms. N—H⋯O hydrogen bonds are also present. PMID:21201593

  20. Physiological Concentrations of Choline Activate Native α7-Containing Nicotinic Acetylcholine Receptors in the Presence of PNU-120596 [1-(5-Chloro-2,4-dimethoxyphenyl)-3-(5-methylisoxazol-3-yl)-urea

    PubMed Central

    Gusev, Alexander G.

    2010-01-01

    The use of PNU-120596 [1-(5-chloro-2,4-dimethoxyphenyl)-3-(5-methylisoxazol-3-yl)-urea], a positive allosteric modulator of α7 nicotinic acetylcholine receptor (nAChR), may be beneficial for enhancing cholinergic therapies. However, the effects of PNU-120596 on activation of native α7-containing nAChRs by physiological concentrations of choline are not known and were investigated in this study using patch-clamp electrophysiology and histaminergic tuberomammillary neurons in hypothalamic slices. In the presence of PNU-120596, subthreshold (i.e., inactive) physiological concentrations of choline (∼10 μM) elicited repetitive step-like whole-cell responses reminiscent of single ion channel openings that were reversibly blocked by 20 nM methyllycaconitine, a selective α7 nAChR antagonist. The effects of choline and PNU-120596 were synergistic as administration of 10 to 40 μM choline or 1 to 4 μM PNU-120596 alone did not elicit responses. In voltage clamp at −60 mV, the persistent activation of α7-containing nAChRs by 10 μM choline plus 1 μM PNU-120596 was estimated to produce a sustained influx of Ca2+ ions at a rate of 8.4 pC/min (∼0.14 pA). In the presence of PNU-120596 in current clamp, transient step-like depolarizations (∼5 mV) enhanced neuronal excitability and triggered voltage-gated conductances; a single opening of an α7-containing nAChR channel appeared to transiently depolarize the entire neuron and facilitate spontaneous firing. Therefore, this study tested and confirmed the hypothesis that PNU-120596 enhances the effects of subthreshold concentrations of choline on native α7-containing nAChRs, allowing physiological levels of choline to activate these receptors and produce whole-cell responses in the absence of exogenous nicotinic agents. In certain neurological disorders, this activation may be therapeutically beneficial, more efficacious, and safer than treatments with nAChR agonists. PMID:19923442

  1. 2,4,5-Trichlorophenol

    Integrated Risk Information System (IRIS)

    2,4,5 - Trichlorophenol ; CASRN 95 - 95 - 4 Human health assessment information on a chemical substance is included in the IRIS database only after a comprehensive review of toxicity data , as outlined in the IRIS assessment development process . Sections I ( Health Hazard Assessments for Noncarcino

  2. Synthesis of novel 7-substituted pyrido[2',3':4,5]furo[3,2-d]pyrimidin-4-amines and their N-aryl analogues and evaluation of their inhibitory activity against Ser/Thr kinases.

    PubMed

    Deau, Emmanuel; Loidreau, Yvonnick; Marchand, Pascal; Nourrisson, Marie-Renée; Loaëc, Nadège; Meijer, Laurent; Levacher, Vincent; Besson, Thierry

    2013-12-15

    The efficient synthesis of 7-substituted pyrido[2',3':4,5]furo[3,2-d]pyrimidin-4-amines and their N-aryl analogues is described. 3,5-Dibromopyridine was converted into 3-amino-6-bromofuro[3,2-b]pyridine-2-carbonitrile intermediate which was formylated with DMFDMA. Functionalization at position 7 of the tricyclic scaffold was accomplished, before or after cyclisation step, by palladium-catalyzed Suzuki-Miyaura cross-coupling while the pyrimidin-4-amines and N-aryl counterparts were synthesized by microwave-assisted formamide degradation and Dimroth rearrangement, respectively. The final products were evaluated for their potent inhibition of a series of five Ser/Thr kinases (CDK5/p25, CK1δ/ε, CLK1, DYRK1A, GSK3α/β). Compound 35 showed the best inhibitory activity with an IC50 value of 49 nM and proved to be specific to CLK1 among the panel of tested kinases.

  3. Crystal structure of ethyl 2-[9-(5-bromo-2-hy-droxy-phen-yl)-1,8-dioxo-1,2,3,4,5,6,7,8,9,10-deca-hydro-acridin-10-yl]acetate.

    PubMed

    Mohamed, Shaaban K; Akkurt, Mehmet; Jasinski, Jerry P; Abdelhamid, Antar A; Tamam, Asmaa H; Albayati, Mustafa R

    2015-12-01

    In the title compound, C23H24BrNO5, the central 1,4-di-hydro-pyridine ring of the 1,2,3,4,5,6,7,8,9,10-deca-hydro-acridine ring system adopts a half-chair conformation. The two cyclo-hexene rings fused to the central ring both have a twisted-boat conformation. The mean planes of the bromo-hydroxy-phenyl ring and the major and minor components of the disordered ethyl amino-acetate moiety make dihedral angles of 78.99 (12), 85.9 (2) and 88.3 (9)°, respectively, with the 1,4-di-hydro-pyridine ring. The terminal ethyl group of the ethyl amino-acetate moiety is disordered over two sets of sites with refined occupancies of 0.768 (17) and 0.232 (17). The mol-ecular conformation is stabilized by an intra-molecular O-H⋯O hydrogen bond, forming an S(8) ring motif. In the crystal, C-H⋯O hydrogen bonds connect the mol-ecules into layers parallel to (001), enclosing R 1 (2)(7) ring motifs.

  4. 2,6-Bis[(S)-1-phenyl­eth­yl]-1H,5H-pyrrolo­[3,4-f]isoindole-1,3,5,7(2H,6H)-tetrone

    PubMed Central

    Abdel-Aziz, Alaa A.-M.; El-Azab, Adel S.; Alanazi, Amer M.; Ng, Seik Weng; Tiekink, Edward R. T.

    2012-01-01

    In the title compound, C26H20N2O4, the central isoindole core is almost planar (r.m.s. deviation = 0.043 Å). The phenyl rings lie to either side of the plane [dihedral angles = 88.64 (5) and 67.74 (6)°] and the dihedral angle between the phenyl rings is 63.39 (7)°. In the crystal, mol­ecules are linked by C—H⋯O inter­actions; notably, one carbonyl O atom accepts three such bonds. PMID:22412753

  5. 9-Furfuryl-idene-2,3-dimethyl-6,7,8,9-tetrahydro-4H--thieno[2',3':4,5]pyrimidino[1,2-a]pyridin-4-one.

    PubMed

    Bozorov, Khurshed A; Elmuradov, Burkhon Zh; Okmanov, Rasul Ya; Tashkhodjaev, Bakhodir; Shakhidoyatov, Khusnutdin M

    2010-02-06

    The title compound, C(17)H(16)N(2)O(2)S, was obtained by condensation of 2,3-dimethyl-thieno[2',3':4,5]pyrimidino[1,2-a]pyridin-4-one with furfural in the presence of sodium hydroxide. One of the methyl-ene groups of the tetra-hydro-pyrido ring is disordered over two positions in a 0.87 (1):0.13 (1) ratio. The thieno[2,3-d]pyrimidin-4-one unit and the furan ring are both planar (r.m.s. deviation = 0.535 Å), and coplanar with each other, forming a dihedral angle of 5.4 (1)°. Four weak inter-molecular hydrogen bonds (C-H⋯O and C-H⋯N) are observed in the structure, which join mol-ecules into a network parallel to (101).

  6. Crystal structure and solvent-dependent behaviours of 3-amino-1,6-diethyl-2,5,7-trimethyl-4,4-di­phenyl-3a,4a-di­aza-4-bora-s-indacene

    PubMed Central

    Yang, Lijing; Drew, Brett; Yalagala, Ravi Shekar; Chaviwala, Rameez; Simionescu, Razvan; Lough, Alan J.; Yan, Hongbin

    2017-01-01

    In the title compound (3-amino-4,4-diphenyl-BODIPY), C28H32BN3, the central six-membered ring has a flattened sofa conformation, with one of the N atoms deviating by 0.142 (4) Å from the mean plane of the other five atoms, which have an r.m.s. deviation of 0.015 Å. The dihedral angle between the two essentially planar outer five-membered rings is 8.0 (2)°. In the crystal, mol­ecules are linked via weak N—H⋯π inter­actions, forming chains along [010]. The com­pound displays solvent-dependent behaviours in both NMR and fluorescence spectroscopy. In the 1H NMR spectra, the aliphatic resonance signals virtually coalesce in solvents such as chloro­form, di­chloro­methane and di­bromo­ethane; however, they are fully resolved in solvents such as dimethyl sulfoxide (DMSO), methanol and toluene. The excitation and fluorescence intensities in chloro­form decreased significantly over time, while in DMSO the decrease is not so profound. In toluene, the excitation and fluorescent intensities are not time-dependent. This behaviour is presumably attributed to the assembly of 3-amino-4,4-diphenyl-BODIPY in solution that leads to the formation of noncovalent structures, while in polar or aromatic solvents, the formation of these assemblies is disrupted, leading to resolution of signals in the NMR spectra. PMID:28316814

  7. Reactions of 1,3-Dibromo-1,1-difluoro Compounds with 1,8-Diazabicyclo[5.4.0]undec-7-ene.

    PubMed

    Elsheimer, Seth; Foti, Christopher J.; Bartberger, Michael D.

    1996-09-06

    Difluorodienes result from the double dehydrobromination of 4-aryl-1,3-dibromo-1,1-difluorobutanes with DBU. Attempted syntheses of analogous 4-alkyl or 4-alkoxy dienes yield monoelimination products under mild conditions and unexpected trifluoro compounds under more vigorous conditions. 4-Aryl-1,1-difluoro-1,3-butadienes react rapidly with 4-phenyl-1,2,4-triazoline-3,5-dione in Diels-Alder reactions, but these dienes are unreactive toward several other electron-deficient and electron-rich dienophiles.

  8. DFT investigation of the mecahanism and stereochemistry of electrophilic transannular addition reaction of bromine to tricyclo[4.2.2.02,5]deca-3,7-diene.

    PubMed

    Abbasoglu, Rza; Misir, Miraç Nedim

    2012-03-01

    Full geometric optimization of tricyclo[4.2.2.02,5]deca-3,7-diene (TDD) has been done by DFT/B3LYP methods and the structure of the molecule was investigated. Cyclobuten double bond (I) of molecule is syn pyramidalized, and bicyclookten double bond (II) is also exo pyramidalized. The double bond (I) is more pyramidalized than the double bond (II) and it has higher reactivity. The TDD-Br2 system has been investigated by B3LYP/6-311++G(d,p) method and their stable configurations have been determined. The cationic intermediates and products obtained as a result of the addition reaction has been studied using B3LYP/6-311G(d,p) and B3LYP/6-311++G(d,p) methods. Bridged bromonium cation is more stable than U-type cation. Considering that the bridged cation does not isomerize to the less stable U-type cation, it is not possible for the U-type product to be obtained in the reaction. The bridged bromonium cation transformed into the more stable N-type cation and the N-type product was obtained via this cation. The thermodynamic stability of the anti, exo and anti, endo isomers of N-type dibromide molecule were almost identical. N-type product is 11.759 kcal mol more stable than U-type product.

  9. 3',5-dihydroxy-3,4',7-trimethoxyflavone-induces ER-stress-associated HCT-116 programmed cell death via redox signaling.

    PubMed

    Singh, Mahendra Pal; Han, Jaehong; Kang, Sun Chul

    2017-04-01

    Quercetin, a well cognized bioactive flavone possessing great medicinal value, has limited usage. The rapid gastrointestinal digestion of quercetin is also a major obstacle for its clinical implementation due to low bioavailability and poor aqueous solubility. 3',5-dihydroxy-3,4',7-trimethoxyflavone (DTMF), a novel semi-synthetic derivative of quercetin, is known to modulate several biological activities. Therefore, in the present study we examined the cytotoxic mechanism of DTMF in concentration-dependent manner (25, 50, and 100μM; 24h) against HCT-116 human colon carcinoma cells. The cytotoxic potential of DTMF was characterized based on deformed cell morphology, increased ROS accumulation, loss of mitochondrial membrane potential (ΔѰm), increased mitochondrial mass, chromatin condensation, and typical DNA-fragmentation in HCT-116 cells. The results showed that DTMF-induced enhanced ROS production at higher concentration (100μM) as evidenced by upregulated expression of ER stress and apoptotic proteins with concomitant increase in PERK, CHOP, and JNK levels, when compared to N-acetyl cysteine (NAC, ROS inhibitor) treated HCT-116 cells, which depicts that DTMF might act as a crucial mediator of apoptosis signaling. Collectively, our results suggest that DTMF stimulates ROS-mediated oxidative stress, which in turn induces PERK-CHOP and JNK pathway of apoptosis to promote HCT-116 cell death.

  10. Binuclear complexes of bis-chelating ligands based on [1,4]dioxocino[6,5-b:7,8-b']dipyridine moieties.

    PubMed

    Casalino, Marcello; De Felice, Vincenzo; Fraldi, Natascia; Panunzi, Achille; Ruffo, Francesco

    2009-07-06

    Ligands based on a [1,4]dioxocino[6,5-b:7,8-b']dipyridine (doxpy) core were prepared and characterized. They all present two equal chelating moieties each one including one N, O, or S donor in addition to a pyridinic nitrogen. These ligands displayed high selectivity for the formation of binuclear complexes. At least one d(8) ion (Pd(II) or Pt(II)) complex was prepared for each type of ligand. The stereochemical behavior of the ligands is discussed on the basis of NMR spectra. Stable atropoisomers were obtained in the case of N-oxides or in case chiral centers were introduced in the ethereal bridge. As for the complexes, stable enantiomers appear to be in principle attainable for all the new compounds. A test on the cooperative ability of two Pd(II) centers has been grounded on the microstructure of the styrene/CO copolymer catalytically produced by a binuclear pyridine-imino complex. In fact, comparison with the microstructure of the copolymers produced by related single-site mono- and (open-chain) binuclear catalysts reveals significant difference, thus giving indication of possible synergic metal activity.

  11. Flavor unity in SU(7): Low-mass magnetic monopole, doubly charged lepton,and Q = 5/3,-4/3 quarks

    SciTech Connect

    Kim, J.E.

    1981-06-01

    A specific flavor unification is suggested in the SU(7) gauge group. This model can be trivially extended to O(14). A global symmetry GAMMA forbids mixings of the b (Q = -1/3) quark with the d and s quarks, and of the t (Q = 2/3) quark with the u and c quarks. Since the b and t quarks carry different GAMMA quantum numbers, they do not belong to the same SU(2)/sub L/ doublet. A mechanism for the GAMMA-symmetry violation is suggested, which allows c-t mixing without b-quark mixing. There are unconventionally charged light (masses < or approx. =300 GeV) fermions: a doubly charged lepton T/sup - -/, a Q = -4/3 quark x, and a Q = 5/3 quark y. The bare value of the Weinberg angle sin/sup 2/theta/sup 0//sub W/ = 3/20 is renormalized to the low-energy value by introducing an intermediate mass scale M/sub 1/. A topologically stable magnetic monopole is light (massroughly-equalM/sub 1//..cap alpha..) and hence there does not exist a conflict arising from the grand unified theories and the hot-big-bang cosmology.

  12. Synthesis and Structural Investigation of a New Manganese-Antimony Oxoethoxide, Mn 7Sb 4( μ5-O) 2( μ4-O) 2( μ3-OEt) 2( μ-OEt) 16(HOEt) 2

    NASA Astrophysics Data System (ADS)

    Bemm, U.; Norrestam, R.; Nygren, M.; Westin, G.

    1997-12-01

    A new manganese-antimony oxoethoxide with the formula Mn 7Sb 4O 4(OEt) 18(HOEt) 2has been prepared and characterized by single-crystal X-ray diffraction and FT-IR techniques. The structure of the compound has the noncentrosymmetric tetragonal space group symmetry P4 2(No. 77) with unit-cell parameters a=15.164(3), c=14.729(5) Å, V=3387(2) Å 3, Z=2, and Dx=1.803(1) g cm -1Fw=1838.8 g mol -1. The crystal structure has been refined against the 2227 most significant reflections to an Rvalue of 0.059 ( Rw=0.077). The single-crystal X-ray diffraction intensities were collected at 170(1) K using MoK αradiation. The structure analysis shows that the structure consists of roughly spherically shaped molecules of C2symmetry and of composition Mn 7Sb 4O 4(OEt) 18(HOEt) 2. The antimony atoms are five-coordinated by oxygen atoms, while four of the manganese atoms are five-coordinated and three are six-coordinated. The antimony atoms are located in the outer regions of the molecule and the antimony lone pair regions are pointing away from the molecule. Four oxooxygens are located in the core of the molecule. The ethanol molecules coordinating the antimony atoms are involved in short intramolecular hydrogen bonds. A TLS analysis of the rigid-body motion of the central metal-oxygen core structure shows that two oxygen atoms involved in the intramolecular hydrogen bond do not follow the pattern of the rest of the atoms. The agreement between observed and predicted parameters of the remaining atoms supports the assumed rigidity in the central metal and oxygen core fragment. Structural relationships are found to other spherically shaped alkoxides such as Mn 8Sb 4O 4(OEt) 20and Pb 6Nb 4O 4(OEt) 24.

  13. Measurement of elliptic flow of light nuclei at sNN=200 , 62.4, 39, 27, 19.6, 11.5, and 7.7 GeV at the BNL Relativistic Heavy Ion Collider

    DOE PAGES

    Adamczyk, L.; Adkins, J. K.; Agakishiev, G.; ...

    2016-09-23

    Here we present measurements of second-order azimuthal anisotropy ( v2 ) at midrapidity ( |y| < 1.0 ) for light nuclei d , t , 3He (formore » $$\\sqrt{s}$$$_{NN}$$ = 200 , 62.4, 39, 27, 19.6, 11.5, and 7.7 GeV) and antinuclei$$\\bar{d}$$ ( $$\\sqrt{s}$$$_{NN}$$ = 200 , 62.4, 39, 27, and 19.6 GeV) and 3 ¯¯¯¯¯ He ( $$\\sqrt{s}$$$_{NN}$$ = 200 GeV) in the STAR (Solenoidal Tracker at RHIC) experiment. The v2 for these light nuclei produced in heavy-ion collisions is compared with those for p and $$\\bar{p}$$. We observe mass ordering in nuclei v2 ( pT) at low transverse momenta ( pT < 2.0 GeV/c). We also find a centrality dependence of v2 for d and $$\\bar{d}$$ . The magnitude of v2 for t and 3He agree within statistical errors. Light-nuclei v2 are compared with predictions from a blast-wave model. Atomic mass number ( A ) scaling of light-nuclei v2 (pT) seems to hold for pT / A < 1.5 GeV/c . Results on light-nuclei v2 from a transport-plus-coalescence model are consistent with the experimental measurements.« less

  14. Measurement of elliptic flow of light nuclei at √{sN N}=200 , 62.4, 39, 27, 19.6, 11.5, and 7.7 GeV at the BNL Relativistic Heavy Ion Collider

    NASA Astrophysics Data System (ADS)

