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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

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

Authors :
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
Source :
Bioorganic & Medicinal Chemistry Letters. 16:288-292
Publication Year :
2006
Publisher :
Elsevier BV, 2006.

Abstract

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.

Details

ISSN :
0960894X
Volume :
16
Database :
OpenAIRE
Journal :
Bioorganic & Medicinal Chemistry Letters
Accession number :
edsair.doi.dedup.....f287d246c2a3746f106e9752c3bac59e
Full Text :
https://doi.org/10.1016/j.bmcl.2005.10.006