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

Autor:	Rhonda M. Crosson, David A. Koss, Michelle L. Haven, Carolyn Rose Kilroy, Martha L. Minich, Robert J. Rafka, Eric L. Nimz, Morton Barry James, Scott B. Seibel, Lisa A. Lund, Carol F. Petras, Kristin M. Lundy DeMello, Chao Li, Annette M. Silvia, Bryson Rast, Kathleen M. Callaghan, Andrei Shavnya, Michael P. Lynch, Subas M. Sakya, Ziegler Carl B, Jin Li, Nicole L. Kolosko, Bronk Brian Scott, Donald W. Mann, Jason K. Dutra, Burton H. Jaynes, Henry Cheng, Glen W. Kirk
Rok vydání:	2004
Předmět:	Pyridines Stereochemistry Clinical Biochemistry Administration Oral Pharmaceutical Science Biochemistry Chemical synthesis Sulfone Structure-Activity Relationship chemistry.chemical_compound Dogs Oral administration In vivo Drug Discovery Animals Cyclooxygenase Inhibitors Molecular Biology chemistry.chemical_classification Cyclooxygenase 2 Inhibitors biology Chemistry Organic Chemistry In vitro Isoenzymes Enzyme Cyclooxygenase 2 Prostaglandin-Endoperoxide Synthases Enzyme inhibitor biology.protein Molecular Medicine COX-2 inhibitor
Zdroj:	Bioorganic & Medicinal Chemistry Letters. 14:95-98
ISSN:	0960-894X
Popis:	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 progression. The in vitro and in vivo activity of 12a for the canine COX-2 enzyme as well as its in vivo efficacy and pharmacokinetic properties in dog are highlighted.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::03f71036c4dab955ec24afc57075467a https://doi.org/10.1016/j.bmcl.2003.10.004 Zobrazit plný text záznamu Full Text from ScienceDirect