Novel synthesis of nitro-quinoxalinone derivatives as aldose reductase inhibitors

被引：17

作者：

Hussain, Saghir ^{[1
]}

Parveen, Shagufta ^{[1
]}

Qin, Xiangyu ^{[1
]}

Hao, Xin ^{[1
]}

Zhang, Shuzhen ^{[1
]}

Chen, Xin ^{[1
]}

Zhu, Changjin ^{[1
]}

Ma, Bing ^{[1
]}

机构：

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

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2014年 / 24卷 / 09期

基金：

高等学校博士学科点专项科研基金; 中国国家自然科学基金;

关键词：

Quinoxalinone derivatives; Aldose reductase inhibitors; Structure-activity relationship; DIABETIC COMPLICATIONS; POTENT; RAT; PREVENTION; NEUROPATHY; CATARACT; AGENTS;

D O I：

10.1016/j.bmcl.2014.03.053

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A novel, non-acid series of nitroquinoxalinone derivatives was synthesized and tested for their inhibitory activity against aldose reductase as targeting enzyme. All active compounds displayed an 8-nitro group, and showed significant activity in IC50 values ranging from 1.54 to 18.17 mu M. Among them 6,7-dichloro-5,8-dinitro-3-phenoxyquinoxalin-2(H-1)-one (7e), exhibited the strongest aldose reductase activity with an IC50 value of 1.54 mu M and a good SAR (structure-activity relationship) profile. (C) 2014 Elsevier Ltd. All rights reserved.

引用

页码：2086 / 2089

页数：4

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