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：

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：

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

页码：12761 / 12769

页数：9

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