Indolyl esters and amides related to indomethacin are selective COX-2 inhibitors

…, BC Crews, S Saleh, D Prudhomme, LJ Marnett

Index: Kalgutkar, Amit S.; Crews, Brenda C.; Saleh, Sam; Prudhomme, Daniel; Marnett, Lawrence J. Bioorganic and Medicinal Chemistry, 2005 , vol. 13, # 24 p. 6810 - 6822

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Citation Number: 77

Abstract

Previous studies from our laboratory have revealed that esterification/amidation of the carboxylic acid moiety in the nonsteroidal anti-inflammatory drug, indomethacin, generates potent and selective COX-2 inhibitors. In the present study, a series of reverse ester/amide derivatives were synthesized and evaluated as selective COX-2 inhibitors. Most of the reverse esters/amides displayed time-dependent COX-2 inhibition with IC50 values in the ...