Synthesis and evaluation of the α-glucosidase inhibitory activity of 3-[4-(phenylsulfonamido)benzoyl]-2H-1-benzopyran-2-one derivatives

被引：33

作者：

Wang, Shaojie ^{[1
]}

Yan, Jufang ^{[2
]}

Wang, Xiaoyan ^{[1
]}

Yang, Zhuo ^{[1
]}

Lin, Fengwei ^{[1
]}

Zhang, Tingjian ^{[1
]}

机构：

[1] Shenyang Pharmaceut Univ, Key Lab New Drugs Design & Discovery Liaoning Pro, Shenyang 110016, Peoples R China

[2] Drug Screening Ctr, Di Ao Pharmaceut Grp, Chengdu 123388, Peoples R China

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2010年 / 45卷 / 03期

关键词：

Chalcone; 3-[4-(Phenylsulfonamido)benzoyl]-2H-1-benzopyran-2-one; alpha-Glucosidase inhibitor; BIOLOGICAL EVALUATION; CHALCONE DERIVATIVES; SULFONAMIDE CHALCONE; SAR;

D O I：

10.1016/j.ejmech.2009.12.031

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

In the course of studies directed toward the discovery of novel non-sugar a-glucosidase inhibitors for the treatment of diabetes, a series of 3-[4-(phenylsulfonamido)benzoyl]-2H-1-benzopyran-2-one derivatives was synthesized and evaluated as a-glucosidase inhibitors. Most compounds showed good inhibitory activity with IC(50) values ranging from 0.0645 mu M to 26.746 mu M. 7-Hydroxy-6-methoxy-3-[4-(4-methylphenylsulfonamido)benzoyl]-2H-1-benzopyran-2-one 7u manifested the most potent inhibitory activity with an IC(50) value of 0.0645 mu M. (C) 2009 Elsevier Masson SAS. All rights reserved.

引用

页码：1250 / 1255

页数：6

共 21 条

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