Bioorganic and Medicinal Chemistry Letters p. 1715 - 1720 (1999)
Update date:2022-08-05
Topics:
Dube, Daniel
Brideau, Christine
Deschenes, Denis
Fortin, Rejean
Friesen, Richard W.
Gordon, Robert
Girard, Yves
Riendeau, Denis
Savoie, Chantal
Chan, Chi-Chung
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.
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(1992)