Synthesis and bioevaluation of 2-phenyl-5-methyl-2H-1,2,3-triazole-4-carboxylic acid/carbohydrazide derivatives as potent xanthine oxidase inhibitors

被引：0

作者：

Shi A. ^{[1
,2
]}

Wang D. ^{[1
]}

Wang H. ^{[1
]}

Wu Y. ^{[1
]}

Tian H. ^{[1
]}

Guan Q. ^{[2
]}

Bao K. ^{[1
]}

Zhang W. ^{[1
]}

机构：

[1] Key Laboratory of Structure-Based Drug Design and Discovery, Ministry of Education, Shenyang Pharmaceutical University, Shenyang

[2] School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Shenyang

来源：

Guan, Qi (guanqi@syphu.edu.cn) | 1600年 / Royal Society of Chemistry卷 / 06期

基金：

中国国家自然科学基金;

关键词：

801.4 Physical Chemistry;

D O I：

10.1039/C6RA24651F

中图分类号：

学科分类号：

摘要：

A series of 2-phenyl-5-methyl-2H-1,2,3-triazole-4-carboxylic acids/carbohydrazides as analogues of febuxostat were synthesized and evaluated for their in vitro xanthine oxidase (XO) inhibitory activity. Among these compounds, the carboxylic acid derivatives 7a-h and 8a-h exhibited high potency in the submicromolar/nanomolar range. Steady-state kinetics experiment revealed that 7f was a mixed-type inhibitor of xanthine oxidase. In addition, a molecular docking study of 7f was performed to determine its binding mode at the active site of xanthine oxidase. © The Royal Society of Chemistry.

引用

页码：114879 / 114888

页数：9

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