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

Article Details

Citation

Dube D, Brideau C, Deschenes D, Fortin R, Friesen RW, Gordon R, Girard Y, Riendeau D, Savoie C, Chan CC

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

Bioorg Med Chem Lett. 1999 Jun 21;9(12):1715-20.

PubMed ID
10397507 [ View in PubMed
]
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.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
IndomethacinProstaglandin G/H synthase 2IC 50 (nM)500N/AN/ADetails