Výsledky vyhledávání - "Carol F. Petras"

5-Heteroatom substituted pyrazoles as canine COX-2 inhibitors. Part III: Molecular modeling studies on binding contribution of 1-(5-methylsulfonyl)pyrid-2-yl and 4-nitrile

Autor: Xinjun Hou, Kristin M. Lundy DeMello, Carol F. Petras, Subas M. Sakya, Cheng Hengmiao, Martha L. Minich, Donald W. Mann, Bryson Rast, Burton H. Jaynes, Michelle L. Haven, Scott B. Seibel, Andrei Shavnya, Jin Li

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 17:1067-1072

The structure-activity relationship toward canine COX-1 and COX-2 in vitro whole blood activity of 4-hydrogen versus 4-cyano substituted 5-aryl or 5-heteroatom substituted N-phenyl versus N-2-pyridyl sulfone pyrazoles is discussed. The differences be

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::93ad9e39836d5513ea4f0aa8a0a1f1a1
https://doi.org/10.1016/j.bmcl.2006.11.026

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Synthesis and SAR of heteroaryl-phenyl-substituted pyrazole derivatives as highly selective and potent canine COX-2 inhibitors

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 16:2076-2080

The discovery of heteroaryl-phenyl-substituted pyrazole derivatives as canine selective COX-2 inhibitors is described. Structure–activity relationship (SAR) studies of this class of compounds led to the identification of compound 1 which demonstrat

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::096af07029de50fcfe74128b57b3a069
https://doi.org/10.1016/j.bmcl.2006.01.059

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5-Heteroatom substituted pyrazoles as canine COX-2 inhibitors. Part 1: Structure–activity relationship studies of 5-alkylamino pyrazoles and discovery of a potent, selective, and orally active analog

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 16:288-292

Structure-activity relationship (SAR) studies of the novel 2-[3-di and trifluoromethyl-5-alkylamino pyrazo-1-yl]-5-methanesulfonyl (SO(2)Me)/sulfamoyl (SO(2)NH(2))-pyridine derivatives for canine COX enzymes are described. The studies led to the iden

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f287d246c2a3746f106e9752c3bac59e
https://doi.org/10.1016/j.bmcl.2005.10.006

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In vitro and in vivo profile of 2-(3-di-fluoromethyl-5-phenylpyrazol-1-yl)-5-methanesulfonylpyridine, a potent, selective, and orally active canine COX-2 inhibitor

Autor: Burton H. Jaynes, Michelle L. Haven, Scott B. Seibel, Nicole L. Kolosko, Carolyn Rose Kilroy, Kristin M. Lundy DeMello, Donald W. Mann, Michael P. Lynch, Cheng Hengmiao, Lisa A. Lund, Robert J. Rafka, Jin Li, Carol F. Petras, Subas M. Sakya, Bronk Brian Scott

Publikováno v: Bioorganic & Medicinal Chemistry. 13:1805-1809

The synthesis of a novel canine COX-2 selective inhibitor, 2-(3-difluoromethyl-5-phenylpyrazol-1-yl)-5-methanesulfonylpyridine, and its in vitro and in vivo profile are described. Pyrazole 8 demonstrated excellent potency and selectivity for canine C

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::442d5fd80e9563aadcaab6043c177abd
https://doi.org/10.1016/j.bmc.2004.11.048

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Discovery of a potent, selective and orally active canine COX-2 inhibitor, 2-(3-difluoromethyl-5-phenyl-pyrazol-1-yl)-5-methanesulfonyl-pyridine

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 14:95-98

Structure-activity relationship (SAR) studies of 2-[3-di(and tri)fluoromethyl-5-arylpyrazol-1-yl]-5-methanesulfonylpyridine derivatives for canine COX enzymes are described. This led to the identification of 12a as a lead candidate for further progre

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::03f71036c4dab955ec24afc57075467a
https://doi.org/10.1016/j.bmcl.2003.10.004

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Comparative structure-activity relationship studies of 1-(5-methylsulfonylpyrid-2-yl)-5-alkyl and (hetero)aryl triazoles and pyrazoles in canine COX inhibition

Autor: Donald W. Mann, Carol F. Petras, Chao Li, Subas M. Sakya, Andrei Shavnya, Michael P. Lynch, Burton H. Jaynes, Cheng Hengmiao, Bryson Rast, David A. Koss, Jin Li, Michelle L. Haven, Scott B. Seibel

Publikováno v: Bioorganicmedicinal chemistry letters. 18(3)

Structure–activity relationship (SAR) studies of novel 5-alkyl and 5-aryl/heteroaryl substituted 1,2,4-triazoles are described. The in vitro activity is compared to the pyrazole class of compounds with analogous side chains to delineate the contrib

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::dec972ae287e43a03df1763fa92bdd76
https://pubmed.ncbi.nlm.nih.gov/18182290

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5-Heteroatom-substituted pyrazoles as canine COX-2 inhibitors: Part 2. Structure-activity relationship studies of 5-alkylethers and 5-thioethers

Publikováno v: Bioorganicmedicinal chemistry letters. 16(5)

Structure-activity relationship (SAR) studies of novel 2-[3-trifluoromethyl-5-alkyl(thio)ether pyrazo-1-yl]-5-methanesulfonyl pyridine derivatives for canine COX enzymes are described. The 4-cyano-5-alkyl ethers were found to have excellent potency a

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::41c1d7a31ee47ce7d3e43437166665af
https://pubmed.ncbi.nlm.nih.gov/16380252

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