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

被引:117
作者
Ishibuchi, S
Morimoto, H
Oe, T
Ikebe, T
Inoue, H
Fukunari, A
Kamezawa, M
Yamada, I
Naka, Y
机构
[1] Welfide Corp, Drug Discovery Res Labs, Hirakata, Osaka 5731153, Japan
[2] Welfield Corp, Drug Dev Labs, Fukuoka 8718550, Japan
[3] Kurume Univ, Sch Med, Radioisotope Inst Basic & Clin Med, Kurume, Fukuoka 8300011, Japan
关键词
D O I
10.1016/S0960-894X(01)00093-2
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
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. (C) 2001 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码:879 / 882
页数:4
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