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Bioorg Med Chem Lett. 2004 Jan 5;14(1):95-8.

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

Author information

1
Veterinary Medicine Research and Development, Pfizer Inc., Groton, CT 06340, USA. jin_li@groton.pfizer.com

Abstract

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.

PMID:
14684306
DOI:
10.1016/j.bmcl.2003.10.004
[Indexed for MEDLINE]

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