    Adamczyk, L.; Adkins, J. K.; Agakishiev, G.; Aggarwal, M. M.; Ahammed, Z.; Alekseev, I.; Aparin, A.; Arkhipkin, D.; Aschenauer, E. C.; Attri, A.; Averichev, G. S.; Bai, X.; Bairathi, V.; Bellwied, R.; Bhasin, A.; Bhati, A. K.; Bhattarai, P.; Bielcik, J.; Bielcikova, J.; Bland, L. C.; Bordyuzhin, I. G.; Bouchet, J.; Brandenburg, J. D.; Brandin, A. V.; Bunzarov, I.; Butterworth, J.; Caines, H.; Calderón de la Barca Sánchez, M.; Campbell, J. M.; Cebra, D.; Chakaberia, I.; Chaloupka, P.; Chang, Z.; Chatterjee, A.; Chattopadhyay, S.; Chen, J. H.; Chen, X.; Cheng, J.; Cherney, M.; Christie, W.; Contin, G.; Crawford, H. J.; Das, S.; De Silva, L. C.; Debbe, R. R.; Dedovich, T. G.; Deng, J.; Derevschikov, A. A.; di Ruzza, B.; Didenko, L.; Dilks, C.; Dong, X.; Drachenberg, J. L.; Draper, J. E.; Du, C. M.; Dunkelberger, L. E.; Dunlop, J. C.; Efimov, L. G.; Engelage, J.; Eppley, G.; Esha, R.; Evdokimov, O.; Eyser, O.; Fatemi, R.; Fazio, S.; Federic, P.; Fedorisin, J.; Feng, Z.; Filip, P.; Fisyak, Y.; Flores, C. E.; Fulek, L.; Gagliardi, C. A.; Garand, D.; Geurts, F.; Gibson, A.; Girard, M.; Greiner, L.; Grosnick, D.; Gunarathne, D. S.; Guo, Y.; Gupta, S.; Gupta, A.; Guryn, W.; Hamad, A. I.; Hamed, A.; Haque, R.; Harris, J. W.; He, L.; Heppelmann, S.; Heppelmann, S.; Hirsch, A.; Hoffmann, G. W.; Horvat, S.; Huang, T.; Huang, X.; Huang, B.; Huang, H. Z.; Huck, P.; Humanic, T. J.; Igo, G.; Jacobs, W. W.; Jang, H.; Jentsch, A.; Jia, J.; Jiang, K.; Judd, E. G.; Kabana, S.; Kalinkin, D.; Kang, K.; Kauder, K.; Ke, H. W.; Keane, D.; Kechechyan, A.; Khan, Z. H.; Kikoła, D. P.; Kisel, I.; Kisiel, A.; Kochenda, L.; Koetke, D. D.; Kosarzewski, L. K.; Kraishan, A. F.; Kravtsov, P.; Krueger, K.; Kumar, L.; Lamont, M. A. C.; Landgraf, J. M.; Landry, K. D.; Lauret, J.; Lebedev, A.; Lednicky, R.; Lee, J. H.; Li, X.; Li, C.; Li, X.; Li, Y.; Li, W.; Lin, T.; Lisa, M. A.; Liu, F.; Ljubicic, T.; Llope, W. J.; Lomnitz, M.; Longacre, R. S.; Luo, X.; Ma, R.; Ma, G. L.; Ma, Y. G.; Ma, L.; Magdy, N.; Majka, R.; Manion, A.; Margetis, S.; Markert, C.; Matis, H. S.; McDonald, D.; McKinzie, S.; Meehan, K.; Mei, J. C.; Minaev, N. G.; Mioduszewski, S.; Mishra, D.; Mohanty, B.; Mondal, M. M.; Morozov, D. A.; Mustafa, M. K.; Nandi, B. K.; Nasim, Md.; Nayak, T. K.; Nigmatkulov, G.; Niida, T.; Nogach, L. V.; Noh, S. Y.; Novak, J.; Nurushev, S. B.; Odyniec, G.; Ogawa, A.; Oh, K.; Okorokov, V. A.; Olvitt, D.; Page, B. S.; Pak, R.; Pan, Y. X.; Pandit, Y.; Panebratsev, Y.; Pawlik, B.; Pei, H.; Perkins, C.; Pile, P.; Pluta, J.; Poniatowska, K.; Porter, J.; Posik, M.; Poskanzer, A. M.; Pruthi, N. K.; Putschke, J.; Qiu, H.; Quintero, A.; Ramachandran, S.; Raniwala, R.; Raniwala, S.; Ray, R. L.; Ritter, H. G.; Roberts, J. B.; Rogachevskiy, O. V.; Romero, J. L.; Ruan, L.; Rusnak, J.; Rusnakova, O.; Sahoo, N. R.; Sahu, P. K.; Sakrejda, I.; Salur, S.; Sandweiss, J.; Sarkar, A.; Schambach, J.; Scharenberg, R. P.; Schmah, A. M.; Schmidke, W. B.; Schmitz, N.; Seger, J.; Seyboth, P.; Shah, N.; Shahaliev, E.; Shanmuganathan, P. V.; Shao, M.; Sharma, M. K.; Sharma, B.; Shen, W. Q.; Shi, Z.; Shi, S. S.; Shou, Q. Y.; Sichtermann, E. P.; Sikora, R.; Simko, M.; Singha, S.; Skoby, M. J.; Smirnov, N.; Smirnov, D.; Solyst, W.; Song, L.; Sorensen, P.; Spinka, H. M.; Srivastava, B.; Stanislaus, T. D. S.; Stepanov, M.; Stock, R.; Strikhanov, M.; Stringfellow, B.; Sumbera, M.; Summa, B.; Sun, X. M.; Sun, Z.; Sun, Y.; Surrow, B.; Svirida, D. N.; Tang, Z.; Tang, A. H.; Tarnowsky, T.; Tawfik, A.; Thäder, J.; Thomas, J. H.; Timmins, A. R.; Tlusty, D.; Todoroki, T.; Tokarev, M.; Trentalange, S.; Tribble, R. E.; Tribedy, P.; Tripathy, S. K.; Tsai, O. D.; Ullrich, T.; Underwood, D. G.; Upsal, I.; Van Buren, G.; van Nieuwenhuizen, G.; Vandenbroucke, M.; Varma, R.; Vasiliev, A. N.; Vertesi, R.; Videbæk, F.; Vokal, S.; Voloshin, S. A.; Vossen, A.; Wang, Y.; Wang, G.; Wang, J. S.; Wang, H.; Wang, Y.; Wang, F.; Webb, G.; Webb, J. C.; Wen, L.; Westfall, G. D.; Wieman, H.; Wissink, S. W.; Witt, R.; Wu, Y.; Xiao, Z. G.; Xie, W.; Xie, G.; Xin, K.; Xu, H.; Xu, Z.; Xu, J.; Xu, Y. F.; Xu, Q. H.; Xu, N.; Yang, Y.; Yang, S.; Yang, C.; Yang, Y.; Yang, Y.; Yang, Q.; Ye, Z.; Ye, Z.; Yepes, P.; Yi, L.; Yip, K.; Yoo, I.-K.; Yu, N.; Zbroszczyk, H.; Zha, W.; Zhang, J.; Zhang, Y.; Zhang, X. P.; Zhang, Z.; Zhang, J. B.; Zhang, S.; Zhang, S.; Zhang, J.; Zhao, J.; Zhong, C.; Zhou, L.; Zhu, X.; Zoulkarneeva, Y.; Zyzak, M.; STAR Collaboration

    2016-09-01

    We present measurements of second-order azimuthal anisotropy (v2) at midrapidity (|y |<1.0 ) for light nuclei d ,t ,3He (for √{sN N}=200 , 62.4, 39, 27, 19.6, 11.5, and 7.7 GeV) and antinuclei d ¯ (√{sN N}=200 , 62.4, 39, 27, and 19.6 GeV) and ¯3He (√{sN N}=200 GeV) in the STAR (Solenoidal Tracker at RHIC) experiment. The v2 for these light nuclei produced in heavy-ion collisions is compared with those for p and p ¯. We observe mass ordering in nuclei v2(pT) at low transverse momenta (pT<2.0 GeV/c ). We also find a centrality dependence of v2 for d and d ¯. The magnitude of v2 for t and 3He agree within statistical errors. Light-nuclei v2 are compared with predictions from a blast-wave model. Atomic mass number (A ) scaling of light-nuclei v2(pT) seems to hold for pT/A <1.5 GeV /c . Results on light-nuclei v2 from a transport-plus-coalescence model are consistent with the experimental measurements.

  15. 18 CFR 5.7 - Tribal consultation.

    Code of Federal Regulations, 2014 CFR

    2014-04-01

    ....7 Section 5.7 Conservation of Power and Water Resources FEDERAL ENERGY REGULATORY COMMISSION, DEPARTMENT OF ENERGY REGULATIONS UNDER THE FEDERAL POWER ACT INTEGRATED LICENSE APPLICATION PROCESS § 5.7... of intent required by § 5.5 between each Indian tribe likely to be affected by the potential...

  16. 18 CFR 5.7 - Tribal consultation.

    Code of Federal Regulations, 2011 CFR

    2011-04-01

    ....7 Section 5.7 Conservation of Power and Water Resources FEDERAL ENERGY REGULATORY COMMISSION, DEPARTMENT OF ENERGY REGULATIONS UNDER THE FEDERAL POWER ACT INTEGRATED LICENSE APPLICATION PROCESS § 5.7... of intent required by § 5.5 between each Indian tribe likely to be affected by the potential...

  17. MF498 [N-{[4-(5,9-Diethoxy-6-oxo-6,8-dihydro-7H-pyrrolo[3,4-g]quinolin-7-yl)-3-methylbenzyl]sulfonyl}-2-(2-methoxyphenyl)acetamide], a selective E prostanoid receptor 4 antagonist, relieves joint inflammation and pain in rodent models of rheumatoid and osteoarthritis.

    PubMed

    Clark, Patsy; Rowland, Steven E; Denis, Danielle; Mathieu, Marie-Claude; Stocco, Rino; Poirier, Hugo; Burch, Jason; Han, Yongxin; Audoly, Laurent; Therien, Alex G; Xu, Daigen

    2008-05-01

    Previous evidence has implicated E prostanoid receptor 4 (EP4) in mechanical hyperalgesia induced by subplantar inflammation. However, its role in chronic arthritis remains to be further defined because previous attempts have generated two conflicting lines of evidence, with one showing a marked reduction of arthritis induced by a collagen antibody in mice lacking EP4, but not EP1-EP3, and the other showing no impact of EP4 antagonism on arthritis induced by collagen. Here, we assessed the effect of a novel and selective EP4 antagonist MF498 [N-{[4-(5,9-diethoxy-6-oxo-6,8-dihydro-7H-pyrrolo[3,4-g]quinolin-7-yl)-3-methylbenzyl]sulfonyl}-2-(2-methoxyphenyl)acetamide] on inflammation in adjuvant-induced arthritis (AIA), a rat model for rheumatoid arthritis (RA), and joint pain in a guinea pig model of iodoacetate-induced osteoarthritis (OA). In the AIA model, MF498, but not the antagonist for EP1, MF266-1 [1-(5-{3-[2-(benzyloxy)-5-chlorophenyl]-2-thienyl}pyridin-3-yl)-2,2,2-trifluoroethane-1,1-diol] or EP3 MF266-3 [(2E)-N-[(5-bromo-2-methoxyphenyl)sulfonyl]-3-[5-chloro-2-(2-naphthylmethyl)phenyl]acrylamide], inhibited inflammation, with a similar efficacy as a selective cyclooxygenase 2 (COX-2) inhibitor MF-tricyclic. In addition, MF498 was as effective as an nonsteroidal anti-inflammatory drug, diclofenac, or a selective microsomal prostaglandin E synthase-1 inhibitor, MF63 [2-(6-chloro-1H-phenanthro[9,10-d]imidazol-2-yl)isophthalonitrile], in relieving OA-like pain in guinea pigs. When tested in rat models of gastrointestinal toxicity, the EP4 antagonist was well tolerated, causing no mucosal leakage or erosions. Lastly, we evaluated the renal effect of MF498 in a furosemide-induced diuresis model and demonstrated that the compound displayed a similar renal effect as MF-tricyclic [3-(3,4-difluorophenyl)-4-(4-(methylsulfonyl)phenyl)-2-(5H)-furanone], reducing furosemide-induced natriuresis by approximately 50%. These results not only suggest that EP4 is the major EP

  18. 7 CFR 7.4 - Selection of committee members.

    Code of Federal Regulations, 2010 CFR

    2010-01-01

    ... 7 Agriculture 1 2010-01-01 2010-01-01 false Selection of committee members. 7.4 Section 7.4... CONSERVATION STATE, COUNTY AND COMMUNITY COMMITTEES § 7.4 Selection of committee members. State committee... community committee members shall be elected in accordance with § 7.9 of this part....

  19. (2R*,4R*,7S*,10R*,12R*)-3,11,13,15-Tetra-oxa-penta-cyclo-[5.5.3.0(1,7).0(2,4).0(10,12)]penta-deca-5,8-dien-14-one.

    PubMed

    Mehta, Goverdhan; Sen, Saikat; Kumar, C S Ananda

    2013-01-01

    The title compound, C11H8O5, features a 'skipped' diene, an anti-bis-(epoxide) and a cyclic carbonate, all embedded in a densely functionalized [4.4.3]propellane scaffold. The crystal packing of this diepoxide is effected primarily by C-H⋯O hydrogen bonds, which link the mol-ecules into tapes along the b axis. Inter-tape connectivity is brought about by centrosymmetrically disposed pairs of C⋯O contacts [3.183 (4) Å] between the C(δ+)=O(δ-) dipoles of neighbouring carbonate moieties.

  20. Na8Au9.8(4)Ga7.2 and Na17Au5.87(2)Ga46.63: The diversity of pseudo 5-fold symmetries in the Na-Au-Ga system

    NASA Astrophysics Data System (ADS)

    Smetana, Volodymyr; Corbett, John D.; Miller, Gordon J.

    2013-11-01

    The Na-rich part (~30% Na) of the Na-Au-Ga system between NaAu2, NaGa4, and Na22Ga39 has been found to contain the ternary phases Na8Au9.8(4)Ga7.2 (I) and Na17Au5.87(2)Ga46.63 (II), according to the results of single crystal X-ray diffraction measurements. I is orthorhombic, Cmcm, a=5.3040(1), b=24.519(5), c=14.573(3) Å, and contains a network of clusters with local 5-fold symmetry along the a-axis. Such clusters are frequent building units in decagonal quasicrystals and their approximants. II is rhombohedral, R3¯m, a=16.325(2), c=35.242(7) Å, and contains building blocks that are structurally identical to the Bergman-type clusters as well as fused icosahedral units known with active metals, triels and late transition elements. II also contains a polycationic network with elements of the clathrate V type structure. Tight-binding electronic structure calculations using linear muffin-tin-orbital (LMTO) methods on idealized models of I and II indicate that both compounds are metallic with evident pseudogaps at the corresponding Fermi levels. The overall Hamilton bond populations are generally dominated by Au-Ga and Au-Au bonds in I and by Ga-Ga bonds in II; moreover, the Na-Au and Na-Ga contributions in I are unexpectedly large, ~20% of the total. A similar involvement of sodium in covalent bonding has also been found in the electron-richer i-Na13Au12Ga15 quasicrystal approximant.

  1. Design and Synthesis of a New Series of 4-Heteroarylamino-1'-azaspiro[oxazole-5,3'-bicyclo[2.2.2]octanes as α7 Nicotinic Receptor Agonists. 1. Development of Pharmacophore and Early Structure-Activity Relationship.

    PubMed

    Cook, James; Zusi, F Christopher; McDonald, Ivar M; King, Dalton; Hill, Matthew D; Iwuagwu, Christiana; Mate, Robert A; Fang, Haiquan; Zhao, Rulin; Wang, Bei; Cutrone, Jingfang; Ma, Baoqing; Gao, Qi; Knox, Ronald J; Matchett, Michele; Gallagher, Lizbeth; Ferrante, Meredith; Post-Munson, Debra; Molski, Thaddeus; Easton, Amy; Miller, Regina; Jones, Kelli; Digavalli, Siva; Healy, Francine; Lentz, Kimberley; Benitex, Yulia; Clarke, Wendy; Natale, Joanne; Siuciak, Judith A; Lodge, Nicholas; Zaczek, Robert; Denton, Rex; Morgan, Daniel; Bristow, Linda J; Macor, John E; Olson, Richard E

    2016-12-22

    The design and synthesis of a series of quinuclidine-containing spirooxazolidines ("spiroimidates") and their utility as α7 nicotinic acetylcholine receptor partial agonists are described. Selected members of the series demonstrated excellent selectivity for α7 over the highly homologous 5-HT3A receptor. Modification of the N-spiroimidate heterocycle substituent led to (1S,2R,4S)-N-isoquinolin-3-yl)-4'H-4-azaspiro[bicyclo[2.2.2]octane-2,5'oxazol]-2'-amine (BMS-902483), a potent α7 partial agonist, which improved cognition in preclinical rodent models.

  2. Cobalt(I), -(II), and -(III) complexes of a tetraaza 14-membered macrocycle, 5,7,7,12,14,14-hexamethyl-1,4,8,11-tetraazacyclotetradeca-4,11-diene (L). Crystal and molecular structures of (CoL(CO))ClO sub 4 , trans-CoLCl sub 2 , and cis-(CoL(CO sub 3 ))ClO sub 4

    SciTech Connect

    Szalda, D.J.; Fujita, E.; Creutz, C. )

    1989-04-19

    The carbon monoxide adduct of the cobalt(I) title macrocycle has been prepared via reaction of CoL{sup +} with CO{sub 2} and with CO and isolated as a perchlorate salt: IR (Nujol){nu}{sub CO} 1916 cm{sup {minus}1}; UV-vis (CH{sub 3}CH, {lambda}{sub max} ({epsilon})) 310 nm (3900 M{sup {minus}1} cm{sup {minus}1}), 430 sh (770), 510 sh (360), 1040 (240). In CH{sub 3}CN solvent its stability constant is {approx} 3 {times} 10{sup 8} M{sup {minus}1} at 25{degree}C. Structures of the square-pyramidal carbonyl complex and two other complexes of the title macrocycle have been determined from single-crystal x-ray diffraction data collected with use of Mo K{alpha} radiation. Crystallographic data: (CoL(CO))(ClO{sub 4}) (1), C2, a = 15.362 (3) {angstrom}, b = 7.580 (5) {angstrom}, c = 9.611 (3) {angstrom}, {beta} = 108.91 (2){degree}, V = 1059 (1) {angstrom}{sup 3}, Z = 2 (R = 0.057, R{sub w} = 0.069); N-meso,trans-CoLCl{sub 2} (2), Pbca, a = 11.570 (3) {angstrom}, b = 12.695 (3) {angstrom}, c = 13.309 (2) {angstrom}, V = 1954 (1) {angstrom}{sup 3}, Z = 4 (R = 0.075, R{sub w} = 0.070); cis-(CoL(CO{sub 3}))ClO{sub 4} (3), C2, a = 15.072 (5) {angstrom}, b = 7.603 (4) {angstrom}, c = 9.703 (3) {angstrom}, {beta} = 109.74 (3){degree}, V = 1047 (1) {angstrom}{sup 3}, Z = 2 (R = 0.033, R{sub w} = 0.048). The three structures contain square-pyramidal, five-coordinate cobalt(I) (1), strongly axially distorted six-coordinate cobalt(II) (2), and six-coordinate cobalt(III) with L occupying cis-coordination positions (3). They thus provide a striking illustration of the adaptability of L to a variety of coordination numbers and oxidation states. 30 refs., 3 figs., 8 tabs.

  3. 1-[3-Aminobenzisoxazol-5'-yl]-3-trifluoromethyl-6-[2'-(3-(R)-hydroxy-N-pyrrolidinyl)methyl-[1,1']-biphen-4-yl]-1,4,5,6-tetrahydropyrazolo-[3,4-c]-pyridin-7-one (BMS-740808) a highly potent, selective, efficacious, and orally bioavailable inhibitor of blood coagulation factor Xa.

    PubMed

    Pinto, Donald J P; Orwat, Michael J; Quan, Mimi L; Han, Qi; Galemmo, Robert A; Amparo, Eugene; Wells, Brian; Ellis, Christopher; He, Ming Y; Alexander, Richard S; Rossi, Karen A; Smallwood, Angela; Wong, Pancras C; Luettgen, Joseph M; Rendina, Alan R; Knabb, Robert M; Mersinger, Lawrence; Kettner, Charles; Bai, Steven; He, Kan; Wexler, Ruth R; Lam, Patrick Y S

    2006-08-01

    Attempts to further optimize the pyrazole factor Xa inhibitors centered on masking the aryl aniline P4 moiety. Scaffold optimization resulted in the identification of a novel bicyclic pyrazolo-pyridinone scaffold which retained fXa potency. The novel bicyclic scaffold preserved all binding interactions observed with the monocyclic counterpart and importantly the carboxamido moiety was integrated within the scaffold making it less susceptible to hydrolysis. These efforts led to the identification of 1-[3-aminobenzisoxazol-5'-yl]-3-trifluoromethyl-6-[2'-(3-(R)-hydroxy-N-pyrrolidinyl)methyl-[1,1']-biphen-4-yl]-1,4,5,6-tetrahydropyrazolo-[3,4-c]-pyridin-7-one 6f (BMS-740808), a highly potent (fXa Ki=30 pM) with a rapid onset of inhibition (2.7x10(7) M-1 s-1) in vitro, selective (>1000-fold over other proteases), efficacious in the AVShunt thrombosis model, and orally bioavailable inhibitor of blood coagulation factor Xa.

  4. Characterization and effects of methyl-2- (4-aminophenyl)-1, 2-dihydro-1-oxo-7- (2-pyridinylmethoxy)-4-(3,4, 5-trimethoxyphenyl)-3-isoquinoline carboxylate sulfate (T-1032), a novel potent inhibitor of cGMP-binding cGMP-specific phosphodiesterase (PDE5).

    PubMed

    Kotera, J; Fujishige, K; Michibata, H; Yuasa, K; Kubo, A; Nakamura, Y; Omori, K

    2000-11-01

    An isoquinolone derivative, methyl-2-(4-aminophenyl)-1, 2-dihydro-1-oxo-7-(2-pyridinylmethoxy)-4-(3,4, 5-trimethoxyphenyl)-3-isoquinoline carboxylate sulfate (T-1032), was found to be a novel potent inhibitor of cyclic GMP (cGMP)-binding cGMP-specific phosphodiesterase (PDE5). We investigated the inhibitory effects of T-1032 on six PDE isozymes isolated from canine tissues. T-1032 specifically inhibited the hydrolysis of cGMP by PDE5 partially purified from canine lung, at a low concentration (IC(50) = 1.0 nM, K(i) = 1.2 nM), in a competitive manner. In contrast, the IC(50) values of T-1032 for PDE1, PDE2, PDE3, and PDE4 were more than 1 microM. T-1032 also inhibited PDE6 from canine retina with an IC(50) of 28 nM, which is of the same order of magnitude as the IC(50) of sildenafil. cGMP hydrolytic activities of two alternative splice variants of canine PDE5 expressed in COS-7 cells were inhibited by this compound to a similar extent. T-1032 increased the intracellular concentration of cGMP in cultured rat vascular smooth muscle cells in the presence and absence of C-type natriuretic peptide, an activator of membrane-bound guanylate cyclase, whereas the compound did not change cyclic AMP levels. These data indicated that T-1032, which belongs to a new structural class of PDE5 inhibitors, is a potent and selective PDE5 inhibitor. This compound may be useful in pharmacological studies to examine the role of a cGMP/PDE5 pathway in tissues.

  5. Synthesis and structural investigation of some pyrimido[5,4-c]quinolin-4(3H)-one derivatives with a long-chain arylpiperazine moiety as potent 5-HT(1A/2A) and 5-HT(7) receptor ligands.

    PubMed

    Lewgowd, Wieslawa; Bojarski, Andrzej J; Szczesio, Malgorzata; Olczak, Andrzej; Glowka, Marek L; Mordalski, Stefan; Stanczak, Andrzej

    2011-08-01

    A series of new pyrimido[5,4-c]quinolin-4(3H)-ones with variable length of the spacer between amide and 4-arylpiperazine moiety were prepared to further explore the role of a terminal portion in the serotonergic activity. The majority of compounds demonstrated high in vitro affinity for 5-HT(1A) receptor, and moderate-to-low affinity for 5-HT(2A) and 5-HT(7) receptors. X-ray analysis, two-dimensional NMR, conformational studies and docking into the 5-HT(1A) receptor model were conducted to investigate conformational preferences of selected 5-HT(1A) receptor ligands in different environments. The extended conformation of tetramethylene derivatives was found in a solid state, in DMSO (for a protonated form) and as a global energy minimum during conformational analysis in simulated water environment. Ligand geometry in top-scored complexes, obtained by docking to a set of 100 receptor models, were either fully extended or with central spacer torsion in synclinal conformation.

  6. 12 CFR 5.7 - Investigations.

