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

Autor:	Suzanne H. St. Denis, Michelle L. Haven, Scott B. Seibel, Carol F. Petras, Subas M. Sakya, Lisa A. Lund, Annette M. Silvia, Michael P. Lynch, Bryson Rast, Cheng Hengmiao, Martha L. Minich, Burton H. Jaynes, Kristin M. Lundy DeMello, Donald W. Mann, Andrei Shavnya, Anne Hickman, Ziegler Carl B, David A. Koss, David M. George, Robert J. Rafka, Jin Li
Rok vydání:	2006
Předmět:	Stereochemistry Clinical Biochemistry Heteroatom Drug Evaluation Preclinical Administration Oral Pharmaceutical Science In Vitro Techniques Biochemistry Chemical synthesis Sulfone Structure-Activity Relationship chemistry.chemical_compound Dogs In vivo Drug Discovery Animals Structure–activity relationship Molecular Biology chemistry.chemical_classification Cyclooxygenase 2 Inhibitors Molecular Structure biology Organic Chemistry In vitro Disease Models Animal Enzyme chemistry Cyclooxygenase 2 Enzyme inhibitor Cats biology.protein Pyrazoles Molecular Medicine
Zdroj:	Bioorganic & Medicinal Chemistry Letters. 16:288-292
ISSN:	0960-894X
Popis:	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 identification of 2e as lead with potent in vitro activity, selectivity, and in vivo activity in dogs and cats.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f287d246c2a3746f106e9752c3bac59e https://doi.org/10.1016/j.bmcl.2005.10.006 Zobrazit plný text záznamu Full Text from ScienceDirect