Synthesis, in vitro evaluation and molecular docking studies of novel coumarin-isatin derivatives as α-glucosidase inhibitors

被引：33

作者：

Wang, Guangcheng ^{[1
]}

Wang, Jing ^{[1
]}

He, Dianxiong ^{[1
]}

Li, Xin ^{[1
]}

Li, Juan ^{[1
]}

Peng, Zhiyun ^{[1
]}

机构：

[1] Jishou Univ, Coll Chem & Chem Engn, Jishou, Peoples R China

来源：

CHEMICAL BIOLOGY & DRUG DESIGN | 2017年 / 89卷 / 03期

关键词：

coumarin; enzyme kinetic study; isatin; molecular docking; alpha-glucosidase inhibitor; AGENTS; UPDATE;

D O I：

10.1111/cbdd.12867

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

This study synthesized a series of novel coumarin-isatin derivatives and evaluated them for alpha-glucosidase inhibitory activity. The majority of the screened compounds exhibited excellent inhibition activities with IC50 values of 2.56 +/- 0.08-268.79 +/- 3.04 mu m, when compared to acarbose. Among the newly derivatives, compound 5p was found to be the most active compound in the library of coumarin-isatin derivatives. Furthermore, enzyme kinetic studies showed that compound 5p is a non-competitive inhibitor with a K-i of 2.14 mu m. Molecular docking analysis revealed the existence of hydrophobic and hydrogen interactions between compound 5p and the active site of alpha-glucosidase. Our results indicate that coumarin-isatin derivatives as a new class of alpha-glucosidase inhibitors.

引用

页码：456 / 463

页数：8

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