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

Authors
Dube, D Brideau, C Deschenes, D Fortin, R Friesen, RW Gordon, R Girard, Y Riendeau, D Savoie, C Chan, CC
Citation
D. Dube et al., 2-heterosubstituted-3-(4-methylsulfonyl)phenyl-5-trifluoromethyl pyridinesas selective and orally active cyclooxygenase-2 inhibitors, BIOORG MED, 9(12), 1999, pp. 1715-1720
Citations number
29
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
9
Issue
12
Year of publication
1999
Pages
1715 - 1720
Database
ISI
SICI code
0960-894X(19990621)9:12<1715:2P>2.0.ZU;2-O
Abstract
A series of novel 2-alkoxy, 2-thioalkoxy and 2-amino-3-(4-methylsulfonyl)ph enylpyridines has been synthesized and shown to be highly potent and select ive cyclooxygenase-2 (COX-2) inhibitors. Structure-activity relationship st udies have demonstrated that central pyridine ring substituents play an imp ortant role in the COX-2 potency, selectivity vs the COX-1 enzyme, and oral activity. (C) 1999 Published by Elsevier Science Ltd. All rights reserved.