A new series of N2-substituted-5-(p-toluenesulfonylamino)phthalimide analogues as α-glucosidase inhibitors

被引：18

作者：

Bian, Xiaoli ^{[1
]}

Wang, Qian ^{[2
]}

Ke, Changhu ^{[1
]}

Zhao, Guilan ^{[1
]}

Li, Yiping ^{[1
]}

机构：

[1] Xi An Jiao Tong Univ, Coll Pharm, Xian 710061, Shaanxi Provinc, Peoples R China

[2] Shaanxi Univ Sci & Technol, Dept Pharm, Coll Life Sci & Engn, Xian 710021, Peoples R China

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2013年 / 23卷 / 07期

基金：

中国国家自然科学基金;

关键词：

5-(p-Toluenesulfonylamino)phthalimide; alpha-Glucosidase inhibitors; Postprandial hyperglycemia; Diabetes; CARDIOVASCULAR-DISEASE; COMPLICATIONS;

D O I：

10.1016/j.bmcl.2013.02.011

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Several members of a new family of non-sugar-type alpha-glycosidase inhibitors, bearing a 5-(p-toluenesulfonylamino)phthalimide moiety and various substituent at the N2 position, were synthesized and their activities were investigated. The newly synthesized compounds displayed different inhibition profile towards yeast alpha-glycosidase and rat intestinal alpha-glycosidase. Almost all the compounds had strong inhibitory activities against yeast alpha-glycosidase. Regarding rat intestinal alpha-glycosidase, only analogs with N2-aromatic substituents displayed varying degrees of inhibitory activities on rat intestinal maltase and lactase and nearly all compounds showed no inhibition against rat intestinal alpha-amylase. Structure-activity relationship studies indicated that 5-(p-toluenesulfonylamino)phthalimide moiety is a favorable scaffold to exert the alpha-glucosidase inhibitory activity and substituents at the N2 position have considerable influence on the efficacy of the inhibition activities. (C) 2013 Elsevier Ltd. All rights reserved.

引用

页码：2022 / 2026

页数：5

共 24 条

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