Synthesis and Structure-Activity Relationship Studies of Quinoxaline Derivatives as Aldose Reductase Inhibitors

被引：70

作者：

Wu, Bobin ^{[1
]}

Yang, Yanchun ^{[1
]}

Qin, Xiangyu ^{[1
]}

Zhang, Shuzhen ^{[1
]}

Jing, Chaojun ^{[1
]}

Zhu, Changjin ^{[1
]}

Ma, Bing ^{[1
]}

机构：

[1] Beijing Inst Technol, Dept Appl Chem, Beijing 100081, Peoples R China

来源：

CHEMMEDCHEM | 2013年 / 8卷 / 12期

基金：

中国国家自然科学基金; 高等学校博士学科点专项科研基金;

关键词：

aldehyde reductases; aldose reductases; diabetes complications; inhibitors; polyol pathway; quinoxalines; structure-activity relationships; ACETIC-ACID DERIVATIVES; DIABETIC COMPLICATIONS; ANTIOXIDANT ACTIVITY; ALDEHYDE REDUCTASE; POTENT INHIBITORS; HIGHLY POTENT; SELECTIVITY; 1,1-DIOXIDE; ANTAGONISTS; CONGENERS;

D O I：

10.1002/cmdc.201300324

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

ARIs for diabetes: A series of 2-(3-benzyl-2-oxoquinoxalin-1(2H)-yl)acetic acid derivatives were designed and synthesized as inhibitors of aldose reductase (AR), a novel target for the treatment of diabetes complications. Most of the derivatives proved to be potent and selective, with IC50 values in the low nanomolar to micromolar range. Copyright © 2013 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.

引用

页码：1913 / 1917

页数：5

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