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

被引：116

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

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2001年 / 11卷 / 07期

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 [药物化学];

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.

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页码：879 / 882

页数：4

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