    Code of Federal Regulations, 2010 CFR

    2010-01-01

    ... 12 Banks and Banking 1 2010-01-01 2010-01-01 false Investigations. 5.7 Section 5.7 Banks and... CORPORATE ACTIVITIES Rules of General Applicability § 5.7 Investigations. (a) Authority. The OCC may examine... decision. (b) Fees. The OCC may assess fees for investigations or examinations conducted under paragraph...

  7. 12 CFR 5.7 - Investigations.

    Code of Federal Regulations, 2012 CFR

    2012-01-01

    ... 12 Banks and Banking 1 2012-01-01 2012-01-01 false Investigations. 5.7 Section 5.7 Banks and... CORPORATE ACTIVITIES Rules of General Applicability § 5.7 Investigations. (a) Authority. The OCC may examine... decision. (b) Fees. The OCC may assess fees for investigations or examinations conducted under paragraph...

  8. 12 CFR 5.7 - Investigations.

    Code of Federal Regulations, 2014 CFR

    2014-01-01

    ... 12 Banks and Banking 1 2014-01-01 2014-01-01 false Investigations. 5.7 Section 5.7 Banks and... CORPORATE ACTIVITIES Rules of General Applicability § 5.7 Investigations. (a) Authority. The OCC may examine... decision. (b) Fees. The OCC may assess fees for investigations or examinations conducted under paragraph...

  9. Exploring the binding mechanism of 5-hydroxy-3‧,4‧,7-trimethoxyflavone with bovine serum albumin: Spectroscopic and computational approach

    NASA Astrophysics Data System (ADS)

    Sudha, A.; Srinivasan, P.; Thamilarasan, V.; Sengottuvelan, N.

    2016-03-01

    The current study was carried out to investigate the binding mechanism of a potential flavonoid compound 5-hydroxy-3‧,4‧,7-trimethoxyflavone (HTMF) with bovine serum albumin (BSA) using ultraviolet-visible, fluorescence, circular dichroism (CD) spectral measurements along with molecular docking and molecular dynamics (MD) simulation. It was confirmed from fluorescence spectra that the intrinsic fluorescence of BSA was robustly quenched by HTMF through a static quenching mechanism. The number of binding sites (n) for HTMF binding on BSA was found to be about one. The thermodynamic parameters estimated from the van't Hoff plot specified that hydrophobic force was the predominant force in the HTMF-BSA complex and there also exist hydrogen bonds and electrostatic interactions. The effect of HTMF on the BSA conformation examined using CD studies revealed that there is a decrease in the helical content of BSA upon HTMF interaction. The results of molecular docking study shed light on the binding mode which exposed that HTMF bind within the hydrophobic pocket of the subdomain IIIA of BSA. The stability of HTMF-BSA complex with respect to free protein was analyzed from the molecular dynamic studies. The electronic structure analysis of HTMF was achieved by using density functional theory (DFT) calculations at B3LYP/6-31G** level to support its antioxidant role. The results of computational analysis are in good consistence with the experimental data and the present findings suggested that HTMF exhibits a good binding propensity to BSA protein which will be helpful for the drug design.

  10. Spectral investigation of the effect of anion on the stability of non covalent assemblies of 2,3,5,6,8,9,11,12-octahydro-1,4,7,10,13-benzopentaoxacyclopentadecine (benzo-15-crown-5) with sodium halides

    NASA Astrophysics Data System (ADS)

    Ghildiyal, Namrata; Pant, Geeta Joshi nee; Rawat, M. S. M.; Singh, Khushboo

    2017-01-01

    A series of complexes of 2,3,5,6,8,9,11,12-octahydro-1,4,7,10,13-benzopentaoxacyclopentadecine (benzo-15-crown-5) with sodium halides was synthesized in acetonitrile. The effect of anion on the stability and spectral properties of complexes of benzo-15-crown-5 with sodium halides was investigated. The synthesis of complexes of sodium fluoride and sodium chloride are reported for the first time. Chloroform was used as solvent to study the assembly in solution state by 1H and 13C NMR techniques. Single crystal diffraction studies on the easily crystallizable bromide complex confirmed 1:1 stoichiometry of the complex. IR and Raman studies provided valuable evidence for a water molecule shared between the crown encapsulated cation and the counter ion to give a solvent shared ion pair (SSIP). The fluorescence spectra of the complexes were obtained in chloroform by excitation at 270 nm to study the effect of complexation on the fluorescent properties of benzo-15-crown-5.

  11. Synthesis of Natural Homoisoflavonoids Having Either 5,7-Dihydroxy-6-methoxy or 7-Hydroxy-5,6-dimethoxy Groups

    PubMed Central

    Lee, Hyungjun; Yuan, Yue; Rhee, Inmoo; Corson, Timothy W.; Seo, Seung-Yong

    2016-01-01

    Naturally occurring homoisoflavonoids containing either 5,7-dihydroxy-6-methoxy or 7-hydroxy-5,6-dimethoxy groups such as the antiangiogenic homoisoflavanone, cremastranone, were synthesized via three or four linear steps from the known 4-chromenone. This facile synthesis includes chemoselective 1,4-reduction of 4-chromenone and selective deprotection of 3-benzylidene-4-chromanone a containing C7-benzyloxy group. PMID:27529212

  12. 15 CFR 5.7 - Reports.

    Code of Federal Regulations, 2010 CFR

    2010-01-01

    ... 15 Commerce and Foreign Trade 1 2010-01-01 2010-01-01 false Reports. 5.7 Section 5.7 Commerce and Foreign Trade Office of the Secretary of Commerce OPERATION OF VENDING STANDS § 5.7 Reports. No later than fifteen days following the end of each fiscal year the responsible officials set forth in § 5.3(c)...

  13. Pump-probe photoelectron velocity-map imaging of autoionizing singly excited 4s{sup 1}4p{sup 6}np{sup 1}(n=7,8) and doubly excited 4s{sup 2}4p{sup 4}5s{sup 1}6p{sup 1} resonances in atomic krypton

    SciTech Connect

    Doughty, Benjamin; Haber, Louis H.; Leone, Stephen R.

    2011-10-15

    Pump-probe photoelectron velocity-map imaging, using 27-eV high-harmonic excitation and 786-nm ionization, is used to resolve overlapping autoionizing resonances in atomic krypton, obtaining two-photon photoelectron angular distributions (PADs) for singly and doubly excited states. Two features in the photoelectron spectrum are assigned to singly excited 4s{sup 1}4p{sup 6}np{sup 1} (n = 7,8) configurations and four features provide information about double excitation configurations. The anisotropy parameters for the singly excited 7p configuration are measured to be {beta}{sub 2} = 1.61 {+-} 0.06 and {beta}{sub 4} = 1.54 {+-} 0.16 while the 8p configuration gives {beta}{sub 2} = 1.23 {+-} 0.19 and {beta}{sub 4} = 0.60 {+-} 0.15. These anisotropies most likely represent the sum of overlapping PADs from states of singlet and triplet spin multiplicities. Of the four bands corresponding to ionization of doubly excited states, two are assigned to 4s{sup 2}4p{sup 4}5s{sup 1}6p{sup 1} configurations that are probed to different J-split ion states. The two remaining doubly excited states are attributed to a previously observed, but unassigned, resonance in the vacuum-ultraviolet photoabsorption spectrum. The PADs from each of the double excitation states are also influenced by overlap from neighboring states that are not completely spectrally resolved. The anisotropies of the observed double excitation states are reported, anticipating future theoretical and experimental work to separate the overlapping PADs into the state resolved PADs. The results can be used to test theories of excited state ionization.

  14. 7 CFR 772.5 - Security maintenance.

    Code of Federal Regulations, 2011 CFR

    2011-01-01

    ... 7 Agriculture 7 2011-01-01 2011-01-01 false Security maintenance. 772.5 Section 772.5 Agriculture Regulations of the Department of Agriculture (Continued) FARM SERVICE AGENCY, DEPARTMENT OF AGRICULTURE SPECIAL PROGRAMS SERVICING MINOR PROGRAM LOANS § 772.5 Security maintenance. (a) General. Borrowers...

  15. 7 CFR 772.5 - Security maintenance.

    Code of Federal Regulations, 2012 CFR

    2012-01-01

    ... 7 Agriculture 7 2012-01-01 2012-01-01 false Security maintenance. 772.5 Section 772.5 Agriculture... SPECIAL PROGRAMS SERVICING MINOR PROGRAM LOANS § 772.5 Security maintenance. (a) General. Borrowers are responsible for maintaining the collateral that is serving as security for their Minor Program loan...

  16. 7 CFR 772.5 - Security maintenance.

    Code of Federal Regulations, 2014 CFR

    2014-01-01

    ... 7 Agriculture 7 2014-01-01 2014-01-01 false Security maintenance. 772.5 Section 772.5 Agriculture... SPECIAL PROGRAMS SERVICING MINOR PROGRAM LOANS § 772.5 Security maintenance. (a) General. Borrowers are responsible for maintaining the collateral that is serving as security for their Minor Program loan...

  17. 7 CFR 771.5 - Loan purposes.

    Code of Federal Regulations, 2014 CFR

    2014-01-01

    ... 7 Agriculture 7 2014-01-01 2014-01-01 false Loan purposes. 771.5 Section 771.5 Agriculture... SPECIAL PROGRAMS BOLL WEEVIL ERADICATION LOAN PROGRAM § 771.5 Loan purposes. (a) Loan funds may be used..., travel and office operations; (3) Salaries and benefits. (b) Loan funds may not be used to pay...

  18. 7 CFR 701.5 - Land eligibility.

    Code of Federal Regulations, 2010 CFR

    2010-01-01

    ... 7 Agriculture 7 2010-01-01 2010-01-01 false Land eligibility. 701.5 Section 701.5 Agriculture... ADMINISTERED UNDER THIS PART § 701.5 Land eligibility. (a) For land to be eligible, the Deputy Administrator must determine that land that is the subject of the cost share: (1) Will have new conservation...

  19. 7 CFR 772.5 - Security maintenance.

    Code of Federal Regulations, 2010 CFR

    2010-01-01

    ... 7 Agriculture 7 2010-01-01 2010-01-01 false Security maintenance. 772.5 Section 772.5 Agriculture Regulations of the Department of Agriculture (Continued) FARM SERVICE AGENCY, DEPARTMENT OF AGRICULTURE SPECIAL PROGRAMS SERVICING MINOR PROGRAM LOANS § 772.5 Security maintenance. (a) General. Borrowers...

  20. 5,5,7,12,12,14-Hexamethyl-1,8-bis-(4-nitro-benz-yl)-1,4,8,11-tetra-aza-cyclo-tetra-deca-ne.

    PubMed

    Gayathri, K; Sathya, S; Usha, G; Ramanjaneya Reddy, G; Balasubramanian, S

    2014-01-01

    The asymmetric unit of the title compound, C30H46N6O4, contains one half-mol-ecule. The C(benzene)-C(CH2)-N-C(-Me) torsion angle is -79.89 (13)° suggesting a synclinal orientation of the nitro-benzene ring with respect to the macrocycle. The conformation of the macrocycle is stabilized by intra-molecular N-H⋯N hydrogen bonds.

  1. 5,5,7,12,14,14-Hexamethyl-1,8-diaza-4,11-diazo­niacyclo­tetra­deca-4,11-diene dichloride trihydrate

    PubMed Central

    Ismail, Wafiuddin; Yamin, Bohari M.; Daran, Jean-Claude

    2012-01-01

    In the title compound, C16H34N4 2+·2Cl−·3H2O, the two protonated N atoms in the macrocyclic ring of the dication are located at diagonally opposite positions. There are two intramolecular N—H⋯N hydrogen bonds in the cation. The crystal structure features O—H⋯Cl, O—H⋯O, C—H⋯Cl and N—H⋯Cl hydrogen bonds. PMID:22590349

  2. Crystal chemistry of anhydrous Li uranyl phosphates and arsenates. II. Tubular fragments and cation-cation interactions in the 3D framework structures of Li{sub 6}[(UO{sub 2}){sub 12}(PO{sub 4}){sub 8}(P{sub 4}O{sub 13})], Li{sub 5}[(UO{sub 2}){sub 13}(AsO{sub 4}){sub 9}(As{sub 2}O{sub 7})], Li[(UO{sub 2}){sub 4}(AsO{sub 4}){sub 3}] and Li{sub 3}[(UO{sub 2}){sub 7}(AsO{sub 4}){sub 5}O

    SciTech Connect

    Alekseev, Evgeny V.; Krivovichev, Sergey V.; Depmeier, Wulf

    2009-11-15

    Single crystals of the new compounds Li{sub 6}[(UO{sub 2}){sub 12}(PO{sub 4}){sub 8}(P{sub 4}O{sub 13})] (1), Li{sub 5}[(UO{sub 2}){sub 13}(AsO{sub 4}){sub 9}(As{sub 2}O{sub 7})] (2), Li[(UO{sub 2}){sub 4}(AsO{sub 4}){sub 3}] (3) and Li{sub 3}[(UO{sub 2}){sub 7}(AsO{sub 4}){sub 5}O)] (4) have been prepared using high-temperature solid state reactions. The crystal structures have been solved by direct methods: 1-monoclinic, C2/m, a=26.963(3) A, b=7.063(1) A, c=19.639(1) A, beta=126.890(4){sup o}, V=2991.2(6) A{sup 3}, Z=2, R{sub 1}=0.0357 for 3248 unique reflections with |F{sub 0}|>=4sigma{sub F}; 2-triclinic, P1-bar, a=7.1410(8) A, b=13.959(1) A, c=31.925(1) A, alpha=82.850(2){sup o}, beta=88.691(2){sup o}, gamma=79.774(3){sup o}, V=3107.4(4) A{sup 3}, Z=2, R{sub 1}=0.0722 for 9161 unique reflections with |F{sub 0}|>=4sigma{sub F}; 3-tetragonal, I4{sub 1}/amd, a=7.160(3) A, c=33.775(9) A, V=1732(1) A{sup 3}, Z=4, R{sub 1}=0.0356 for 318 unique reflections with |F{sub 0}|>=4sigma{sub F}; 4-tetragonal, P4-bar, a=7.2160(5) A, c=14.6540(7) A, V=763.04(8) A{sup 3}, Z=1, R{sub 1}=0.0423 for 1600 unique reflections with |F{sub 0}|>=4sigma{sub F}. Structures of all the phases under consideration are based on complex 3D frameworks consisting of different types of uranium polyhedra (UO{sub 6} and UO{sub 7}) and different types of tetrahedral TO{sub 4} anions (T=P or As): PO{sub 4} and P{sub 4}O{sub 13} in 1, AsO{sub 4} and As{sub 2}O{sub 7} in 2, and single AsO{sub 4} tetrahedra in 3 and 4. In the structures of 1 and 2, UO{sub 7} pentagonal bipyramids share edges to form (UO{sub 5}){sub i}nfinity chains extended along the b axis in 1 and along the a axis in 2. The chains are linked via single TO{sub 4} tetrahedra into tubular units with external diameters of 11 A in 1 and 11.5 A in 2, and internal diameters of 4.1 A in 1 and 4.5 A in 2. The channels accommodate Li{sup +} cations. The tubular units are linked into 3D frameworks by intertubular complexes. Structures of 3 and 4

  3. z ≳ 7 Galaxies with Red Spitzer/IRAC [3.6]-[4.5] Colors in the Full CANDELS Data Set: The Brightest-Known Galaxies at z ~ 7-9 and a Probable Spectroscopic Confirmation at z = 7.48

    NASA Astrophysics Data System (ADS)

    Roberts-Borsani, G. W.; Bouwens, R. J.; Oesch, P. A.; Labbe, I.; Smit, R.; Illingworth, G. D.; van Dokkum, P.; Holden, B.; Gonzalez, V.; Stefanon, M.; Holwerda, B.; Wilkins, S.

    2016-06-01

    We identify four unusually bright (H {}160,{AB} < 25.5) galaxies from Hubble Space Telescope (HST) and Spitzer CANDELS data with probable redshifts z ˜ 7-9. These identifications include the brightest-known galaxies to date at z ≳ 7.5. As Y-band observations are not available over the full CANDELS program to perform a standard Lyman-break selection of z > 7 galaxies, we employ an alternate strategy using deep Spitzer/IRAC data. We identify z ˜ 7.1-9.1 galaxies by selecting z ≳ 6 galaxies from the HST CANDELS data that show quite red IRAC [3.6]-[4.5] colors, indicating strong [O iii]+Hβ lines in the 4.5 μm band. This selection strategy was validated using a modest sample for which we have deep Y-band coverage, and subsequently used to select the brightest z ≥ 7 sources. Applying the IRAC criteria to all HST-selected optical dropout galaxies over the full ˜900 arcmin2 of the CANDELS survey revealed four unusually bright z ˜ 7.1, 7.6, 7.9, and 8.6 candidates. The median [3.6]-[4.5] color of our selected z ˜ 7.1-9.1 sample is consistent with rest-frame [O iii]+Hβ EWs of ˜1500 Å in the [4.5] band. Keck/MOSFIRE spectroscopy has been independently reported for two of our selected sources, showing Lyα at redshifts of 7.7302 ± 0.0006 and {8.683}-0.004+0.001, respectively. We present similar Keck/MOSFIRE spectroscopy for a third selected galaxy with a probable 4.7σ Lyα line at z spec = 7.4770 ± 0.0008. All three have H160-band magnitudes of ˜25 mag and are ˜0.5 mag more luminous (M 1600 ˜ -22.0) than any previously discovered z ˜ 8 galaxy, with important implications for the UV luminosity function (LF). Our three brightest and highest redshift z > 7 galaxies all lie within the CANDELS-EGS field, providing a dramatic illustration of the potential impact of field-to-field variance.

  4. Crystal structure of (2-{3-[4-(4'-cyano-biphenyl-4-yl-oxy)but-oxy]pyridin-2-yl-κN}-5-(dodec-yloxy)phenyl-κC (1))(9-oxo-tetra-cos-7-en-7-olato-κ(2) O,O')platinum(II).

    PubMed

    Luo, Kaijun; Liu, Hanlin; Guo, Qing; Luo, Daibing

    2014-12-01

    The central Pt(II) atom in the title compound, [Pt(C40H47N2O3)(C24H45O2)], has a slightly distorted square-planar coordination environment. The dihedral angle between the plane formed by Pt and the chelating C and N atoms and that formed by Pt and the chelating O atoms is 2.1 (3)°. The angle between the planes of the two rings in the biphenyl-4-carbo-nitrile unit is 35.1 (5)°. One lateral alkane chain is disordered over two sets of sites with site occupancy factors in a 0.595 (7):0.405 (7) ratio.

  5. Ring-expansion synthesis and crystal structure of dimethyl 4-ethyl-1,4,5,6,7,8-hexa­hydro­azonino[5,6-b]indole-2,3-di­carboxyl­ate

    PubMed Central

    Nguyen, Van Tuyen; Sorokina, Elena A.; Listratova, Anna V.; Voskressensky, Leonid G.; Lobanov, Nikolai N.; Dorovatovskii, Pavel V.

    2017-01-01

    The title compound, C20H24N2O4, is the product of a ring-expansion reaction from a seven-membered hexa­hydro­azepine to a nine-membered azonine. The azonine ring of the mol­ecule adopts a chair–boat conformation. In the crystal, mol­ecules are linked by bifurcated N—H⋯(O,O) hydrogen bonds, generating [010] zigzag chains. The title compound shows inhibitory activity against acetyl­cholinesterase and butyrylcholinesterase, and might be considered as a candidate for the design of new types of anti-Alzheimer’s drugs. PMID:28316803

  6. In vitro metabolism of 2-[6-(4-chlorophenyl)-2,2-dimethyl-7-phenyl-2,3-dihydro-1H-pyrrolizin-5-yl] acetic acid (licofelone, ML3000), an inhibitor of cyclooxygenase-1 and -2 and 5-lipoxygenase.

    PubMed

    Albrecht, Wolfgang; Unger, Anke; Nussler, Andreas K; Laufer, Stefan

    2008-05-01

    2-[6-(4-Chlorophenyl)-2,2-dimethyl-7-phenyl-2,3-dihydro-1H-pyrrolizin-5-yl] acetic acid (licofelone) is a dual inhibitor of both cyclooxygenase isoforms and 5-lipoxygenase and under development for treatment of osteoarthritis. In conventional in vitro assays using liver microsomes and NADPH as cosubstrate, a high metabolic stability of licofelone was observed. In the presence of UDP-glucuronic acid, licofelone is rapidly converted into the corresponding acyl glucuronide, M1. These results are in conflict with data from clinical studies. After administration of licofelone to humans, M1 plasma concentrations were negligibly low, whereas the exposure of the hydroxy-metabolite M2 achieved values of approximately 20% compared with that of the parent drug. Metabolism studies with human hepatocytes and dual-activity assays with microsomes, which allowed the simultaneous monitoring of hydroxylation and glucuronidation reactions, were performed, and the metabolic pathway of licofelone was elucidated. After glucuronidation, predominantly catalyzed by UDP glucuronosyltransferase (UGT) isoforms UGT2B7, UGT1A9, and UGT1A3, M1 is converted into the hydroxy-glucuronide M3 in a CYP2C8-dependent reaction. The enzyme specificities were investigated using recombinant human cytochrome P450 and UGT isoforms as test systems. In vitro drug-interaction studies using the 6alpha-hydroxylation of paclitaxel as control reaction confirmed that neither licofelone nor M1 is a relevant inhibitor of CYP2C8. The formation of M3 was also observed with liver microsomes from cynomolgus monkeys, but in incubations with mouse and rat liver microsomes, M1 remained unchanged. The clinical relevance of these findings is discussed.

  7. The genome of alkaliphilic Bacillus pseudofirmus OF4 reveals adaptations that support the ability to grow in an external pH range from 7.5 to 11.4

    PubMed Central

    Janto, Benjamin; Ahmed, Azad; Ito, Masahiro; Liu, Jun; Hicks, David B.; Pagni, Sarah; Fackelmayer, Oliver J.; Smith, Terry-Ann; Earl, Joshua; Elbourne, Liam D.H.; Hassan, Karl; Paulsen, Ian T.; Kolstø, Anne-Brit; Tourasse, Nicolas J.; Ehrlich, Garth D.; Boissy, Robert; Ivey, D. Mack; Li, Gang; Xue, Yanfen; Ma, Yanhe; Hu, Fen Z.; Krulwich, Terry A.

