2-Heterosubstituted-3-(4-methylsulfonyl) phenyl-5-trifluoromethyl pyridines as selective and orally active cyclooxygenase-2 inhibitors

…, C Brideau, D Deschênes, R Fortin, RW Friesen…

Index: Dube, Daniel; Brideau, Christine; Deschenes, Denis; Fortin, Rejean; Friesen, Richard W.; Gordon, Robert; Girard, Yves; Riendeau, Denis; Savoie, Chantal; Chan, Chi-Chung Bioorganic and Medicinal Chemistry Letters, 1999 , vol. 9, # 12 p. 1715 - 1720

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Citation Number: 26

Abstract

A series of novel 2-alkoxy, 2-thioalkoxy and 2-amino-3-(4-methylsulfonyl) phenylpyridines has been synthesized and shown to be highly potent and selective cyclooxygenase-2 (COX- 2) inhibitors. Structure-activity relationship studies have demonstrated that central pyridine ring substituents play an important role in the COX-2 potency, selectivity vs the COX-1 enzyme, and oral activity.