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
收藏
页码：114879 / 114888
页数：9
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