2-heterosubstituted-3-(4-methylsulfonyl)phenyl-5-trifluoromethyl pyridines as selective and orally active cyclooxygenase-2 inhibitors.
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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.
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- Binding Properties
Drug Target Property Measurement pH Temperature (°C) Indomethacin Prostaglandin G/H synthase 2 IC 50 (nM) 500 N/A N/A Details