    2011-01-01

    Summary Bacillus pseudofirmus OF4 is an extreme but facultative alkaliphile that grows non-fermentatively in a pH range from 7.5 to above 11.4 and can withstand large sudden increases in external pH. It is a model organism for studies of bioenergetics at high pH, at which energy demands are higher than at neutral pH because both cytoplasmic pH homeostasis and ATP synthesis require more energy. The alkaliphile also tolerates a cytoplasmic pH > 9.0 at external pH values at which the pH homeostasis capacity is exceeded, and manages other stresses that are exacerbated at alkaline pH, e.g. sodium, oxidative and cell wall stresses. The genome of B. pseudofirmus OF4 includes two plasmids that are lost from some mutants without viability loss. The plasmids may provide a reservoir of mobile elements that promote adaptive chromosomal rearrangements under particular environmental conditions. The genome also reveals a more acidic pI profile for proteins exposed on the outer surface than found in neutralophiles. A large array of transporters and regulatory genes are predicted to protect the alkaliphile from its overlapping stresses. In addition, unanticipated metabolic versatility was observed, which could ensure requisite energy for alkaliphily under diverse conditions. PMID:21951522

  8. Genome of alkaliphilic Bacillus pseudofirmus OF4 reveals adaptations that support the ability to grow in an external pH range from 7.5 to 11.4.

    PubMed

    Janto, Benjamin; Ahmed, Azad; Ito, Masahiro; Liu, Jun; Hicks, David B; Pagni, Sarah; Fackelmayer, Oliver J; Smith, Terry-Ann; Earl, Joshua; Elbourne, Liam D H; Hassan, Karl; Paulsen, Ian T; Kolstø, Anne-Brit; Tourasse, Nicolas J; Ehrlich, Garth D; Boissy, Robert; Ivey, D Mack; Li, Gang; Xue, Yanfen; Ma, Yanhe; Hu, Fen Z; Krulwich, Terry A

    2011-12-01

    Bacillus pseudofirmus OF4 is an extreme but facultative alkaliphile that grows non-fermentatively in a pH range from 7.5 to above 11.4 and can withstand large sudden increases in external pH. It is a model organism for studies of bioenergetics at high pH, at which energy demands are higher than at neutral pH because both cytoplasmic pH homeostasis and ATP synthesis require more energy. The alkaliphile also tolerates a cytoplasmic pH > 9.0 at external pH values at which the pH homeostasis capacity is exceeded, and manages other stresses that are exacerbated at alkaline pH, e.g. sodium, oxidative and cell wall stresses. The genome of B. pseudofirmus OF4 includes two plasmids that are lost from some mutants without viability loss. The plasmids may provide a reservoir of mobile elements that promote adaptive chromosomal rearrangements under particular environmental conditions. The genome also reveals a more acidic pI profile for proteins exposed on the outer surface than found in neutralophiles. A large array of transporters and regulatory genes are predicted to protect the alkaliphile from its overlapping stresses. In addition, unanticipated metabolic versatility was observed, which could ensure requisite energy for alkaliphily under diverse conditions.

  9. Corrosion inhibition of mild steel in 1M HCl by D-glucose derivatives of dihydropyrido [2,3-d:6,5-d′] dipyrimidine-2, 4, 6, 8(1H,3H, 5H,7H)-tetraone

    PubMed Central

    Verma, Chandrabhan; Quraishi, M. A.; Kluza, K.; Makowska-Janusik, M.; Olasunkanmi, Lukman O.; Ebenso, Eno E.

    2017-01-01

    D-glucose derivatives of dihydropyrido-[2,3-d:6,5-d′]-dipyrimidine-2, 4, 6, 8(1H,3H, 5H,7H)-tetraone (GPHs) have been synthesized and investigated as corrosion inhibitors for mild steel in 1M HCl solution using gravimetric, electrochemical, surface, quantum chemical calculations and Monte Carlo simulations methods. The order of inhibition efficiencies is GPH-3 > GPH-2 > GPH-1. The results further showed that the inhibitor molecules with electron releasing (-OH, -OCH3) substituents exhibit higher efficiency than the parent molecule without any substituents. Polarization study suggests that the studied compounds are mixed-type but exhibited predominantly cathodic inhibitive effect. The adsorption of these compounds on mild steel surface obeyed the Langmuir adsorption isotherm. SEM, EDX and AFM analyses were used to confirm the inhibitive actions of the molecules on mild steel surface. Quantum chemical (QC) calculations and Monte Carlo (MC) simulations studies were undertaken to further corroborate the experimental results. PMID:28317849

  10. Spin dynamics, short-range order, and spin freezing in Y{sub 0.5}Ca{sub 0.5}BaCo{sub 4}O{sub 7}

    SciTech Connect

    Stewart, J. R.; Ehlers, G.; Mutka, H.; Fouquet, P.; Payen, C.; Lortz, R.

    2011-01-15

    Y{sub 0.5}Ca{sub 0.5}BaCo{sub 4}O{sub 7} was recently introduced as a possible candidate for capturing some of the predicted classical spin kagome ground-state features. Stimulated by this conjecture, we have taken up a more complete study of the spin correlations in this compound with neutron scattering methods on a powder sample characterized with high-resolution neutron diffraction and the temperature dependence of magnetic susceptibility and specific heat. We have found that the frustrated near-neighbor magnetic correlations involve not only the kagome planes but concern the full Co sublattice, as evidenced by the analysis of the wave-vector dependence of the short-range order. We conclude from our results that the magnetic moments are located on the Co sublattice as a whole and that correlations extend beyond the two-dimensional kagome planes. We identify intriguing dynamical properties, observing high-frequency fluctuations with a Lorentzian linewidth {Gamma}{<=}20 meV at ambient temperature. On cooling a low-frequency ({approx}1 meV) dynamical component develops alongside the high-frequency fluctuations, which eventually becomes static at temperatures below T{approx_equal}50 K. The high-frequency response with an overall linewidth of {approx}10 meV prevails at T{<=}2 K, coincident with a fully elastic short-range-ordered contribution.

  11. Corrosion inhibition of mild steel in 1M HCl by D-glucose derivatives of dihydropyrido [2,3-d:6,5-d‧] dipyrimidine-2, 4, 6, 8(1H,3H, 5H,7H)-tetraone

    NASA Astrophysics Data System (ADS)

    Verma, Chandrabhan; Quraishi, M. A.; Kluza, K.; Makowska-Janusik, M.; Olasunkanmi, Lukman O.; Ebenso, Eno E.

    2017-03-01

    D-glucose derivatives of dihydropyrido-[2,3-d:6,5-d‧]-dipyrimidine-2, 4, 6, 8(1H,3H, 5H,7H)-tetraone (GPHs) have been synthesized and investigated as corrosion inhibitors for mild steel in 1M HCl solution using gravimetric, electrochemical, surface, quantum chemical calculations and Monte Carlo simulations methods. The order of inhibition efficiencies is GPH-3 > GPH-2 > GPH-1. The results further showed that the inhibitor molecules with electron releasing (-OH, -OCH3) substituents exhibit higher efficiency than the parent molecule without any substituents. Polarization study suggests that the studied compounds are mixed-type but exhibited predominantly cathodic inhibitive effect. The adsorption of these compounds on mild steel surface obeyed the Langmuir adsorption isotherm. SEM, EDX and AFM analyses were used to confirm the inhibitive actions of the molecules on mild steel surface. Quantum chemical (QC) calculations and Monte Carlo (MC) simulations studies were undertaken to further corroborate the experimental results.

  12. Long-Term Corrosion Tests of Prototypical SAM2X5 (Fe49.7Cr17.7Mn1.9Mo7.4W1.6B15.2C3.8Si2.4) Coatings

    SciTech Connect

    Farmer, J C; Choi, J S; Saw, C K; Rebak, R H; Day, S D; Lian, T; Hailey, P D; Payer, J H; Branagan, D J; Aprigliano, L F

    2007-05-10

    An iron-based amorphous metal with good corrosion resistance and a high absorption cross-section for thermal neutrons has been developed and is reported here. This amorphous alloy has the approximate formula Fe{sub 49.7}Cr{sub 17.7}Mn{sub 1.9}Mo{sub 7.4}W{sub 1.6}B{sub 15.2}C{sub 3.8}Si{sub 2.4} and is known as SAM2X5. Chromium (Cr), molybdenum (Mo) and tungsten (W) were added to provide corrosion resistance, while boron (B) was added to promote glass formation and the absorption of thermal neutrons. Since this amorphous metal has a higher boron content than conventional borated stainless steels, it provides the nuclear engineer with design advantages for criticality control structures with enhanced safety. While melt-spun ribbons with limited practical applications were initially produced, large quantities (several tons) of gas atomized powder have now been produced on an industrial scale, and applied as thermal-spray coatings on prototypical half-scale spent nuclear fuel containers and neutron-absorbing baskets. These prototypes and other SAM2X5 samples have undergone a variety of corrosion testing, including both salt-fog and long-term immersion testing. The modes and rates of corrosion have been determined in the various environments, and are reported here. While these coatings have less corrosion resistance than melt-spun ribbons and optimized coatings produced in the laboratory, substantial corrosion resistance has been achieved.

  13. Circulating precursor CCR7(lo)PD-1(hi) CXCR5⁺ CD4⁺ T cells indicate Tfh cell activity and promote antibody responses upon antigen reexposure.

    PubMed

    He, Jing; Tsai, Louis M; Leong, Yew Ann; Hu, Xin; Ma, Cindy S; Chevalier, Nina; Sun, Xiaolin; Vandenberg, Kirsten; Rockman, Steve; Ding, Yan; Zhu, Lei; Wei, Wei; Wang, Changqi; Karnowski, Alexander; Belz, Gabrielle T; Ghali, Joanna R; Cook, Matthew C; Riminton, D Sean; Veillette, André; Schwartzberg, Pamela L; Mackay, Fabienne; Brink, Robert; Tangye, Stuart G; Vinuesa, Carola G; Mackay, Charles R; Li, Zhanguo; Yu, Di

    2013-10-17

    Follicular B helper T (Tfh) cells support high affinity and long-term antibody responses. Here we found that within circulating CXCR5⁺ CD4⁺ T cells in humans and mice, the CCR7(lo)PD-1(hi) subset has a partial Tfh effector phenotype, whereas CCR7(hi)PD-1(lo) cells have a resting phenotype. The circulating CCR7(lo)PD-1(hi) subset was indicative of active Tfh differentiation in lymphoid organs and correlated with clinical indices in autoimmune diseases. Thus the CCR7(lo)PD-1(hi) subset provides a biomarker to monitor protective antibody responses during infection or vaccination and pathogenic antibody responses in autoimmune diseases. Differentiation of both CCR7(hi)PD-1(lo) and CCR7(lo)PD-1(hi) subsets required ICOS and BCL6, but not SAP, suggesting that circulating CXCR5⁺ helper T cells are primarily generated before germinal centers. Upon antigen reencounter, CCR7(lo)PD-1(hi) CXCR5⁺ precursors rapidly differentiate into mature Tfh cells to promote antibody responses. Therefore, circulating CCR7(lo)PD-1(hi) CXCR5⁺ CD4⁺ T cells are generated during active Tfh differentiation and represent a new mechanism of immunological early memory.

  14. 41 CFR 51-5.7 - Payments.

    Code of Federal Regulations, 2010 CFR

    2010-07-01

    ... COMMITTEE FOR PURCHASE FROM PEOPLE WHO ARE BLIND OR SEVERELY DISABLED 5-CONTRACTING REQUIREMENTS § 51-5.7 Payments. Payments for products or services of persons who are blind or have other severe...

  15. Formic acid catalysed rearrangement of 5beta-methyldihydrothevinols (= 3,6-dimethoxy-5,17-dimethyl-4,5-epoxy-6,14-ethanomorphinan-7-methanols): synthesis of new doubly bridged morphinan derivatives.

    PubMed

    Rennison, David; Grundt, Peter; Goodyer, Claire; Lewis, John W; Husbands, Stephen M

    2005-02-01

    We recently showed that substitution of a 5beta-methyl group allows the isolation of 14-alkenyldihydrocodeinones from the action of hot formic acid on certain dihydrothevinols. It has now been shown that, in those dihydrothevinols which are converted to stable side chain olefins by such treatment, introduction of a 5beta-methyl group results in the formation of new doubly bridged morphinan derivatives in addition to the dihydrocodeinones or olefins. The new morphinans have low affinities for opioid receptors.

  16. 2,4-Dialkyl-8,9,10,11-tetrahydrobenzo[g]pyrimido[4,5-c]isoquinoline-1,3,7,12(2H,4H)-tetraones as new leads against Mycobacterium tuberculosis.

    PubMed

    Claes, Pieter; Cappoen, Davie; Uythethofken, Cynthia; Jacobs, Jan; Mertens, Birgit; Mathys, Vanessa; Verschaeve, Luc; Huygen, Kris; De Kimpe, Norbert

    2014-04-22

    Given the re-emergence of tuberculosis in Europe and beyond, the search for novel bio-active compound classes against this disease is of utmost importance. As a result of a high intrinsic tolerance of the etiological agent, Mycobacterium tuberculosis, towards most antibiotics and xenobiotics, the search for such new compounds is far from trivial. Further exacerbated by the rapid generation and spread of drug resistant M. tuberculosis and fuelled by the HIV/AIDS pandemic, halting the tuberculosis epidemic is of paramount importance. As part of our program to design new 2-aza-anthraquinones with anti-mycobacterial activity, various dialkyltetrahydrobenzo[g]pyrimido[4,5-c]isoquinolinetetraones were designed and synthesised. The compounds were submitted to a biological evaluation in which the activity against M.tb H37Rv(lux) was observed, as well as the acute toxicity towards J774 A.1 macrophages. From these results, the selectivity index was calculated. Furthermore, the activity of the most promising compounds was further studied against a multi-drug resistant LAM-1 strain and against intracellular replicating M.tb. The study was further extended with a comet assay and a VITOTOX™ assay to investigate the possibility of observable genotoxic effects caused by these compounds.

  17. 5 CFR 7.3 - Citizenship.

    Code of Federal Regulations, 2014 CFR

    2014-01-01

    ... 5 Administrative Personnel 1 2014-01-01 2014-01-01 false Citizenship. 7.3 Section 7.3 Administrative Personnel OFFICE OF PERSONNEL MANAGEMENT CIVIL SERVICE RULES GENERAL PROVISIONS (RULE VII) § 7.3 Citizenship. (a) No person shall be admitted to competitive examination unless such person is a citizen...

  18. 5 CFR 7.2 - Reemployment rights.

    Code of Federal Regulations, 2014 CFR

    2014-01-01

    ... 5 Administrative Personnel 1 2014-01-01 2014-01-01 false Reemployment rights. 7.2 Section 7.2 Administrative Personnel OFFICE OF PERSONNEL MANAGEMENT CIVIL SERVICE RULES GENERAL PROVISIONS (RULE VII) § 7.2 Reemployment rights. OPM, whenever it determines it to be necessary, shall prescribe regulations governing...

  19. 5 CFR 1830.7 - Fees.

    Code of Federal Regulations, 2010 CFR

    2010-01-01

    ... 5 Administrative Personnel 3 2010-01-01 2010-01-01 false Fees. 1830.7 Section 1830.7 Administrative Personnel OFFICE OF SPECIAL COUNSEL PRIVACY § 1830.7 Fees. Requests for copies of records shall be subject to duplication fees set forth in part 1820 of this chapter....

  20. [Ni(PPh2NAr2)2(NCMe)][BF4]2 as an electrocatalyst for H2 production: PPh2NAr2 = 1,5-(di(4-(thiophene-3-yl)phenyl)-3,7-diphenyl-1,5-diaza-3,7-diphosphacyclooctane)

    SciTech Connect

    Pool, Douglas H.; DuBois, Daniel L.

    2009-08-01

    A new cyclic 1,5-diaza-3,7-diphosphacyclooctane ligand was prepared with phenyl substituents on phosphorus and (thiophene-3-yl)phenyl substituents on nitrogen. This ligand reacts with [Ni(CH3CN)6][BF4]2 to form the corresponding [Ni(PPh2NAr2)2(NCMe)][BF4]2 complex, 3, which is an active electrocatalyst for H2 production. Kinetic studies indicate that the catalytic rate is first order in catalyst and second order in acid at low concentrations of acid, but at higher acid concentrations the catalytic rate becomes independent of acid concentration. The rate-determining step at high acid concentrations is attributed to the elimination of H2 from a reduced Ni species. The modest overpotential of 280 mV and a turnover frequency of 56 s-1 confirms that high activity observed is a general feature of this class of complexes and not an exception. Oxidation of the pendant thiophene substituents of 3 results in the formation of films on the electrode surface. However these films are not electroactive and electrocatalysis of proton reduction is not observed with these modified electrodes. Pacific Northwest National Laboratory is operated by Battelle for the US Department of Energy.

  1. Design, Synthesis, and Antitumor Activity of Novel 5-Pyridyl-1,3,4-oxadiazole Derivatives against the Breast Cancer Cell Line MCF-7.

    PubMed

    Khalil, Nadia Abdalla; Kamal, Aliaa Moh; Emam, Soha Hussein

    2015-01-01

    Various 1,3,4-oxadiazole-2-thiol derivatives have considerable potential in the field of antitumor activity. On the basis of the structure of the highly active reported oxadiazole analogues, 36 novel compounds were designed. Their molecular transport properties were predicted using a computer-aided program, and they were then synthesized and tested for anticancer activity against the breast cancer cell line MCF-7. Most of the tested compounds showed excellent to potent cytotoxic activity. Docking studies were carried out to examine the possibilities of the target compounds to become lead compounds in the future after more biological investigations. Compounds 18 and 22 were more active than the reference drug with IC₅₀ values of 0.010 µM and 0.012 µM, respectively, and binding energy scores of -10.32 and -10.25, respectively.

  2. Installation Restoration Program (IRP) for IRP Sites Numbers 4, 5, 7 and 14. 152 Tactical Reconnaissance Group, Nevada Air National Guard, Reno Tahoe International Airport, Reno, Nevada

    DTIC Science & Technology

    1996-01-01

    CD 0d4e!UO ~ -- * Nh - a LO a301 co4 E . *E; V - < (v (I, rs _ CO C2 2_ .- -t v)-- - - - - - - - - - - - - - - ERM C.W C *Y P-444 Wý 1) C m...FUNDIN NU1MIEwrShq9 aa Ai ainlGad 5nd TactM ica ReonisneGoup Renomst Tahoeaoet f ntrna1=, mtional - A (irpor.’t, W Rena.( NevadaH"urer ovce.Drctr’ ndPeo I wf...recommended for the all sites. 14. SUNJET ’TERS Prga:CmrhnieEvrnetlRsosIS. NUMBER qArPAG1S Installation RestorationPorm opeesv niomna epne a Comnpensation and

  3. Discovery of a Novel Series of Orally Bioavailable and CNS Penetrant Glucagon-like Peptide-1 Receptor (GLP-1R) Noncompetitive Antagonists Based on a 1,3-Disubstituted-7-aryl-5,5-bis(trifluoromethyl)-5,8-dihydropyrimido[4,5-d]pyrimidine-2,4(1H,3H)-dione Core.

    PubMed

    Nance, Kellie D; Days, Emily L; Weaver, C David; Coldren, Anastasia; Farmer, Tiffany D; Cho, Hyekyung P; Niswender, Colleen M; Blobaum, Anna L; Niswender, Kevin D; Lindsley, Craig W

    2017-02-23

    A duplexed, functional multiaddition high throughput screen and subsequent optimization effort identified the first orally bioavailable and CNS penetrant glucagon-like peptide-1 receptor (GLP-1R) noncompetitive antagonist. Antagonist 5d not only blocked exendin-4-stimulated insulin release in islets but also lowered insulin levels while increasing blood glucose in vivo.

  4. A novel [Mn2(μ-(C6H5)2CHCOO)2(bipy)4](bipy)(ClO4)2 complex loaded solid lipid nanoparticles: synthesis, characterization and in vitro cytotoxicity on MCF-7 breast cancer cells.

    PubMed

    Guney Eskiler, G; Cecener, G; Dikmen, G; Kani, I; Egeli, U; Tunca, B

    2016-09-01

    Manganese (Mn)-based complexes have been drawing attention due to the fact that they are more effective than other metal complexes. However, the use of Mn(II)-based complexes in medicine remains limited because of certain side effects. The aim of this study was to investigate the cytotoxic and apoptotic effects of a novel Mn(II) complex [Mn2(μ-(C6H5)2CHCOO)2(bipy)4](bipy)(ClO4)2 and Mn(II) complex loaded solid lipid nanoparticles (SLNs) on MCF-7 and HUVEC control cells. The average diameter of Mn(II) complex was about 1120 ± 2.43 nm, while the average particle size of Mn(II) complex-SLNs was ∼340 ± 2.27 nm. The cytotoxic effects of Mn(II) complex and Mn(II)-SLNs were 86.8 and 66.4%, respectively (p < .05). Additionally, both Mn(II) complex (39.25%) and Mn(II)-SLNs (38.05%) induced apoptosis and increased the arrest of G0/G1 phase. However, Mn(II) complex exerted toxic effects on the HUVEC control cell (63.4%), whereas no toxic effects was observed when treated with Mn(II)-SLNs at 150 μM. As a consequence, SLNs might be potentially used for metal-based complexes in the treatment of cancer due to reducing size and toxic effects of metal-based complexes.

  5. 48 CFR 915.404-4-70-7 - Alternative techniques.

    Code of Federal Regulations, 2011 CFR

    2011-10-01

    ... 48 Federal Acquisition Regulations System 5 2011-10-01 2011-10-01 false Alternative techniques. 915.404-4-70-7 Section 915.404-4-70-7 Federal Acquisition Regulations System DEPARTMENT OF ENERGY CONTRACTING METHODS AND CONTRACT TYPES CONTRACTING BY NEGOTIATION Contract Pricing 915.404-4-70-7...

