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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 |
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| Authors: | Sakya Subas M DeMello Kristin M Lundy Minich Martha L Rast Bryson Shavnya Andrei Rafka Robert J Koss David A Cheng Hengmiao Li Jin Jaynes Burton H Ziegler Carl B Mann Donald W Petras Carol F Seibel Scott B Silvia Annette M George David M Lund Lisa A St Denis Suzanne Hickman Anne Haven Michelle L Lynch Michael P |
| Affiliation: | Veterinary Medicine Research and Development Pfizer Inc., Groton, CT 06340, USA. subas.m.sakya@pfizer.com |
| 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. |
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