Synthesis and Biological Evaluation of Novel Aryl-2H-pyrazole Derivatives as Potent Non-purine Xanthine Oxidase Inhibitors

被引：11

作者：

Sun, Zhi-Gang ^{[1
]}

Zhou, Xiao-Jing ^{[1
]}

Zhu, Ming-Li ^{[1
]}

Ding, Wen-Ze ^{[1
]}

Li, Zhen ^{[1
]}

Zhu, Hai-Liang ^{[1
]}

机构：

[1] Nanjing Univ, State Key Lab Pharmaceut Biotechnol, Nanjing 210093, Jiangsu, Peoples R China

来源：

CHEMICAL & PHARMACEUTICAL BULLETIN | 2015年 / 63卷 / 08期

关键词：

pyrazole; xanthine oxidase; inhibitory; OXIDOREDUCTASE; DISCOVERY; MECHANISM;

D O I：

10.1248/cpb.c15-00282

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of aryl-2H-pyrazole derivatives were synthesized and evaluated for inhibitory activity against xanthine oxidase in vitro as potent xanthine oxidase inhibitors. Among them, 2 aryl-2H-pyrazole derivatives showed significant inhibitory activities against xanthine oxidase. Compound 19 emerged as the most potent xanthine oxidase inhibitor (IC50=9.8 mu M) in comparison with allopurinol (IC50=9.5 mu M). The docking study revealed that compound 19 might have strong interactions with the active site of xanthine oxidase. This compound is thus a new candidate for further development for the treatment of gout.

引用

页码：603 / 607

页数：5

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