S0960-894x(96)00100-X From Indomethacin to a Selective Cox-2 Inhibitor: Development of Indolalkanoic Acids as Potent and Selective Cyclooxygenase-2 Inhibitors

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

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S0960-894x(96)00100-X From Indomethacin to a Selective Cox-2 Inhibitor: Development of Indolalkanoic Acids as Potent and Selective Cyclooxygenase-2 Inhibitors

Journal article published in 1996 by W. C. Black, C. Bayly, M. Belley, C. C. Chart, S. Charleson, D. Denis, J. Y. Gauthier, R. Gordon, D. Guay, S. Kargman, C. K. Lau, Y. Leblanc, J. Mancini, M. Ouellet, D. Percival and other authors.

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Abstract

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.