Author/Authors :
Daniel Dubé، نويسنده , , Christine Brideau، نويسنده , , Denis Deschênes، نويسنده , , Rejean Fortin، نويسنده , , Richard W. Friesen، نويسنده , , Robert Gordon، نويسنده , , Jean-Yves Girard، نويسنده , , Denis Riendeau، نويسنده , , Chantal Savoie، نويسنده , , Chi-Chung Chan، نويسنده ,
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.