2-Heterosubstituted-3-(4-methylsulfonyl)phenyl-5-trifluoromethyl Pyridines as Selective and Orally Active Cyclooxygenase-2 Inhibitors.
2010
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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