FROM INDOMETHACIN TO A SELECTIVE COX-2 INHIBITOR - DEVELOPMENT OF INDOLALKANOIC ACIDS AS POTENT AND SELECTIVE CYCLOOXYGENASE-2 INHIBITORS

Authors
BLACK WC BAYLY C BELLEY M CHAN CC CHARLESON S DENIS D GAUTHIER JY GORDON R GUAY D KARGMAN S LAU CK LEBLANC Y MANCINI J OUELLET M PERCIVAL D ROY P SKOREY K TAGARI P VICKERS P WONG E XU L PRASIT P
Citation
Wc. Black et al., FROM INDOMETHACIN TO A SELECTIVE COX-2 INHIBITOR - DEVELOPMENT OF INDOLALKANOIC ACIDS AS POTENT AND SELECTIVE CYCLOOXYGENASE-2 INHIBITORS, Bioorganic & medicinal chemistry letters, 6(6), 1996, pp. 725-730
Citations number
24
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
6
Issue
6
Year of publication
1996
Pages
725 - 730
Database
ISI
SICI code
0960-894X(1996)6:6<725:FITASC>2.0.ZU;2-5
Abstract
A series of potent and highly selective cyclooxygenase-2 inhibitors ha ve been prepared by replacing the benzoyl group of indomethacin with a 4-bromobenzyl group, and by extending the acetic acid side chain. The se compounds show anti-inflammatory activity in rats with no evidence of GI toxicity, even at high doses.