Novel synthesis of nitro-quinoxalinone derivatives as aldose reductase inhibitors

被引：16
|
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：
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：
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
收藏
页码：2086 / 2089
页数：4
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