Multifunctional aldose reductase inhibitors based on 2H-benzothiazine 1,1-dioxide

被引：19
作者：
Han, Zhongfei [1 ]
Hao, Xin [1 ]
Gao, Zehong [1 ]
Ma, Bing [1 ]
Zhu, Changjin [1 ]
机构：
[1] Beijing Inst Technol, Dept Appl Chem, 5 Zhongguancun South St, Beijing 100081, Peoples R China
来源：
RSC ADVANCES | 2016年 / 6卷 / 16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：
ACETIC-ACID DERIVATIVES; ANTIOXIDANT ACTIVITY; 5-ARYLIDENE-4-THIAZOLIDINONE DERIVATIVES; DIABETIC COMPLICATIONS; IN-VITRO; POTENT; NEUROPATHY; DESIGN; SCAFFOLD; DOCKING;
D O I：
10.1039/c5ra25984c
中图分类号：
O6 [化学];
学科分类号：
0703 ;
摘要：
A series of benzothiazine derivatives were designed and synthesized for the development of drug candidates for diabetic complications. A number of derivatives having a phenolic hydroxyl-substituted N2-aromatic side chain and a C4-acetic acid head group on the core structure were found to be potent and selective aldose reductase inhibitors. 8a with a phenolic 4-hydroxyl at N2-styryl side chain was proved to be the most active with an IC50 value of 0.094 mu M. All compounds with the N2-styryl side chain showed good antioxidant activity using the DPPH radical scavenging test, and among them, compounds with phenolic hydroxyl-substituted N2-styryl were potent both in activities of ALR2 inhibition and antioxidation. The results suggest a success in the development of multifunctional aldose reductase inhibitors based on the benzothiazine framework.
引用
收藏
页码：12761 / 12769
页数：9
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