Design, synthesis, and biological evaluation of 6-substituted-3-(4-methanesulfonylphenyl)-4-phenylpyran-2-ones: a novel class of diarylheterocyclic selective …

PN Praveen Rao, M Amini, H Li…

Index: Rao, P.N. Praveen; Amini, Mohsen; Li, Huiying; Habeeb, Amgad G.; Knaus, Edward E. Journal of Medicinal Chemistry, 2003 , vol. 46, # 23 p. 4872 - 4882

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Citation Number: 74

Abstract

A group of 6-alkyl (alkoxy or alkylthio)-4-aryl-3-(4-methanesulfonylphenyl) pyran-2-ones (14a-v), possessing either a H or F substituent at the para-position of the C-4 phenyl ring, were designed for evaluation as selective cyclooxygenase-2 (COX-2) inhibitors with in vivo antiinflammatory-analgesic activities. Although 6-ethylthio-3-(4-methanesulfonylphenyl)-4- phenylpyran-2-one (14s) exhibited a very high in vitro COX-2 inhibitory potency (IC50= ...