|Title||Discovery of a potent, selective and orally active canine COX-2 inhibitor, 2-(3-difluoromethyl-5-phenyl-pyrazol-1-yl)-5-methanesulfonyl-pyridine|
|Publication Type||Journal Article|
|Year of Publication||2004|
|Authors||Li, Jin, Kristin Lundy M. DeMello, Henry Cheng, Subas M. Sakya, Brian S. Bronk, Robert J. Rafka, Burton H. Jaynes, Carl B. Ziegler, Carolyn Kilroy, Donald W. Mann, Eric L. Nimz, Michael P. Lynch, Michelle L. Haven, Nicole L. Kolosko, Martha L. Minich, Chao Li, Jason K. Dutra, Bryson Rast, Rhonda M. Crosson, Barry J. Morton, Glen W. Kirk, Kathleen M. Callaghan, David A. Koss, Andrei Shavnya, Lisa A. Lund, Scott B. Seibel, Carol F. Petras, and Annette Silvia|
|Secondary Title||Bioorganic & Medicinal Chemistry Letters|
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.
0960-894Xdoi: DOI: 10.1016/j.bmcl.2003.10.004