Synthesis and structure–activity relationships of 1-phenylpyrazoles as xanthine oxidase inhibitors

…, H Inoue, A Fukunari, M Kamezawa, I Yamada…

Index: Ishibuchi, Seigo; Morimoto, Hiroshi; Oe, Takanori; Ikebe, Tsuguo; Inoue, Hiroyoshi; Fukunari, Atsushi; Kamezawa, Miho; Yamada, Ichimaro; Naka, Yoichi Bioorganic and Medicinal Chemistry Letters, 2001 , vol. 11, # 7 p. 879 - 882

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Citation Number: 86

Abstract

A series of 1-phenylpyrazoles was evaluated for inhibitory activity against xanthine oxidase in vitro. Of the compounds prepared, 1-(3-cyano-4-neopentyloxyphenyl) pyrazole-4- carboxylic acid (Y-700) had the most potent enzyme inhibition and displayed longer-lasting hypouricemic action than did allopurinol in a rat model of hyperuricemia induced by the uricase inhibitor potassium oxonate.