  6. 48 CFR 915.404-4-70-7 - Alternative techniques.

    Code of Federal Regulations, 2013 CFR

    2013-10-01

    ... 48 Federal Acquisition Regulations System 5 2013-10-01 2013-10-01 false Alternative techniques. 915.404-4-70-7 Section 915.404-4-70-7 Federal Acquisition Regulations System DEPARTMENT OF ENERGY CONTRACTING METHODS AND CONTRACT TYPES CONTRACTING BY NEGOTIATION Contract Pricing 915.404-4-70-7...

  7. 48 CFR 915.404-4-70-7 - Alternative techniques.

    Code of Federal Regulations, 2014 CFR

    2014-10-01

    ... 48 Federal Acquisition Regulations System 5 2014-10-01 2014-10-01 false Alternative techniques. 915.404-4-70-7 Section 915.404-4-70-7 Federal Acquisition Regulations System DEPARTMENT OF ENERGY CONTRACTING METHODS AND CONTRACT TYPES CONTRACTING BY NEGOTIATION Contract Pricing 915.404-4-70-7...

  8. 48 CFR 915.404-4-70-7 - Alternative techniques.

    Code of Federal Regulations, 2012 CFR

    2012-10-01

    ... 48 Federal Acquisition Regulations System 5 2012-10-01 2012-10-01 false Alternative techniques. 915.404-4-70-7 Section 915.404-4-70-7 Federal Acquisition Regulations System DEPARTMENT OF ENERGY CONTRACTING METHODS AND CONTRACT TYPES CONTRACTING BY NEGOTIATION Contract Pricing 915.404-4-70-7...

  9. 48 CFR 915.404-4-70-7 - Alternative techniques.

    Code of Federal Regulations, 2010 CFR

    2010-10-01

    ... 48 Federal Acquisition Regulations System 5 2010-10-01 2010-10-01 false Alternative techniques. 915.404-4-70-7 Section 915.404-4-70-7 Federal Acquisition Regulations System DEPARTMENT OF ENERGY CONTRACTING METHODS AND CONTRACT TYPES CONTRACTING BY NEGOTIATION Contract Pricing 915.404-4-70-7...

  10. Handbook of Accelerator Physics and Engineering (sections 2.7.1 - 2.7.5 and 7.6.2)

    SciTech Connect

    Roser, T.

    1999-04-19

    The sections written by this author are: 2.7.1- Thomas - BMT equation; 2.2.2- Spinor Algebra; 2.7.3- Spin Rotators and Siberian Snakes; 2.7.4- Ring with Spin Rotator and Siberian Snakes; 2.7.5- Depolarizing Resonances and Spin Flippers; & 7.6.2- Proton Beam Polarimeters

  11. 7 CFR 735.5 - Penalties.

    Code of Federal Regulations, 2012 CFR

    2012-01-01

    ... 7 Agriculture 7 2012-01-01 2012-01-01 false Penalties. 735.5 Section 735.5 Agriculture Regulations of the Department of Agriculture (Continued) FARM SERVICE AGENCY, DEPARTMENT OF AGRICULTURE REGULATIONS FOR WAREHOUSES REGULATIONS FOR THE UNITED STATES WAREHOUSE ACT General Provisions §...

  12. 7 CFR 735.5 - Penalties.

    Code of Federal Regulations, 2011 CFR

    2011-01-01

    ... 7 Agriculture 7 2011-01-01 2011-01-01 false Penalties. 735.5 Section 735.5 Agriculture Regulations of the Department of Agriculture (Continued) FARM SERVICE AGENCY, DEPARTMENT OF AGRICULTURE REGULATIONS FOR WAREHOUSES REGULATIONS FOR THE UNITED STATES WAREHOUSE ACT General Provisions §...

  13. 7 CFR 735.5 - Penalties.

    Code of Federal Regulations, 2014 CFR

    2014-01-01

    ... 7 Agriculture 7 2014-01-01 2014-01-01 false Penalties. 735.5 Section 735.5 Agriculture Regulations of the Department of Agriculture (Continued) FARM SERVICE AGENCY, DEPARTMENT OF AGRICULTURE REGULATIONS FOR WAREHOUSES REGULATIONS FOR THE UNITED STATES WAREHOUSE ACT General Provisions §...

  14. 7 CFR 550.5 - Competition.

    Code of Federal Regulations, 2010 CFR

    2010-01-01

    ... 7 Agriculture 6 2010-01-01 2010-01-01 false Competition. 550.5 Section 550.5 Agriculture... Competition. REE agencies may enter into non-assistance cooperative agreements, as authorized by this part, without regard to any requirements for competition. (7 U.S.C. 3318(e))....

  15. 7 CFR 550.5 - Competition.

    Code of Federal Regulations, 2011 CFR

    2011-01-01

    ... 7 Agriculture 6 2011-01-01 2011-01-01 false Competition. 550.5 Section 550.5 Agriculture... Competition. REE agencies may enter into non-assistance cooperative agreements, as authorized by this part, without regard to any requirements for competition. (7 U.S.C. 3318(e))....

  16. 18 CFR 5.7 - Tribal consultation.

    Code of Federal Regulations, 2013 CFR

    2013-04-01

    ... 18 Conservation of Power and Water Resources 1 2013-04-01 2013-04-01 false Tribal consultation. 5.7 Section 5.7 Conservation of Power and Water Resources FEDERAL ENERGY REGULATORY COMMISSION, DEPARTMENT OF ENERGY REGULATIONS UNDER THE FEDERAL POWER ACT INTEGRATED LICENSE APPLICATION PROCESS §...

  17. 18 CFR 5.7 - Tribal consultation.

    Code of Federal Regulations, 2012 CFR

    2012-04-01

    ... 18 Conservation of Power and Water Resources 1 2012-04-01 2012-04-01 false Tribal consultation. 5.7 Section 5.7 Conservation of Power and Water Resources FEDERAL ENERGY REGULATORY COMMISSION, DEPARTMENT OF ENERGY REGULATIONS UNDER THE FEDERAL POWER ACT INTEGRATED LICENSE APPLICATION PROCESS §...

  18. 18 CFR 5.7 - Tribal consultation.

    Code of Federal Regulations, 2010 CFR

    2010-04-01

    ... 18 Conservation of Power and Water Resources 1 2010-04-01 2010-04-01 false Tribal consultation. 5.7 Section 5.7 Conservation of Power and Water Resources FEDERAL ENERGY REGULATORY COMMISSION, DEPARTMENT OF ENERGY REGULATIONS UNDER THE FEDERAL POWER ACT INTEGRATED LICENSE APPLICATION PROCESS §...

  19. 7 CFR 550.5 - Competition.

    Code of Federal Regulations, 2012 CFR

    2012-01-01

    ... 7 Agriculture 6 2012-01-01 2012-01-01 false Competition. 550.5 Section 550.5 Agriculture... Competition. REE agencies may enter into non-assistance cooperative agreements, as authorized by this part, without regard to any requirements for competition. (7 U.S.C. 3318(e))....

  20. 7 CFR 550.5 - Competition.

    Code of Federal Regulations, 2013 CFR

    2013-01-01

    ... 7 Agriculture 6 2013-01-01 2013-01-01 false Competition. 550.5 Section 550.5 Agriculture... Competition. REE agencies may enter into non-assistance cooperative agreements, as authorized by this part, without regard to any requirements for competition. (7 U.S.C. 3318(e))....

  1. 7 CFR 550.5 - Competition.

    Code of Federal Regulations, 2014 CFR

    2014-01-01

    ... 7 Agriculture 6 2014-01-01 2014-01-01 false Competition. 550.5 Section 550.5 Agriculture... Competition. REE agencies may enter into non-assistance cooperative agreements, as authorized by this part, without regard to any requirements for competition. (7 U.S.C. 3318(e))....

  2. 7 CFR 770.5 - Loan limitations.

    Code of Federal Regulations, 2011 CFR

    2011-01-01

    ... 7 Agriculture 7 2011-01-01 2011-01-01 false Loan limitations. 770.5 Section 770.5 Agriculture Regulations of the Department of Agriculture (Continued) FARM SERVICE AGENCY, DEPARTMENT OF AGRICULTURE... will contribute to excessive erosion of highly erodible land or to the conversion of wetlands...

  3. 7 CFR 770.5 - Loan limitations.

    Code of Federal Regulations, 2014 CFR

    2014-01-01

    ... 7 Agriculture 7 2014-01-01 2014-01-01 false Loan limitations. 770.5 Section 770.5 Agriculture Regulations of the Department of Agriculture (Continued) FARM SERVICE AGENCY, DEPARTMENT OF AGRICULTURE... will contribute to excessive erosion of highly erodible land or to the conversion of wetlands...

  4. 7 CFR 1126.5 - Distributing plant.

    Code of Federal Regulations, 2010 CFR

    2010-01-01

    ... 7 Agriculture 9 2010-01-01 2009-01-01 true Distributing plant. 1126.5 Section 1126.5 Agriculture Regulations of the Department of Agriculture (Continued) AGRICULTURAL MARKETING SERVICE (Marketing Agreements... Handling Definitions § 1126.5 Distributing plant. See § 1000.5....

  5. 7 CFR 1124.5 - Distributing plant.

    Code of Federal Regulations, 2011 CFR

    2011-01-01

    ... 7 Agriculture 9 2011-01-01 2011-01-01 false Distributing plant. 1124.5 Section 1124.5 Agriculture Regulations of the Department of Agriculture (Continued) AGRICULTURAL MARKETING SERVICE (Marketing Agreements... Regulating Handling Definitions § 1124.5 Distributing plant. See § 1000.5....

  6. 7 CFR 1006.5 - Distributing plant.

    Code of Federal Regulations, 2010 CFR

    2010-01-01

    ... 7 Agriculture 9 2010-01-01 2009-01-01 true Distributing plant. 1006.5 Section 1006.5 Agriculture Regulations of the Department of Agriculture (Continued) AGRICULTURAL MARKETING SERVICE (Marketing Agreements... Handling Definitions § 1006.5 Distributing plant. See § 1000.5....

  7. 7 CFR 1005.5 - Distributing plant.

    Code of Federal Regulations, 2011 CFR

    2011-01-01

    ... 7 Agriculture 9 2011-01-01 2011-01-01 false Distributing plant. 1005.5 Section 1005.5 Agriculture Regulations of the Department of Agriculture (Continued) AGRICULTURAL MARKETING SERVICE (Marketing Agreements... Handling Definitions § 1005.5 Distributing plant. See § 1000.5....

  8. 7 CFR 1033.5 - Distributing plant.

    Code of Federal Regulations, 2010 CFR

    2010-01-01

    ... 7 Agriculture 9 2010-01-01 2009-01-01 true Distributing plant. 1033.5 Section 1033.5 Agriculture Regulations of the Department of Agriculture (Continued) AGRICULTURAL MARKETING SERVICE (Marketing Agreements... Handling Definitions § 1033.5 Distributing plant. See § 1000.5....

  9. 7 CFR 1032.5 - Distributing plant.

    Code of Federal Regulations, 2010 CFR

    2010-01-01

    ... 7 Agriculture 9 2010-01-01 2009-01-01 true Distributing plant. 1032.5 Section 1032.5 Agriculture Regulations of the Department of Agriculture (Continued) AGRICULTURAL MARKETING SERVICE (Marketing Agreements... Handling Definitions § 1032.5 Distributing plant. See § 1000.5....

  10. 7 CFR 1007.5 - Distributing plant.

    Code of Federal Regulations, 2011 CFR

    2011-01-01

    ... 7 Agriculture 9 2011-01-01 2011-01-01 false Distributing plant. 1007.5 Section 1007.5 Agriculture Regulations of the Department of Agriculture (Continued) AGRICULTURAL MARKETING SERVICE (Marketing Agreements... Handling Definitions § 1007.5 Distributing plant. See § 1000.5....

  11. 7 CFR 1005.5 - Distributing plant.

    Code of Federal Regulations, 2010 CFR

    2010-01-01

    ... 7 Agriculture 9 2010-01-01 2009-01-01 true Distributing plant. 1005.5 Section 1005.5 Agriculture Regulations of the Department of Agriculture (Continued) AGRICULTURAL MARKETING SERVICE (Marketing Agreements... Handling Definitions § 1005.5 Distributing plant. See § 1000.5....

  12. 7 CFR 1033.5 - Distributing plant.

    Code of Federal Regulations, 2011 CFR

    2011-01-01

    ... 7 Agriculture 9 2011-01-01 2011-01-01 false Distributing plant. 1033.5 Section 1033.5 Agriculture Regulations of the Department of Agriculture (Continued) AGRICULTURAL MARKETING SERVICE (Marketing Agreements... Handling Definitions § 1033.5 Distributing plant. See § 1000.5....

  13. 7 CFR 1001.5 - Distributing plant.

    Code of Federal Regulations, 2010 CFR

    2010-01-01

    ... 7 Agriculture 9 2010-01-01 2009-01-01 true Distributing plant. 1001.5 Section 1001.5 Agriculture Regulations of the Department of Agriculture (Continued) AGRICULTURAL MARKETING SERVICE (Marketing Agreements... Handling Definitions § 1001.5 Distributing plant. See § 1000.5....

  14. 7 CFR 1032.5 - Distributing plant.

    Code of Federal Regulations, 2011 CFR

    2011-01-01

    ... 7 Agriculture 9 2011-01-01 2011-01-01 false Distributing plant. 1032.5 Section 1032.5 Agriculture Regulations of the Department of Agriculture (Continued) AGRICULTURAL MARKETING SERVICE (Marketing Agreements... Handling Definitions § 1032.5 Distributing plant. See § 1000.5....

  15. 7 CFR 1007.5 - Distributing plant.

    Code of Federal Regulations, 2010 CFR

    2010-01-01

    ... 7 Agriculture 9 2010-01-01 2009-01-01 true Distributing plant. 1007.5 Section 1007.5 Agriculture Regulations of the Department of Agriculture (Continued) AGRICULTURAL MARKETING SERVICE (Marketing Agreements... Handling Definitions § 1007.5 Distributing plant. See § 1000.5....

  16. 7 CFR 1131.5 - Distributing plant.

    Code of Federal Regulations, 2011 CFR

    2011-01-01

    ... 7 Agriculture 9 2011-01-01 2011-01-01 false Distributing plant. 1131.5 Section 1131.5 Agriculture Regulations of the Department of Agriculture (Continued) AGRICULTURAL MARKETING SERVICE (Marketing Agreements... Handling Definitions § 1131.5 Distributing plant. See § 1000.5....

  17. 7 CFR 1030.5 - Distributing plant.

    Code of Federal Regulations, 2010 CFR

    2010-01-01

    ... 7 Agriculture 9 2010-01-01 2009-01-01 true Distributing plant. 1030.5 Section 1030.5 Agriculture Regulations of the Department of Agriculture (Continued) AGRICULTURAL MARKETING SERVICE (Marketing Agreements... Handling Definitions § 1030.5 Distributing plant. See § 1000.5....

  18. 7 CFR 1006.5 - Distributing plant.

    Code of Federal Regulations, 2011 CFR

    2011-01-01

    ... 7 Agriculture 9 2011-01-01 2011-01-01 false Distributing plant. 1006.5 Section 1006.5 Agriculture Regulations of the Department of Agriculture (Continued) AGRICULTURAL MARKETING SERVICE (Marketing Agreements... Handling Definitions § 1006.5 Distributing plant. See § 1000.5....

  19. 7 CFR 1124.5 - Distributing plant.

    Code of Federal Regulations, 2010 CFR

    2010-01-01

    ... 7 Agriculture 9 2010-01-01 2009-01-01 true Distributing plant. 1124.5 Section 1124.5 Agriculture Regulations of the Department of Agriculture (Continued) AGRICULTURAL MARKETING SERVICE (Marketing Agreements... Regulating Handling Definitions § 1124.5 Distributing plant. See § 1000.5....

  20. 7 CFR 1131.5 - Distributing plant.

    Code of Federal Regulations, 2010 CFR

    2010-01-01

    ... 7 Agriculture 9 2010-01-01 2009-01-01 true Distributing plant. 1131.5 Section 1131.5 Agriculture Regulations of the Department of Agriculture (Continued) AGRICULTURAL MARKETING SERVICE (Marketing Agreements... Handling Definitions § 1131.5 Distributing plant. See § 1000.5....

  1. 7 CFR 1030.5 - Distributing plant.

    Code of Federal Regulations, 2011 CFR

    2011-01-01

    ... 7 Agriculture 9 2011-01-01 2011-01-01 false Distributing plant. 1030.5 Section 1030.5 Agriculture Regulations of the Department of Agriculture (Continued) AGRICULTURAL MARKETING SERVICE (Marketing Agreements... Handling Definitions § 1030.5 Distributing plant. See § 1000.5....

  2. 7 CFR 1001.5 - Distributing plant.

    Code of Federal Regulations, 2011 CFR

    2011-01-01

    ... 7 Agriculture 9 2011-01-01 2011-01-01 false Distributing plant. 1001.5 Section 1001.5 Agriculture Regulations of the Department of Agriculture (Continued) AGRICULTURAL MARKETING SERVICE (Marketing Agreements... Handling Definitions § 1001.5 Distributing plant. See § 1000.5....

  3. 7 CFR 1126.5 - Distributing plant.

    Code of Federal Regulations, 2011 CFR

    2011-01-01

    ... 7 Agriculture 9 2011-01-01 2011-01-01 false Distributing plant. 1126.5 Section 1126.5 Agriculture Regulations of the Department of Agriculture (Continued) AGRICULTURAL MARKETING SERVICE (Marketing Agreements... Handling Definitions § 1126.5 Distributing plant. See § 1000.5....

  4. 7 CFR 356.5 - Bonded release.

    Code of Federal Regulations, 2012 CFR

    2012-01-01

    ... 7 Agriculture 5 2012-01-01 2012-01-01 false Bonded release. 356.5 Section 356.5 Agriculture Regulations of the Department of Agriculture (Continued) ANIMAL AND PLANT HEALTH INSPECTION SERVICE, DEPARTMENT OF AGRICULTURE FORFEITURE PROCEDURES § 356.5 Bonded release. (a) The Deputy Administrator...

  5. 7 CFR 1033.5 - Distributing plant.

    Code of Federal Regulations, 2013 CFR

    2013-01-01

    ... 7 Agriculture 9 2013-01-01 2013-01-01 false Distributing plant. 1033.5 Section 1033.5 Agriculture Regulations of the Department of Agriculture (Continued) AGRICULTURAL MARKETING SERVICE (MARKETING AGREEMENTS... Handling Definitions § 1033.5 Distributing plant. See § 1000.5....

  6. 7 CFR 1005.5 - Distributing plant.

    Code of Federal Regulations, 2012 CFR

    2012-01-01

    ... 7 Agriculture 9 2012-01-01 2012-01-01 false Distributing plant. 1005.5 Section 1005.5 Agriculture Regulations of the Department of Agriculture (Continued) AGRICULTURAL MARKETING SERVICE (Marketing Agreements... Handling Definitions § 1005.5 Distributing plant. See § 1000.5....

  7. 7 CFR 1007.5 - Distributing plant.

    Code of Federal Regulations, 2012 CFR

    2012-01-01

    ... 7 Agriculture 9 2012-01-01 2012-01-01 false Distributing plant. 1007.5 Section 1007.5 Agriculture Regulations of the Department of Agriculture (Continued) AGRICULTURAL MARKETING SERVICE (Marketing Agreements... Handling Definitions § 1007.5 Distributing plant. See § 1000.5....

  8. 7 CFR 1124.5 - Distributing plant.

    Code of Federal Regulations, 2012 CFR

    2012-01-01

    ... 7 Agriculture 9 2012-01-01 2012-01-01 false Distributing plant. 1124.5 Section 1124.5 Agriculture Regulations of the Department of Agriculture (Continued) AGRICULTURAL MARKETING SERVICE (Marketing Agreements... Regulating Handling Definitions § 1124.5 Distributing plant. See § 1000.5....

  9. 7 CFR 1124.5 - Distributing plant.

    Code of Federal Regulations, 2013 CFR

    2013-01-01

    ... 7 Agriculture 9 2013-01-01 2013-01-01 false Distributing plant. 1124.5 Section 1124.5 Agriculture Regulations of the Department of Agriculture (Continued) AGRICULTURAL MARKETING SERVICE (MARKETING AGREEMENTS... Regulating Handling Definitions § 1124.5 Distributing plant. See § 1000.5....

  10. 7 CFR 1007.5 - Distributing plant.

    Code of Federal Regulations, 2014 CFR

    2014-01-01

    ... 7 Agriculture 9 2014-01-01 2013-01-01 true Distributing plant. 1007.5 Section 1007.5 Agriculture Regulations of the Department of Agriculture (Continued) AGRICULTURAL MARKETING SERVICE (MARKETING AGREEMENTS... Handling Definitions § 1007.5 Distributing plant. See § 1000.5....

  11. 7 CFR 1126.5 - Distributing plant.

    Code of Federal Regulations, 2013 CFR

    2013-01-01

    ... 7 Agriculture 9 2013-01-01 2013-01-01 false Distributing plant. 1126.5 Section 1126.5 Agriculture Regulations of the Department of Agriculture (Continued) AGRICULTURAL MARKETING SERVICE (MARKETING AGREEMENTS... Handling Definitions § 1126.5 Distributing plant. See § 1000.5....

  12. 7 CFR 1006.5 - Distributing plant.

    Code of Federal Regulations, 2013 CFR

    2013-01-01

    ... 7 Agriculture 9 2013-01-01 2013-01-01 false Distributing plant. 1006.5 Section 1006.5 Agriculture Regulations of the Department of Agriculture (Continued) AGRICULTURAL MARKETING SERVICE (MARKETING AGREEMENTS... Handling Definitions § 1006.5 Distributing plant. See § 1000.5....

  13. 7 CFR 1124.5 - Distributing plant.

