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From indomethacin to a selective COX-2 inhibitor: Development of indolalkanoic acids as potent and selective cyclooxygenase-2 inhibitors

✍ Scribed by W.C. Black; C. Bayly; M. Belley; C.-C. Chan; S. Charleson; D. Denis; J.Y. Gauthier; R. Gordon; D. Guay; S. Kargman; C.K. Lau; Y. Leblanc; J. Mancini; M. Ouellet; D. Percival; P. Roy; K. Skorey; P. Tagari; P. Vickers; E. Wong; L. Xu; P. Prasit

Publisher: Elsevier Science
Year: 1996
Tongue: English
Weight: 307 KB
Volume: 6
Category: Article
ISSN: 0960-894X
DOI: 10.1016/0960-894x(96)00100-x

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✦ Synopsis

A series of potent and highly selective cyclooxygenase-2 inhibitors have been prepared by replacing the benzoyl group of indomethacin with a 4-bromobenzyl group, and by extending the acetic acid side chain. These compounds show anti-inflammatory activity in rats with no evidence of GI toxicity, even at high doses.

Introduction.

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