Ester and amide derivatives of the nonsteroidal antiinflammatory drug, indomethacin, as selective cyclooxygenase-2 inhibitors

AS Kalgutkar, AB Marnett, BC Crews…

Index: Kalgutkar, Amit S.; Marnett, Alan B.; Crews, Brenda C.; Remmel, Rory P.; Marnett, Lawrence J. Journal of Medicinal Chemistry, 2000 , vol. 43, # 15 p. 2860 - 2870

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Citation Number: 329

Abstract

Recent studies from our laboratory have shown that derivatization of the carboxylate moiety in substrate analogue inhibitors, such as 5, 8, 11, 14-eicosatetraynoic acid, and in nonsteroidal antiinflammatory drugs (NSAIDs), such as indomethacin and meclofenamic acid, results in the generation of potent and selective cyclooxygenase-2 (COX-2) inhibitors (Kalgutkar et al. Proc. Natl. Acad. Sci. USA 2000, 97, 925-930). This paper summarizes ...