    Code of Federal Regulations, 2014 CFR

    2014-01-01

    ... 7 Agriculture 9 2014-01-01 2013-01-01 true Distributing plant. 1124.5 Section 1124.5 Agriculture Regulations of the Department of Agriculture (Continued) AGRICULTURAL MARKETING SERVICE (MARKETING AGREEMENTS... Regulating Handling Definitions § 1124.5 Distributing plant. See § 1000.5....

  14. 7 CFR 1032.5 - Distributing plant.

    Code of Federal Regulations, 2014 CFR

    2014-01-01

    ... 7 Agriculture 9 2014-01-01 2013-01-01 true Distributing plant. 1032.5 Section 1032.5 Agriculture Regulations of the Department of Agriculture (Continued) AGRICULTURAL MARKETING SERVICE (MARKETING AGREEMENTS... Handling Definitions § 1032.5 Distributing plant. See § 1000.5....

  15. 7 CFR 1033.5 - Distributing plant.

    Code of Federal Regulations, 2012 CFR

    2012-01-01

    ... 7 Agriculture 9 2012-01-01 2012-01-01 false Distributing plant. 1033.5 Section 1033.5 Agriculture Regulations of the Department of Agriculture (Continued) AGRICULTURAL MARKETING SERVICE (Marketing Agreements... Handling Definitions § 1033.5 Distributing plant. See § 1000.5....

  16. 7 CFR 1001.5 - Distributing plant.

    Code of Federal Regulations, 2013 CFR

    2013-01-01

    ... 7 Agriculture 9 2013-01-01 2013-01-01 false Distributing plant. 1001.5 Section 1001.5 Agriculture Regulations of the Department of Agriculture (Continued) AGRICULTURAL MARKETING SERVICE (MARKETING AGREEMENTS... Handling Definitions § 1001.5 Distributing plant. See § 1000.5....

  17. 7 CFR 1126.5 - Distributing plant.

    Code of Federal Regulations, 2014 CFR

    2014-01-01

    ... 7 Agriculture 9 2014-01-01 2013-01-01 true Distributing plant. 1126.5 Section 1126.5 Agriculture Regulations of the Department of Agriculture (Continued) AGRICULTURAL MARKETING SERVICE (MARKETING AGREEMENTS... Handling Definitions § 1126.5 Distributing plant. See § 1000.5....

  18. 7 CFR 1005.5 - Distributing plant.

    Code of Federal Regulations, 2014 CFR

    2014-01-01

    ... 7 Agriculture 9 2014-01-01 2013-01-01 true Distributing plant. 1005.5 Section 1005.5 Agriculture Regulations of the Department of Agriculture (Continued) AGRICULTURAL MARKETING SERVICE (MARKETING AGREEMENTS... Handling Definitions § 1005.5 Distributing plant. See § 1000.5....

  19. 7 CFR 1131.5 - Distributing plant.

    Code of Federal Regulations, 2014 CFR

    2014-01-01

    ... 7 Agriculture 9 2014-01-01 2013-01-01 true Distributing plant. 1131.5 Section 1131.5 Agriculture Regulations of the Department of Agriculture (Continued) AGRICULTURAL MARKETING SERVICE (MARKETING AGREEMENTS... Handling Definitions § 1131.5 Distributing plant. See § 1000.5....

  20. 7 CFR 1131.5 - Distributing plant.

    Code of Federal Regulations, 2012 CFR

    2012-01-01

    ... 7 Agriculture 9 2012-01-01 2012-01-01 false Distributing plant. 1131.5 Section 1131.5 Agriculture Regulations of the Department of Agriculture (Continued) AGRICULTURAL MARKETING SERVICE (Marketing Agreements... Handling Definitions § 1131.5 Distributing plant. See § 1000.5....

  1. 7 CFR 1126.5 - Distributing plant.

    Code of Federal Regulations, 2012 CFR

    2012-01-01

    ... 7 Agriculture 9 2012-01-01 2012-01-01 false Distributing plant. 1126.5 Section 1126.5 Agriculture Regulations of the Department of Agriculture (Continued) AGRICULTURAL MARKETING SERVICE (Marketing Agreements... Handling Definitions § 1126.5 Distributing plant. See § 1000.5....

  2. 7 CFR 1005.5 - Distributing plant.

    Code of Federal Regulations, 2013 CFR

    2013-01-01

    ... 7 Agriculture 9 2013-01-01 2013-01-01 false Distributing plant. 1005.5 Section 1005.5 Agriculture Regulations of the Department of Agriculture (Continued) AGRICULTURAL MARKETING SERVICE (MARKETING AGREEMENTS... Handling Definitions § 1005.5 Distributing plant. See § 1000.5....

  3. 7 CFR 1007.5 - Distributing plant.

    Code of Federal Regulations, 2013 CFR

    2013-01-01

    ... 7 Agriculture 9 2013-01-01 2013-01-01 false Distributing plant. 1007.5 Section 1007.5 Agriculture Regulations of the Department of Agriculture (Continued) AGRICULTURAL MARKETING SERVICE (MARKETING AGREEMENTS... Handling Definitions § 1007.5 Distributing plant. See § 1000.5....

  4. 7 CFR 1131.5 - Distributing plant.

    Code of Federal Regulations, 2013 CFR

    2013-01-01

    ... 7 Agriculture 9 2013-01-01 2013-01-01 false Distributing plant. 1131.5 Section 1131.5 Agriculture Regulations of the Department of Agriculture (Continued) AGRICULTURAL MARKETING SERVICE (MARKETING AGREEMENTS... Handling Definitions § 1131.5 Distributing plant. See § 1000.5....

  5. 7 CFR 1001.5 - Distributing plant.

    Code of Federal Regulations, 2012 CFR

    2012-01-01

    ... 7 Agriculture 9 2012-01-01 2012-01-01 false Distributing plant. 1001.5 Section 1001.5 Agriculture Regulations of the Department of Agriculture (Continued) AGRICULTURAL MARKETING SERVICE (Marketing Agreements... Handling Definitions § 1001.5 Distributing plant. See § 1000.5....

  6. 7 CFR 1032.5 - Distributing plant.

    Code of Federal Regulations, 2013 CFR

    2013-01-01

    ... 7 Agriculture 9 2013-01-01 2013-01-01 false Distributing plant. 1032.5 Section 1032.5 Agriculture Regulations of the Department of Agriculture (Continued) AGRICULTURAL MARKETING SERVICE (MARKETING AGREEMENTS... Handling Definitions § 1032.5 Distributing plant. See § 1000.5....

  7. 7 CFR 1032.5 - Distributing plant.

    Code of Federal Regulations, 2012 CFR

    2012-01-01

    ... 7 Agriculture 9 2012-01-01 2012-01-01 false Distributing plant. 1032.5 Section 1032.5 Agriculture Regulations of the Department of Agriculture (Continued) AGRICULTURAL MARKETING SERVICE (Marketing Agreements... Handling Definitions § 1032.5 Distributing plant. See § 1000.5....

  8. 7 CFR 1001.5 - Distributing plant.

    Code of Federal Regulations, 2014 CFR

    2014-01-01

    ... 7 Agriculture 9 2014-01-01 2013-01-01 true Distributing plant. 1001.5 Section 1001.5 Agriculture Regulations of the Department of Agriculture (Continued) AGRICULTURAL MARKETING SERVICE (MARKETING AGREEMENTS... Handling Definitions § 1001.5 Distributing plant. See § 1000.5....

  9. 7 CFR 1033.5 - Distributing plant.

    Code of Federal Regulations, 2014 CFR

    2014-01-01

    ... 7 Agriculture 9 2014-01-01 2013-01-01 true Distributing plant. 1033.5 Section 1033.5 Agriculture Regulations of the Department of Agriculture (Continued) AGRICULTURAL MARKETING SERVICE (MARKETING AGREEMENTS... Handling Definitions § 1033.5 Distributing plant. See § 1000.5....

  10. 7 CFR 1006.5 - Distributing plant.

    Code of Federal Regulations, 2014 CFR

    2014-01-01

    ... 7 Agriculture 9 2014-01-01 2013-01-01 true Distributing plant. 1006.5 Section 1006.5 Agriculture Regulations of the Department of Agriculture (Continued) AGRICULTURAL MARKETING SERVICE (MARKETING AGREEMENTS... Handling Definitions § 1006.5 Distributing plant. See § 1000.5....

  11. 7 CFR 1030.5 - Distributing plant.

    Code of Federal Regulations, 2013 CFR

    2013-01-01

    ... 7 Agriculture 9 2013-01-01 2013-01-01 false Distributing plant. 1030.5 Section 1030.5 Agriculture Regulations of the Department of Agriculture (Continued) AGRICULTURAL MARKETING SERVICE (MARKETING AGREEMENTS... Handling Definitions § 1030.5 Distributing plant. See § 1000.5....

  12. 7 CFR 1030.5 - Distributing plant.

    Code of Federal Regulations, 2014 CFR

    2014-01-01

    ... 7 Agriculture 9 2014-01-01 2013-01-01 true Distributing plant. 1030.5 Section 1030.5 Agriculture Regulations of the Department of Agriculture (Continued) AGRICULTURAL MARKETING SERVICE (MARKETING AGREEMENTS... Handling Definitions § 1030.5 Distributing plant. See § 1000.5....

  13. 7 CFR 1006.5 - Distributing plant.

    Code of Federal Regulations, 2012 CFR

    2012-01-01

    ... 7 Agriculture 9 2012-01-01 2012-01-01 false Distributing plant. 1006.5 Section 1006.5 Agriculture Regulations of the Department of Agriculture (Continued) AGRICULTURAL MARKETING SERVICE (Marketing Agreements... Handling Definitions § 1006.5 Distributing plant. See § 1000.5....

  14. 7 CFR 1030.5 - Distributing plant.

    Code of Federal Regulations, 2012 CFR

    2012-01-01

    ... 7 Agriculture 9 2012-01-01 2012-01-01 false Distributing plant. 1030.5 Section 1030.5 Agriculture Regulations of the Department of Agriculture (Continued) AGRICULTURAL MARKETING SERVICE (Marketing Agreements... Handling Definitions § 1030.5 Distributing plant. See § 1000.5....

  15. Na7Cr4(P2O7)4PO4

    PubMed Central

    Bourguiba Fakhar, Noura; Zid, Mohamed Faouzi; Driss, Ahmed

    2013-01-01

    The title compound, hepta­sodium tetra­chromium(III) tetra­kis­(diphosphate) orthophosphate, was synthesized by solid-state reaction. Its structure is isotypic with that of Na7 M 4(P2O7)4PO4 (M = In, Al) compounds and is made up from a three-dimensional [(CrP2O7)4PO4]7− framework with channels running along [001]. The three Na+ cations are located in the voids of the framework. One of the cations is situated on a general position, one is equally disordered around a twofold rotation axis and one is on a fourfold rotoinversion axis. The isolated PO4 tetra­hedron of the anionic framework is also situated on the -4 axis. Structural relationships between the title compound and different diphosphates containing MP2O11 units (M = Mo, V) are discussed. PMID:23723751

  16. Prospecting Lighting Applications with Ligand Field Tools and Density Functional Theory: A First-Principles Account of the 4f(7)-4f(6)5d(1) Luminescence of CsMgBr3:Eu(2+).

    PubMed

    Ramanantoanina, Harry; Cimpoesu, Fanica; Göttel, Christian; Sahnoun, Mohammed; Herden, Benjamin; Suta, Markus; Wickleder, Claudia; Urland, Werner; Daul, Claude

    2015-09-08

    The most efficient way to provide domestic lighting nowadays is by light-emitting diodes (LEDs) technology combined with phosphors shifting the blue and UV emission toward a desirable sunlight spectrum. A route in the quest for warm-white light goes toward the discovery and tuning of the lanthanide-based phosphors, a difficult task, in experimental and technical respects. A proper theoretical approach, which is also complicated at the conceptual level and in computing efforts, is however a profitable complement, offering valuable structure-property rationale as a guideline in the search of the best materials. The Eu(2+)-based systems are the prototypes for ideal phosphors, exhibiting a wide range of visible light emission. Using the ligand field concepts in conjunction with density functional theory (DFT), conducted in nonroutine manner, we develop a nonempirical procedure to investigate the 4f(7)-4f(6)5d(1) luminescence of Eu(2+) in the environment of arbitrary ligands, applied here on the CsMgBr3:Eu(2+)-doped material. Providing a salient methodology for the extraction of the relevant ligand field and related parameters from DFT calculations and encompassing the bottleneck of handling large matrices in a model Hamiltonian based on the whole set of 33,462 states, we obtained an excellent match with the experimental spectrum, from first-principles, without any fit or adjustment. This proves that the ligand field density functional theory methodology can be used in the assessment of new materials and rational property design.

  17. Molecular and crystalline structure of cycloheptanespiro-3'(4'H)-6',7',8',9'-tetrahydrocyclohexa[b][1,4]thiazole-2'(5'H)-thione from powder synchrotron X-ray diffraction data.

    PubMed

    Avila, Edward E; Mora, Asiloé J; Delgado, Gerzon E; Contreras, Ricardo R; Fitch, Andrew N; Brunelli, Michela

    2008-04-01

    A series of bidentate nitrogen-sulfur pro-ligands has been designed and synthesized with the purpose of introducing a structural modification that favours the tetrahedral site distortions of metalloprotein systems with metallic centers surrounded by ligands containing two N atoms and two S atoms as donor groups. Some of these new pro-ligands were obtained only as powders. Here we present the molecular and crystalline structure of cycloheptanespiro-3'(4'H)-6',7',8',9'-tetrahydrocyclohexa[b][1,4]thiazole-2'(5'H)-thione (I) solved and refined from powder synchrotron X-ray diffraction data. Two independent molecules comprising a total of 36 non-H atoms were obtained from the direct-methods solution and refined against the powder X-ray diffraction data using the Rietveld method. The molecular conformations of the heterocyclic benzothiazine ring, the fused heptenyl ring and the heptanyl spiro ring are thoroughly discussed and compared with VASP theoretical calculations and other related structures. The packing of molecules in (I) is based on hydrogen bonds of the type N-H...S and hydrophobic C-H interactions.

  18. Antidepressant-like activity of 2-(4-phenylpiperazin-1-yl)-1, 8-naphthyridine-3-carboxylic acid (7a), a 5-HT₃ receptor antagonist in behaviour based rodent models: evidence for the involvement of serotonergic system.

    PubMed

    Gautam, Baldev Kumar; Jindal, Ankur; Dhar, Arghya Kusum; Mahesh, Radhakrishnan

    2013-08-01

    The present study was designed to investigate the putative antidepressant-like activity of 7a, a 5-HT₃ receptor antagonist, (although indirect evidence of 5-HT3 antagonism) with an optimal log P (3.35) and pA₂ value (7.6) greater than ondansetron (pA₂--6.6) using behavioural tests battery of depression. Acute treatment of 7a (0.5-2 mg/kg, i.p.) in mice produced antidepressant-like effects in forced swim test (FST) and tail suspension test (TST) without affecting the baseline locomotion in actophotometer test in mice. Moreover, the combination of a sub-effective dose of 7a (0.25 mg/kg, i.p.) and fluoxetine (5 mg/kg, i.p.) produced an anti-immobility effect in mouse FST. Pretreatment of mice with p-chlorophenylalanine methyl ester (PCPA; 100 mg/kg, i.p., an inhibitor of serotonin (5-HT) synthesis, for 4 consecutive days) and 1-(m-Chlorophenyl)-biguanide (mCPBG, 10 mg/kg, i.p., a 5-HT₃ receptor agonist) prevented the anti-immobility effects of 7a (2 mg/kg, i.p.) in the mouse FST. In addition, 7a (0.5-2 mg/kg, i.p.) treatment also potentiated the 5-hydroxytryptophan (5-HTP) and pargyline induced head twitch response in mice. Furthermore, sub-chronic treatment (14 days) with 7a (0.5-2 mg/kg, i.p.) and paroxetine (10 mg/kg, i.p.) significantly attenuated the behavioural anomalies induced by bilateral olfactory bulbectomy in rats in a modified open field paradigm. These results suggest that the antidepressant-like action of 7a may be mediated by an interaction with the serotonergic system and this molecule should be further investigated as an alternative therapeutic approach for the treatment of depression.

  19. Naturally resident and exogenously applied T4-like and T5-like bacteriophages can reduce Escherichia coli O157:H7 levels in sheep guts

    Technology Transfer Automated Retrieval System (TEKTRAN)

    In preparing sheep for an in vivo Escherichia coli O157:H7 eradication trial, we found that 20/39 members of a single flock were naturally colonized by O157:H7-infecting phages. Characterization showed these were all one phage type (subsequently named CEV2) infecting 15/16 O157:H7, 7/72 ECOR, and c...

  20. Crystal structure of methyl (3RS,4SR,4aRS,11aRS,11bSR)-5-oxo-3,4,4a,5,7,8,9,10,11,11a-deca-hydro-3,11b-ep-oxy-azepino[2,1-a]iso-indole-4-carboxyl-ate.

    PubMed

    Toze, Flavien A A; Poplevin, Dmitry S; Zubkov, Fedor I; Nikitina, Eugeniya V; Porras, Ciara; Khrustalev, Victor N

    2015-10-01

    The title compound, C15H19NO4, is the a product of the esterification of the corresponding carbonic acid with methanol. The mol-ecule comprises a fused tetra-cyclic system containing three five-membered rings (2-pyrrolidinone, tetra-hydro-furan and di-hydro-furan) and one seven-membered ring (azepane). The five-membered rings have the usual envelope conformations, with the quaternary C atom being the flap atom for the 2-pyrrolidinone ring, and the ether O atom being the common flap atom for the remaining rings. The seven-membered azepane ring adopts a chair conformation with the methine and middle methyl-ene C atoms lying above and below the mean plane defined by the remaining five atoms. The carboxyl-ate substituent is rotated by 77.56 (5)° with respect to the base plane of the tetra-hydro-furan ring. In the crystal, the mol-ecules are bound by weak C-H⋯O hydrogen-bonding inter-actions into puckered layers parallel to (001).

  1. Crystal structure of methyl (3RS,4SR,4aRS,11aRS,11bSR)-5-oxo-3,4,4a,5,7,8,9,10,11,11a-deca­hydro-3,11b-ep­oxy­azepino[2,1-a]iso­indole-4-carboxyl­ate

    PubMed Central

    Toze, Flavien A. A.; Poplevin, Dmitry S.; Zubkov, Fedor I.; Nikitina, Eugeniya V.; Porras, Ciara; Khrustalev, Victor N.

    2015-01-01

    The title compound, C15H19NO4, is the a product of the esterification of the corresponding carbonic acid with methanol. The mol­ecule comprises a fused tetra­cyclic system containing three five-membered rings (2-pyrrolidinone, tetra­hydro­furan and di­hydro­furan) and one seven-membered ring (azepane). The five-membered rings have the usual envelope conformations, with the quaternary C atom being the flap atom for the 2-pyrrolidinone ring, and the ether O atom being the common flap atom for the remaining rings. The seven-membered azepane ring adopts a chair conformation with the methine and middle methyl­ene C atoms lying above and below the mean plane defined by the remaining five atoms. The carboxyl­ate substituent is rotated by 77.56 (5)° with respect to the base plane of the tetra­hydro­furan ring. In the crystal, the mol­ecules are bound by weak C—H⋯O hydrogen-bonding inter­actions into puckered layers parallel to (001). PMID:26594446

  2. 42 CFR 4.7 - Fees.

    Code of Federal Regulations, 2013 CFR

    2013-10-01

    ... 42 Public Health 1 2013-10-01 2013-10-01 false Fees. 4.7 Section 4.7 Public Health PUBLIC HEALTH SERVICE, DEPARTMENT OF HEALTH AND HUMAN SERVICES GENERAL PROVISIONS NATIONAL LIBRARY OF MEDICINE § 4.7 Fees. The Director may charge reasonable fees for any service provided by the Library under this...

  3. 42 CFR 4.7 - Fees.

    Code of Federal Regulations, 2012 CFR

    2012-10-01

    ... 42 Public Health 1 2012-10-01 2012-10-01 false Fees. 4.7 Section 4.7 Public Health PUBLIC HEALTH SERVICE, DEPARTMENT OF HEALTH AND HUMAN SERVICES GENERAL PROVISIONS NATIONAL LIBRARY OF MEDICINE § 4.7 Fees. The Director may charge reasonable fees for any service provided by the Library under this...

  4. 42 CFR 4.7 - Fees.

    Code of Federal Regulations, 2014 CFR

    2014-10-01

    ... 42 Public Health 1 2014-10-01 2014-10-01 false Fees. 4.7 Section 4.7 Public Health PUBLIC HEALTH SERVICE, DEPARTMENT OF HEALTH AND HUMAN SERVICES GENERAL PROVISIONS NATIONAL LIBRARY OF MEDICINE § 4.7 Fees. The Director may charge reasonable fees for any service provided by the Library under this...

  5. 42 CFR 4.7 - Fees.

    Code of Federal Regulations, 2011 CFR

    2011-10-01

    ... 42 Public Health 1 2011-10-01 2011-10-01 false Fees. 4.7 Section 4.7 Public Health PUBLIC HEALTH SERVICE, DEPARTMENT OF HEALTH AND HUMAN SERVICES GENERAL PROVISIONS NATIONAL LIBRARY OF MEDICINE § 4.7 Fees. The Director may charge reasonable fees for any service provided by the Library under this...

  6. 42 CFR 4.7 - Fees.

    Code of Federal Regulations, 2010 CFR

    2010-10-01

    ... 42 Public Health 1 2010-10-01 2010-10-01 false Fees. 4.7 Section 4.7 Public Health PUBLIC HEALTH SERVICE, DEPARTMENT OF HEALTH AND HUMAN SERVICES GENERAL PROVISIONS NATIONAL LIBRARY OF MEDICINE § 4.7 Fees. The Director may charge reasonable fees for any service provided by the Library under this...

  7. 49 CFR 7.4 - Publication required.

    Code of Federal Regulations, 2013 CFR

    2013-10-01

    ... 49 Transportation 1 2013-10-01 2013-10-01 false Publication required. 7.4 Section 7.4 Transportation Office of the Secretary of Transportation PUBLIC AVAILABILITY OF INFORMATION Information Required To Be Made Public by DOT § 7.4 Publication required. (a) General. The material described in §...

  8. 49 CFR 7.4 - Publication required.

    Code of Federal Regulations, 2010 CFR

    2010-10-01

    ... 49 Transportation 1 2010-10-01 2010-10-01 false Publication required. 7.4 Section 7.4 Transportation Office of the Secretary of Transportation PUBLIC AVAILABILITY OF INFORMATION Information Required To Be Made Public by DOT § 7.4 Publication required. (a) General. The material described in §...

  9. 49 CFR 7.4 - Publication required.

    Code of Federal Regulations, 2012 CFR

    2012-10-01

    ... 49 Transportation 1 2012-10-01 2012-10-01 false Publication required. 7.4 Section 7.4 Transportation Office of the Secretary of Transportation PUBLIC AVAILABILITY OF INFORMATION Information Required To Be Made Public by DOT § 7.4 Publication required. (a) General. The material described in §...

  10. 49 CFR 7.4 - Publication required.

    Code of Federal Regulations, 2011 CFR

    2011-10-01

    ... 49 Transportation 1 2011-10-01 2011-10-01 false Publication required. 7.4 Section 7.4 Transportation Office of the Secretary of Transportation PUBLIC AVAILABILITY OF INFORMATION Information Required To Be Made Public by DOT § 7.4 Publication required. (a) General. The material described in §...

  11. Synthesis, characterisation, conformational preferences, dynamic NMR studies and antimicrobial evaluation of N-nitroso- and N-formyl-c-3,t-3-dimethyl-r-2,c-7-diphenyl-1,4-diazepan-5-ones

    NASA Astrophysics Data System (ADS)

    Ponnuswamy, S.; Akila, A.; Kiruthiga devi, D.; Maheshwaran, V.; Ponnuswamy, M. N.

    2016-04-01

    The stereochemical preferences of N-nitroso- and N-formyl-c-3,t-3-dimethyl-r-2,c-7-diphenyl-1,4-diazepan-5-ones 3 & 4, respectively, have been determined using 1D and 2D NMR spectral techniques. Interestingly, the N-nitroso compound 3 is found to prefer an equilibrium between alternate chair conformations with diaxial phenyl groups, while the N-formyl compound 4 prefers flattened boat conformation. This is stereochemically a novel report on the flexible rings adopting a chair conformation with diaxial phenyl groups. The X-ray crystal structure of N-nitroso-c-3,t-3-dimethyl-r-2,c-7-diphenyl-1,4-diazepan-5-one (3) also supports the chair conformation with diaxial phenyl groups. Dynamic 1H NMR spectral studies have been carried out on the N-nitroso and N-formyl diazepan-5-ones 3 &4 and the energy barriers for N-NO and N-CO rotations are found to be 88.7 and 75.7 kJ/mol, respectively. The antimicrobial activities have been determined for the compounds 2-4 and it is found that all the compounds exhibit significant antibacterial and antifungal activities when compared to the standard chloramphenicol.

  12. Polymethylated Myricetin in Trichomes of the Wild Tomato Species Solanum habrochaites and Characterization of Trichome-Specific 3′/5′- and 7/4′-Myricetin O-Methyltransferases1[C][W][OA

    PubMed Central

    Schmidt, Adam; Li, Chao; Shi, Feng; Jones, A. Daniel; Pichersky, Eran

    2011-01-01

    Flavonoids are a class of metabolites found in many plant species. They have been reported to serve several physiological roles, such as in defense against herbivores and pathogens and in protection against harmful ultraviolet radiation. They also serve as precursors of pigment compounds found in flowers, leaves, and seeds. Highly methylated, nonglycosylated derivatives of the flavonoid myricetin flavonoid, have been previously reported from a variety of plants, but O-methyltransferases responsible for their synthesis have not yet been identified. Here, we show that secreting glandular trichomes (designated types 1 and 4) and storage glandular trichomes (type 6) on the leaf surface of wild tomato (Solanum habrochaites accession LA1777) plants contain 3,7,3′-trimethyl myricetin, 3,7,3′,5′-tetramethyl myricetin, and 3,7,3′,4′,5′-pentamethyl myricetin, with gland types 1 and 4 containing severalfold more of these compounds than type 6 glands and with the tetramethylated compound predominating in all three gland types. We have also identified transcripts of two genes expressed in the glandular trichomes and showed that they encode enzymes capable of methylating myricetin at the 3′ and 5′ and the 7 and 4′ positions, respectively. Both genes are preferentially expressed in secreting glandular trichome types 1 and 4 and to a lesser degree in storage trichome type 6, and the levels of the proteins they encode are correspondingly higher in types 1 and 4 glands compared with type 6 glands. PMID:21343428

  13. 7 CFR 8.5 - Revocation of present authorizations.

    Code of Federal Regulations, 2010 CFR

    2010-01-01

    ... 7 Agriculture 1 2010-01-01 2010-01-01 false Revocation of present authorizations. 8.5 Section 8.5 Agriculture Office of the Secretary of Agriculture 4-H CLUB NAME AND EMBLEM § 8.5 Revocation of present authorizations. Effective September 16, 1985, authorization permits for the use of the 4-H Club Name and...

  14. Synthesis, characterization, biological evaluation and docking studies of 2‧-[(2″,4″-difluorobiphenyl-4-yl)carbonyl]-1‧-aryl-1‧,2‧,5‧,6‧,7‧,7a‧-hexahydrospiro[indole-3,3‧-pyrrolizin]-2(1H)-ones

    NASA Astrophysics Data System (ADS)

    Fathimunnisa, M.; Manikandan, H.; Neelakandan, K.; Rajendra Prasad, N.; Selvanayagam, S.; Sridhar, B.

    2016-10-01

    A series of novel 2‧-[(2″,4″-difluorobiphenyl-4-yl)carbonyl]-1‧-aryl-1‧,2‧,5‧,6‧,7‧,7a‧-hexahydrospiro[indole-3,3‧-pyrrolizin]-2(1H)-ones were regioselectively synthesized by multicomponent reaction with excellent yield. They were characterized by elemental analysis and various spectral techniques. Sensing ability of the compound to different metal ions was investigated. To ascertain the inhibitory activity of the compounds they were subjected to in vitro antimicrobial studies against various microbes and cytotoxic studies against Hep-2 cell line. The ligand-receptor interaction of the compounds was explored by molecular docking and the human folate receptor (4LRH) was identified as the potential target protein. DFT calculations were incorporated in the study to compare the molecular structure and geometrical parameters of 2‧-[(2″,4″-difluorobiphenyl-4-yl)carbonyl]-1‧-phenyl-1‧,2‧,5‧,6‧,7‧,7a‧-hexahydrospiro[indole-3,3‧-pyrrolizin]-2(1H)-one with experimental data.

  15. Synthesis and Screening of Modified 6,6'-Bis(5,5,8,8-tetramethyl-5,6,7,8-tetrahydrobenzo[e][1,2,4]triazin-3-yl)-2,2'-bipyridine Ligands for Actinide and Lanthanide Separation in Nuclear Waste Treatment.

    PubMed

    Afsar, Ashfaq; Distler, Petr; Harwood, Laurence M; John, Jan; Westwood, James

    2016-11-04

    Effects of chloro and bromo substitution at the 4-position of the pyridine ring of 6,6'-bis(5,5,8,8-tetramethyl-5,6,7,8-tetrahydrobenzo[e][1,2,4]triazin-3-yl)-2,2'-bipyridine (CyMe4-BTBP) have been studied with regard to the extraction of Am(III) from Eu(III) and Cm(III) from 0.1-3 M HNO3. Similarly to CyMe4-BTBP, a highly efficient (DAm > 10 at 3 M HNO3) and selective (SFAm/Eu > 100 at 3 M HNO3) extraction was observed for Cl-CyMe4-BTBP and Br-CyMe4-BTBP in 1-octanol but in the absence of a phase-transfer agent.

  16. Discovery of 7-N-piperazinylthiazolo[5,4-d]pyrimidine analogues as a novel class of immunosuppressive agents with in vivo biological activity.

    PubMed

    Jang, Mi-Yeon; Lin, Yuan; De Jonghe, Steven; Gao, Ling-Jie; Vanderhoydonck, Bart; Froeyen, Mathy; Rozenski, Jef; Herman, Jean; Louat, Thierry; Van Belle, Kristien; Waer, Mark; Herdewijn, Piet

    2011-01-27

    Herein we describe the synthesis and in vitro and in vivo activity of thiazolo[5,4-d]pyrimidines as a novel class of immunosuppressive agents, useful for preventing graft rejection after organ transplantation. This research resulted in the discovery of a series of compounds with potent activity in the mixed lymphocyte reaction (MLR) assay, which is well-known as the in vitro model for in vivo rejection after organ transplantation. The most potent congeners displayed IC(50) values of less than 50 nM in this MLR assay and hence are equipotent to cyclosporin A, a clinically used immunosuppressive drug. One representative of this series was further evaluated in a preclinical animal model of organ transplantation and showed excellent in vivo efficacy. It validates these compounds as new promising immunosuppressive drugs.

  17. Two compact planetary nebulae of moderate excitation - NGC 6565 (3-4.5 deg) and NGC 6644 (8-7.2 deg)

    NASA Technical Reports Server (NTRS)

    Aller, Lawrence H.; Keyes, Charles D.; Feibelman, Walter

    1988-01-01

    Data obtained with an image-tube scanner at the 3-m Shane telescope are combined with IUE data to obtain plasma diagnostics and chemical compositions for two planetary nebulae of moderately high excitation. Theoretical nebular models were calculated using stellar fluxes given by Husfeld et al. (1984) for T(asterisk) = 85,000 K, log g = 4.72, and elemental abundances were obtained by fitting theoretical to observed line intensities and also by using the model to determine ionization correction factors to be applied to observed ionic concentrations. Although C appears to be about 1.5 times as abundant in NGC 6644 as in NGC 6565, N, O, Ne, S, Cl, and Ar are depleted by factors ranging from 2 to 6 in NGC 6644 as compared to NGC 6565. The high-velocity object, NGC 6644, was evidently made from a less metal-rich mixture than the sun.

  18. Low-temperature T4-like coliphages vB_EcoM-VR5, vB_EcoM-VR7 and vB_EcoM-VR20.

    PubMed

    Kaliniene, Laura; Klausa, Vytautas; Truncaite, Lidija

    2010-06-01

    Bacteriophages vB_EcoM-VR5, vB_EcoM-VR7 and vB_EcoM-VR20, showing an unusual low-temperature plating profile and producing constantly growing plaques, were isolated from aquatic environments of Lithuania. Although vB_EcoM-VR5, vB_EcoM-VR7 and vB_EcoM-VR20 resembled phage T4 both in their genome size and in their major structural protein (gp23) pattern, physiological properties of all three phages tested differed significantly from those of T4. With an optimum temperature for plating around 24 degrees C and a high efficiency of plating in the range 7-30 degrees C, bacteriophages vB_EcoM-VR7 and vB_EcoM-VR20 failed to plate at 37 degrees C, whereas phage vB_EcoM-VR5 could not be plated at 40 degrees C. Sequence analysis of diagnostic g23 PCR products revealed that g23 of vB_EcoM-VR5, vB_EcoM-VR7 and vB_EcoM-VR20 differed from the corresponding T4 g23 DNA sequence by 21, 21 and 20%, respectively.

  19. Ring-strain release in neutral and dicationic 7,8,17,18-tetra­bromo-5,10,15,20-tetra­phenyl­porphyrin: crystal structures of C44H26Br4N4 and C44H28Br4N4 2+·2ClO4 −·3CH2Cl2

    PubMed Central

    Scheidt, W. Robert; Duval, Hugues F.; Oliver, Allen G.

    2016-01-01

    Two porphyrin complexes were studied to determine the effects of protonation on ring deformation within the porphyrin. The porphyrin 7,8,17,18-tetra­bromo-5,10,15,20-tetra­phenyl­porphyrin, C44H26Br4N4, was selected because the neutral species is readily doubly protonated to yield a dication, which was crystallized here with perchlorate counter-ions as a di­chloro­methane tris­olvate, C44H28Br4N4 2+·2ClO4 −·3CH2Cl2. The centrosymmetric neutral species is observed to have a mild ‘ruffling’ of the pyrrole rings and is essentially planar throughout; intra­molecular N—H⋯N hydrogen bonds occur. In contrast, the dication exhibits considerable deformation, with the pyrrole rings oriented well out of the plane of the porphyrin, resulting in a ‘saddle’ conformation of the ring. The charged species forms N—H⋯O hydrogen bonds to the perchlorate anions, which lie above and below the plane of the porphyrin ring. Distortions to the planarity of the pyrrole rings in both cases are very minor. The characterization of the neutral species represents a low-temperature redetermination of the previous room-temperature analyses [Zou et al. (1995 ▸). Acta Cryst. C51, 760–761; Rayati et al. (2008 ▸). Polyhedron, pp. 2285–2290], which showed disorder and physically unrealistic displacement parameters. PMID:27308051

  20. 7 CFR 33.5 - Apples.

    Code of Federal Regulations, 2014 CFR

    2014-01-01

    ... 7 Agriculture 2 2014-01-01 2014-01-01 false Apples. 33.5 Section 33.5 Agriculture Regulations of the Department of Agriculture AGRICULTURAL MARKETING SERVICE (Standards, Inspections, Marketing... ISSUED UNDER AUTHORITY OF THE EXPORT APPLE ACT Definitions § 33.5 Apples. Apples mean fresh whole...

  1. 7 CFR 33.5 - Apples.

    Code of Federal Regulations, 2011 CFR

    2011-01-01

    ... 7 Agriculture 2 2011-01-01 2011-01-01 false Apples. 33.5 Section 33.5 Agriculture Regulations of the Department of Agriculture AGRICULTURAL MARKETING SERVICE (Standards, Inspections, Marketing... ISSUED UNDER AUTHORITY OF THE EXPORT APPLE ACT Definitions § 33.5 Apples. Apples mean fresh whole...

  2. 7 CFR 33.5 - Apples.

    Code of Federal Regulations, 2012 CFR

    2012-01-01

    ... 7 Agriculture 2 2012-01-01 2012-01-01 false Apples. 33.5 Section 33.5 Agriculture Regulations of the Department of Agriculture AGRICULTURAL MARKETING SERVICE (Standards, Inspections, Marketing... ISSUED UNDER AUTHORITY OF THE EXPORT APPLE ACT Definitions § 33.5 Apples. Apples mean fresh whole...

  3. 7 CFR 33.5 - Apples.

    Code of Federal Regulations, 2013 CFR

    2013-01-01

    ... 7 Agriculture 2 2013-01-01 2013-01-01 false Apples. 33.5 Section 33.5 Agriculture Regulations of the Department of Agriculture AGRICULTURAL MARKETING SERVICE (Standards, Inspections, Marketing... ISSUED UNDER AUTHORITY OF THE EXPORT APPLE ACT Definitions § 33.5 Apples. Apples mean fresh whole...

  4. 7 CFR 33.5 - Apples.

    Code of Federal Regulations, 2010 CFR

    2010-01-01

    ... 7 Agriculture 2 2010-01-01 2010-01-01 false Apples. 33.5 Section 33.5 Agriculture Regulations of the Department of Agriculture AGRICULTURAL MARKETING SERVICE (Standards, Inspections, Marketing... ISSUED UNDER AUTHORITY OF THE EXPORT APPLE ACT Definitions § 33.5 Apples. Apples mean fresh whole...

  5. 7 CFR 946.5 - Potatoes.

    Code of Federal Regulations, 2014 CFR

    2014-01-01

    ... 7 Agriculture 8 2014-01-01 2014-01-01 false Potatoes. 946.5 Section 946.5 Agriculture Regulations... ORDERS; FRUITS, VEGETABLES, NUTS), DEPARTMENT OF AGRICULTURE IRISH POTATOES GROWN IN WASHINGTON Order Regulating Handling Definitions § 946.5 Potatoes. Potatoes means all varieties of Irish potatoes grown...

  6. 7 CFR 948.5 - Potatoes.

    Code of Federal Regulations, 2010 CFR

    2010-01-01

    ... 7 Agriculture 8 2010-01-01 2010-01-01 false Potatoes. 948.5 Section 948.5 Agriculture Regulations... Orders; Fruits, Vegetables, Nuts), DEPARTMENT OF AGRICULTURE IRISH POTATOES GROWN IN COLORADO Order Regulating Handling Definitions § 948.5 Potatoes. Potatoes means and includes all varieties of Irish...

  7. 7 CFR 947.5 - Potatoes.

    Code of Federal Regulations, 2013 CFR

    2013-01-01

    ... 7 Agriculture 8 2013-01-01 2013-01-01 false Potatoes. 947.5 Section 947.5 Agriculture Regulations... ORDERS; FRUITS, VEGETABLES, NUTS), DEPARTMENT OF AGRICULTURE IRISH POTATOES GROWN IN MODOC AND SISKIYOU... Definitions § 947.5 Potatoes. Potatoes means all varieties of Irish potatoes grown within the...

  8. 7 CFR 946.5 - Potatoes.

    Code of Federal Regulations, 2013 CFR

    2013-01-01

    ... 7 Agriculture 8 2013-01-01 2013-01-01 false Potatoes. 946.5 Section 946.5 Agriculture Regulations... ORDERS; FRUITS, VEGETABLES, NUTS), DEPARTMENT OF AGRICULTURE IRISH POTATOES GROWN IN WASHINGTON Order Regulating Handling Definitions § 946.5 Potatoes. Potatoes means all varieties of Irish potatoes grown...

  9. 7 CFR 946.5 - Potatoes.

    Code of Federal Regulations, 2011 CFR

    2011-01-01

    ... 7 Agriculture 8 2011-01-01 2011-01-01 false Potatoes. 946.5 Section 946.5 Agriculture Regulations... Orders; Fruits, Vegetables, Nuts), DEPARTMENT OF AGRICULTURE IRISH POTATOES GROWN IN WASHINGTON Order Regulating Handling Definitions § 946.5 Potatoes. Potatoes means all varieties of Irish potatoes grown...

  10. 7 CFR 945.5 - Potatoes.

    Code of Federal Regulations, 2010 CFR

    2010-01-01

    ... 7 Agriculture 8 2010-01-01 2010-01-01 false Potatoes. 945.5 Section 945.5 Agriculture Regulations... Orders; Fruits, Vegetables, Nuts), DEPARTMENT OF AGRICULTURE IRISH POTATOES GROWN IN CERTAIN DESIGNATED COUNTIES IN IDAHO, AND MALHEUR COUNTY, OREGON Order Regulating Handling Definitions § 945.5...

  11. 7 CFR 948.5 - Potatoes.

    Code of Federal Regulations, 2011 CFR

    2011-01-01

    ... 7 Agriculture 8 2011-01-01 2011-01-01 false Potatoes. 948.5 Section 948.5 Agriculture Regulations... Orders; Fruits, Vegetables, Nuts), DEPARTMENT OF AGRICULTURE IRISH POTATOES GROWN IN COLORADO Order Regulating Handling Definitions § 948.5 Potatoes. Potatoes means and includes all varieties of Irish...

  12. 7 CFR 953.5 - Potatoes.

    Code of Federal Regulations, 2013 CFR

    2013-01-01

    ... 7 Agriculture 8 2013-01-01 2013-01-01 false Potatoes. 953.5 Section 953.5 Agriculture Regulations... ORDERS; FRUITS, VEGETABLES, NUTS), DEPARTMENT OF AGRICULTURE IRISH POTATOES GROWN IN SOUTHEASTERN STATES Order Regulating Handling Definitions § 953.5 Potatoes. Potatoes means all varieties of Irish...

  13. 7 CFR 953.5 - Potatoes.

    Code of Federal Regulations, 2010 CFR

    2010-01-01

    ... 7 Agriculture 8 2010-01-01 2010-01-01 false Potatoes. 953.5 Section 953.5 Agriculture Regulations... Orders; Fruits, Vegetables, Nuts), DEPARTMENT OF AGRICULTURE IRISH POTATOES GROWN IN SOUTHEASTERN STATES Order Regulating Handling Definitions § 953.5 Potatoes. Potatoes means all varieties of Irish...

  14. 7 CFR 953.5 - Potatoes.

    Code of Federal Regulations, 2011 CFR

    2011-01-01

    ... 7 Agriculture 8 2011-01-01 2011-01-01 false Potatoes. 953.5 Section 953.5 Agriculture Regulations... Orders; Fruits, Vegetables, Nuts), DEPARTMENT OF AGRICULTURE IRISH POTATOES GROWN IN SOUTHEASTERN STATES Order Regulating Handling Definitions § 953.5 Potatoes. Potatoes means all varieties of Irish...

  15. 7 CFR 953.5 - Potatoes.

    Code of Federal Regulations, 2014 CFR

    2014-01-01

    ... 7 Agriculture 8 2014-01-01 2014-01-01 false Potatoes. 953.5 Section 953.5 Agriculture Regulations... ORDERS; FRUITS, VEGETABLES, NUTS), DEPARTMENT OF AGRICULTURE IRISH POTATOES GROWN IN SOUTHEASTERN STATES Order Regulating Handling Definitions § 953.5 Potatoes. Potatoes means all varieties of Irish...

  16. 7 CFR 945.5 - Potatoes.

    Code of Federal Regulations, 2012 CFR

    2012-01-01

    ... 7 Agriculture 8 2012-01-01 2012-01-01 false Potatoes. 945.5 Section 945.5 Agriculture Regulations... Orders; Fruits, Vegetables, Nuts), DEPARTMENT OF AGRICULTURE IRISH POTATOES GROWN IN CERTAIN DESIGNATED COUNTIES IN IDAHO, AND MALHEUR COUNTY, OREGON Order Regulating Handling Definitions § 945.5...

  17. 7 CFR 953.5 - Potatoes.

    Code of Federal Regulations, 2012 CFR

    2012-01-01

    ... 7 Agriculture 8 2012-01-01 2012-01-01 false Potatoes. 953.5 Section 953.5 Agriculture Regulations... Orders; Fruits, Vegetables, Nuts), DEPARTMENT OF AGRICULTURE IRISH POTATOES GROWN IN SOUTHEASTERN STATES Order Regulating Handling Definitions § 953.5 Potatoes. Potatoes means all varieties of Irish...

  18. 7 CFR 947.5 - Potatoes.

    Code of Federal Regulations, 2011 CFR

    2011-01-01

    ... 7 Agriculture 8 2011-01-01 2011-01-01 false Potatoes. 947.5 Section 947.5 Agriculture Regulations... Orders; Fruits, Vegetables, Nuts), DEPARTMENT OF AGRICULTURE IRISH POTATOES GROWN IN MODOC AND SISKIYOU... Definitions § 947.5 Potatoes. Potatoes means all varieties of Irish potatoes grown within the...

  19. 7 CFR 947.5 - Potatoes.

    Code of Federal Regulations, 2014 CFR

    2014-01-01

    ... 7 Agriculture 8 2014-01-01 2014-01-01 false Potatoes. 947.5 Section 947.5 Agriculture Regulations... ORDERS; FRUITS, VEGETABLES, NUTS), DEPARTMENT OF AGRICULTURE IRISH POTATOES GROWN IN MODOC AND SISKIYOU... Definitions § 947.5 Potatoes. Potatoes means all varieties of Irish potatoes grown within the...

  20. 7 CFR 945.5 - Potatoes.

    Code of Federal Regulations, 2013 CFR

    2013-01-01

    ... 7 Agriculture 8 2013-01-01 2013-01-01 false Potatoes. 945.5 Section 945.5 Agriculture Regulations... ORDERS; FRUITS, VEGETABLES, NUTS), DEPARTMENT OF AGRICULTURE IRISH POTATOES GROWN IN CERTAIN DESIGNATED COUNTIES IN IDAHO, AND MALHEUR COUNTY, OREGON Order Regulating Handling Definitions § 945.5...

  1. 7 CFR 948.5 - Potatoes.

    Code of Federal Regulations, 2012 CFR

    2012-01-01

    ... 7 Agriculture 8 2012-01-01 2012-01-01 false Potatoes. 948.5 Section 948.5 Agriculture Regulations... Orders; Fruits, Vegetables, Nuts), DEPARTMENT OF AGRICULTURE IRISH POTATOES GROWN IN COLORADO Order Regulating Handling Definitions § 948.5 Potatoes. Potatoes means and includes all varieties of Irish...

  2. 7 CFR 946.5 - Potatoes.

    Code of Federal Regulations, 2012 CFR

    2012-01-01

    ... 7 Agriculture 8 2012-01-01 2012-01-01 false Potatoes. 946.5 Section 946.5 Agriculture Regulations... Orders; Fruits, Vegetables, Nuts), DEPARTMENT OF AGRICULTURE IRISH POTATOES GROWN IN WASHINGTON Order Regulating Handling Definitions § 946.5 Potatoes. Potatoes means all varieties of Irish potatoes grown...

  3. 7 CFR 947.5 - Potatoes.

    Code of Federal Regulations, 2012 CFR

    2012-01-01

    ... 7 Agriculture 8 2012-01-01 2012-01-01 false Potatoes. 947.5 Section 947.5 Agriculture Regulations... Orders; Fruits, Vegetables, Nuts), DEPARTMENT OF AGRICULTURE IRISH POTATOES GROWN IN MODOC AND SISKIYOU... Definitions § 947.5 Potatoes. Potatoes means all varieties of Irish potatoes grown within the...

  4. 7 CFR 946.5 - Potatoes.

    Code of Federal Regulations, 2010 CFR

    2010-01-01

    ... 7 Agriculture 8 2010-01-01 2010-01-01 false Potatoes. 946.5 Section 946.5 Agriculture Regulations... Orders; Fruits, Vegetables, Nuts), DEPARTMENT OF AGRICULTURE IRISH POTATOES GROWN IN WASHINGTON Order Regulating Handling Definitions § 946.5 Potatoes. Potatoes means all varieties of Irish potatoes grown...

  5. 7 CFR 945.5 - Potatoes.

    Code of Federal Regulations, 2011 CFR

    2011-01-01

    ... 7 Agriculture 8 2011-01-01 2011-01-01 false Potatoes. 945.5 Section 945.5 Agriculture Regulations... Orders; Fruits, Vegetables, Nuts), DEPARTMENT OF AGRICULTURE IRISH POTATOES GROWN IN CERTAIN DESIGNATED COUNTIES IN IDAHO, AND MALHEUR COUNTY, OREGON Order Regulating Handling Definitions § 945.5...

  6. 7 CFR 945.5 - Potatoes.

    Code of Federal Regulations, 2014 CFR

    2014-01-01

    ... 7 Agriculture 8 2014-01-01 2014-01-01 false Potatoes. 945.5 Section 945.5 Agriculture Regulations... ORDERS; FRUITS, VEGETABLES, NUTS), DEPARTMENT OF AGRICULTURE IRISH POTATOES GROWN IN CERTAIN DESIGNATED COUNTIES IN IDAHO, AND MALHEUR COUNTY, OREGON Order Regulating Handling Definitions § 945.5...

  7. 7 CFR 948.5 - Potatoes.

    Code of Federal Regulations, 2014 CFR

    2014-01-01

    ... 7 Agriculture 8 2014-01-01 2014-01-01 false Potatoes. 948.5 Section 948.5 Agriculture Regulations... ORDERS; FRUITS, VEGETABLES, NUTS), DEPARTMENT OF AGRICULTURE IRISH POTATOES GROWN IN COLORADO Order Regulating Handling Definitions § 948.5 Potatoes. Potatoes means and includes all varieties of Irish...

  8. 7 CFR 947.5 - Potatoes.

    Code of Federal Regulations, 2010 CFR

    2010-01-01

    ... 7 Agriculture 8 2010-01-01 2010-01-01 false Potatoes. 947.5 Section 947.5 Agriculture Regulations... Orders; Fruits, Vegetables, Nuts), DEPARTMENT OF AGRICULTURE IRISH POTATOES GROWN IN MODOC AND SISKIYOU... Definitions § 947.5 Potatoes. Potatoes means all varieties of Irish potatoes grown within the...

  9. 7 CFR 948.5 - Potatoes.

    Code of Federal Regulations, 2013 CFR

    2013-01-01

    ... 7 Agriculture 8 2013-01-01 2013-01-01 false Potatoes. 948.5 Section 948.5 Agriculture Regulations... ORDERS; FRUITS, VEGETABLES, NUTS), DEPARTMENT OF AGRICULTURE IRISH POTATOES GROWN IN COLORADO Order Regulating Handling Definitions § 948.5 Potatoes. Potatoes means and includes all varieties of Irish...

  10. 7 CFR 929.5 - Cranberries.

    Code of Federal Regulations, 2012 CFR

    2012-01-01

    ... 7 Agriculture 8 2012-01-01 2012-01-01 false Cranberries. 929.5 Section 929.5 Agriculture... and Orders; Fruits, Vegetables, Nuts), DEPARTMENT OF AGRICULTURE CRANBERRIES GROWN IN STATES OF... LONG ISLAND IN THE STATE OF NEW YORK Order Regulating Handling Definitions § 929.5...

  11. 7 CFR 929.5 - Cranberries.

    Code of Federal Regulations, 2011 CFR

    2011-01-01

    ... 7 Agriculture 8 2011-01-01 2011-01-01 false Cranberries. 929.5 Section 929.5 Agriculture... and Orders; Fruits, Vegetables, Nuts), DEPARTMENT OF AGRICULTURE CRANBERRIES GROWN IN STATES OF... LONG ISLAND IN THE STATE OF NEW YORK Order Regulating Handling Definitions § 929.5...

  12. 7 CFR 929.5 - Cranberries.

    Code of Federal Regulations, 2013 CFR

    2013-01-01

    ... 7 Agriculture 8 2013-01-01 2013-01-01 false Cranberries. 929.5 Section 929.5 Agriculture... AND ORDERS; FRUITS, VEGETABLES, NUTS), DEPARTMENT OF AGRICULTURE CRANBERRIES GROWN IN STATES OF... LONG ISLAND IN THE STATE OF NEW YORK Order Regulating Handling Definitions § 929.5...

  13. 7 CFR 929.5 - Cranberries.

    Code of Federal Regulations, 2010 CFR

    2010-01-01

    ... 7 Agriculture 8 2010-01-01 2010-01-01 false Cranberries. 929.5 Section 929.5 Agriculture... and Orders; Fruits, Vegetables, Nuts), DEPARTMENT OF AGRICULTURE CRANBERRIES GROWN IN STATES OF... LONG ISLAND IN THE STATE OF NEW YORK Order Regulating Handling Definitions § 929.5...

  14. 7 CFR 929.5 - Cranberries.

    Code of Federal Regulations, 2014 CFR

    2014-01-01

    ... 7 Agriculture 8 2014-01-01 2014-01-01 false Cranberries. 929.5 Section 929.5 Agriculture... AND ORDERS; FRUITS, VEGETABLES, NUTS), DEPARTMENT OF AGRICULTURE CRANBERRIES GROWN IN STATES OF... LONG ISLAND IN THE STATE OF NEW YORK Order Regulating Handling Definitions § 929.5...

  15. 7 CFR 500.5 - Nuisances.

    Code of Federal Regulations, 2010 CFR

    2010-01-01

    ... 7 Agriculture 6 2010-01-01 2010-01-01 false Nuisances. 500.5 Section 500.5 Agriculture Regulations... NATIONAL ARBORETUM Conduct on U.S. National Arboreturm Property § 500.5 Nuisances. (a) The use of loud... creation of other noises of a decibel level high enough to be heard outside of the USNA is prohibited....

  16. 7 CFR 906.5 - Fruit.

    Code of Federal Regulations, 2013 CFR

    2013-01-01

    ... 7 Agriculture 8 2013-01-01 2013-01-01 false Fruit. 906.5 Section 906.5 Agriculture Regulations of... ORDERS; FRUITS, VEGETABLES, NUTS), DEPARTMENT OF AGRICULTURE ORANGES AND GRAPEFRUIT GROWN IN LOWER RIO GRANDE VALLEY IN TEXAS Order Regulating Handling Definitions § 906.5 Fruit. Fruit means either or both...

  17. 7 CFR 906.5 - Fruit.

    Code of Federal Regulations, 2012 CFR

    2012-01-01

    ... 7 Agriculture 8 2012-01-01 2012-01-01 false Fruit. 906.5 Section 906.5 Agriculture Regulations of... Orders; Fruits, Vegetables, Nuts), DEPARTMENT OF AGRICULTURE ORANGES AND GRAPEFRUIT GROWN IN LOWER RIO GRANDE VALLEY IN TEXAS Order Regulating Handling Definitions § 906.5 Fruit. Fruit means either or both...

  18. 7 CFR 906.5 - Fruit.

    Code of Federal Regulations, 2011 CFR

    2011-01-01

    ... 7 Agriculture 8 2011-01-01 2011-01-01 false Fruit. 906.5 Section 906.5 Agriculture Regulations of... Orders; Fruits, Vegetables, Nuts), DEPARTMENT OF AGRICULTURE ORANGES AND GRAPEFRUIT GROWN IN LOWER RIO GRANDE VALLEY IN TEXAS Order Regulating Handling Definitions § 906.5 Fruit. Fruit means either or both...

  19. 7 CFR 906.5 - Fruit.

    Code of Federal Regulations, 2010 CFR

    2010-01-01

    ... 7 Agriculture 8 2010-01-01 2010-01-01 false Fruit. 906.5 Section 906.5 Agriculture Regulations of... Orders; Fruits, Vegetables, Nuts), DEPARTMENT OF AGRICULTURE ORANGES AND GRAPEFRUIT GROWN IN LOWER RIO GRANDE VALLEY IN TEXAS Order Regulating Handling Definitions § 906.5 Fruit. Fruit means either or both...

  20. 7 CFR 906.5 - Fruit.

    Code of Federal Regulations, 2014 CFR

    2014-01-01

    ... 7 Agriculture 8 2014-01-01 2014-01-01 false Fruit. 906.5 Section 906.5 Agriculture Regulations of... ORDERS; FRUITS, VEGETABLES, NUTS), DEPARTMENT OF AGRICULTURE ORANGES AND GRAPEFRUIT GROWN IN LOWER RIO GRANDE VALLEY IN TEXAS Order Regulating Handling Definitions § 906.5 Fruit. Fruit means either or both...

  1. 7 CFR 613.5 - PMCs.

    Code of Federal Regulations, 2010 CFR

    2010-01-01

    ... 7 Agriculture 6 2010-01-01 2010-01-01 false PMCs. 613.5 Section 613.5 Agriculture Regulations of... AGRICULTURE CONSERVATION OPERATIONS PLANT MATERIALS CENTERS § 613.5 PMCs. (a) The Norman A. Berg National PMC..., Elsberry, MO, Bridger, MT, Fallon, NV, Cape May Courthouse, NJ, Los Lunas, NM, Big Flats, NY, Bismarck,...

  2. 7 CFR 1000.5 - Distributing plant.

    Code of Federal Regulations, 2011 CFR

    2011-01-01

    ... 7 Agriculture 9 2011-01-01 2011-01-01 false Distributing plant. 1000.5 Section 1000.5 Agriculture... Definitions § 1000.5 Distributing plant. Distributing plant means a plant that is approved by a duly... plants....

  3. 7 CFR 1000.5 - Distributing plant.

    Code of Federal Regulations, 2010 CFR

    2010-01-01

    ... 7 Agriculture 9 2010-01-01 2009-01-01 true Distributing plant. 1000.5 Section 1000.5 Agriculture... Definitions § 1000.5 Distributing plant. Distributing plant means a plant that is approved by a duly... plants....

  4. 7 CFR 987.5 - Dates.

    Code of Federal Regulations, 2010 CFR

    2010-01-01

    ... 7 Agriculture 8 2010-01-01 2010-01-01 false Dates. 987.5 Section 987.5 Agriculture Regulations of... Orders; Fruits, Vegetables, Nuts), DEPARTMENT OF AGRICULTURE DOMESTIC DATES PRODUCED OR PACKED IN RIVERSIDE COUNTY, CALIFORNIA Order Regulating Handling Definitions § 987.5 Dates. Dates means the...

  5. 7 CFR 981.5 - Unshelled almonds.

    Code of Federal Regulations, 2010 CFR

    2010-01-01

    ... 7 Agriculture 8 2010-01-01 2010-01-01 false Unshelled almonds. 981.5 Section 981.5 Agriculture... and Orders; Fruits, Vegetables, Nuts), DEPARTMENT OF AGRICULTURE ALMONDS GROWN IN CALIFORNIA Order Regulating Handling Definitions § 981.5 Unshelled almonds. Unshelled almonds means almonds the kernels...

  6. 7 CFR 981.5 - Unshelled almonds.

    Code of Federal Regulations, 2014 CFR

    2014-01-01

    ... 7 Agriculture 8 2014-01-01 2014-01-01 false Unshelled almonds. 981.5 Section 981.5 Agriculture... AND ORDERS; FRUITS, VEGETABLES, NUTS), DEPARTMENT OF AGRICULTURE ALMONDS GROWN IN CALIFORNIA Order Regulating Handling Definitions § 981.5 Unshelled almonds. Unshelled almonds means almonds the kernels...

  7. 7 CFR 981.5 - Unshelled almonds.

    Code of Federal Regulations, 2013 CFR

    2013-01-01

    ... 7 Agriculture 8 2013-01-01 2013-01-01 false Unshelled almonds. 981.5 Section 981.5 Agriculture... AND ORDERS; FRUITS, VEGETABLES, NUTS), DEPARTMENT OF AGRICULTURE ALMONDS GROWN IN CALIFORNIA Order Regulating Handling Definitions § 981.5 Unshelled almonds. Unshelled almonds means almonds the kernels...

  8. 7 CFR 981.5 - Unshelled almonds.

    Code of Federal Regulations, 2011 CFR

    2011-01-01

    ... 7 Agriculture 8 2011-01-01 2011-01-01 false Unshelled almonds. 981.5 Section 981.5 Agriculture... and Orders; Fruits, Vegetables, Nuts), DEPARTMENT OF AGRICULTURE ALMONDS GROWN IN CALIFORNIA Order Regulating Handling Definitions § 981.5 Unshelled almonds. Unshelled almonds means almonds the kernels...

  9. 7 CFR 981.5 - Unshelled almonds.

    Code of Federal Regulations, 2012 CFR

    2012-01-01

    ... 7 Agriculture 8 2012-01-01 2012-01-01 false Unshelled almonds. 981.5 Section 981.5 Agriculture... and Orders; Fruits, Vegetables, Nuts), DEPARTMENT OF AGRICULTURE ALMONDS GROWN IN CALIFORNIA Order Regulating Handling Definitions § 981.5 Unshelled almonds. Unshelled almonds means almonds the kernels...

  10. 7 CFR 3550.5 - Environmental requirements.

    Code of Federal Regulations, 2011 CFR

    2011-01-01

    ... 7 Agriculture 15 2011-01-01 2011-01-01 false Environmental requirements. 3550.5 Section 3550.5... AGRICULTURE DIRECT SINGLE FAMILY HOUSING LOANS AND GRANTS General § 3550.5 Environmental requirements. (a) Policy. RHS will consider environmental quality as equal with economic, social, and other...

  11. 7 CFR 3550.5 - Environmental requirements.

    Code of Federal Regulations, 2010 CFR

    2010-01-01

    ... 7 Agriculture 15 2010-01-01 2010-01-01 false Environmental requirements. 3550.5 Section 3550.5... AGRICULTURE DIRECT SINGLE FAMILY HOUSING LOANS AND GRANTS General § 3550.5 Environmental requirements. (a) Policy. RHS will consider environmental quality as equal with economic, social, and other...

  12. 7 CFR 985.5 - Production area.

    Code of Federal Regulations, 2010 CFR

    2010-01-01

    ... 7 Agriculture 8 2010-01-01 2010-01-01 false Production area. 985.5 Section 985.5 Agriculture... HANDLING OF SPEARMINT OIL PRODUCED IN THE FAR WEST Order Regulating Handling Definitions § 985.5 Production area. Production area means all the area within the States of Washington, Idaho, Oregon, and...

  13. 7 CFR 925.5 - Production area.

    Code of Federal Regulations, 2010 CFR

    2010-01-01

    ... 7 Agriculture 8 2010-01-01 2010-01-01 false Production area. 925.5 Section 925.5 Agriculture Regulations of the Department of Agriculture (Continued) AGRICULTURAL MARKETING SERVICE (Marketing Agreements... SOUTHEASTERN CALIFORNIA Definitions § 925.5 Production area. Production area means Imperial County,...

  14. 7 CFR 985.5 - Production area.

    Code of Federal Regulations, 2011 CFR

    2011-01-01

    ... 7 Agriculture 8 2011-01-01 2011-01-01 false Production area. 985.5 Section 985.5 Agriculture... HANDLING OF SPEARMINT OIL PRODUCED IN THE FAR WEST Order Regulating Handling Definitions § 985.5 Production area. Production area means all the area within the States of Washington, Idaho, Oregon, and...

  15. 7 CFR 925.5 - Production area.

    Code of Federal Regulations, 2011 CFR

    2011-01-01

    ... 7 Agriculture 8 2011-01-01 2011-01-01 false Production area. 925.5 Section 925.5 Agriculture Regulations of the Department of Agriculture (Continued) AGRICULTURAL MARKETING SERVICE (Marketing Agreements... SOUTHEASTERN CALIFORNIA Definitions § 925.5 Production area. Production area means Imperial County,...

  16. 7 CFR 922.5 - Apricots.

    Code of Federal Regulations, 2010 CFR

    2010-01-01

    ... 7 Agriculture 8 2010-01-01 2010-01-01 false Apricots. 922.5 Section 922.5 Agriculture Regulations... Orders; Fruits, Vegetables, Nuts), DEPARTMENT OF AGRICULTURE APRICOTS GROWN IN DESIGNATED COUNTIES IN WASHINGTON Order Regulating Handling Definitions § 922.5 Apricots. Apricots means all varieties of...

  17. 7 CFR 922.5 - Apricots.

    Code of Federal Regulations, 2012 CFR

    2012-01-01

    ... 7 Agriculture 8 2012-01-01 2012-01-01 false Apricots. 922.5 Section 922.5 Agriculture Regulations... Orders; Fruits, Vegetables, Nuts), DEPARTMENT OF AGRICULTURE APRICOTS GROWN IN DESIGNATED COUNTIES IN WASHINGTON Order Regulating Handling Definitions § 922.5 Apricots. Apricots means all varieties of...

  18. 7 CFR 922.5 - Apricots.

    Code of Federal Regulations, 2013 CFR

    2013-01-01

    ... 7 Agriculture 8 2013-01-01 2013-01-01 false Apricots. 922.5 Section 922.5 Agriculture Regulations... ORDERS; FRUITS, VEGETABLES, NUTS), DEPARTMENT OF AGRICULTURE APRICOTS GROWN IN DESIGNATED COUNTIES IN WASHINGTON Order Regulating Handling Definitions § 922.5 Apricots. Apricots means all varieties of...

  19. 7 CFR 922.5 - Apricots.

    Code of Federal Regulations, 2014 CFR

    2014-01-01

    ... 7 Agriculture 8 2014-01-01 2014-01-01 false Apricots. 922.5 Section 922.5 Agriculture Regulations... ORDERS; FRUITS, VEGETABLES, NUTS), DEPARTMENT OF AGRICULTURE APRICOTS GROWN IN DESIGNATED COUNTIES IN WASHINGTON Order Regulating Handling Definitions § 922.5 Apricots. Apricots means all varieties of...

  20. 7 CFR 922.5 - Apricots.

    Code of Federal Regulations, 2011 CFR

    2011-01-01

    ... 7 Agriculture 8 2011-01-01 2011-01-01 false Apricots. 922.5 Section 922.5 Agriculture Regulations... Orders; Fruits, Vegetables, Nuts), DEPARTMENT OF AGRICULTURE APRICOTS GROWN IN DESIGNATED COUNTIES IN WASHINGTON Order Regulating Handling Definitions § 922.5 Apricots. Apricots means all varieties of...