Graphite catalyzed solvent free synthesis of dihydropyrimidin-2(1H)-ones/thiones and their antidiabetic activity

被引：84

作者：

Dhumaskar, Kashinath L. ^{[1
]}

Meena, Surya Nandan ^{[2
]}

Ghadi, Sanjeev C. ^{[2
]}

Tilve, Santosh G. ^{[1
]}

机构：

[1] Goa Univ, Dept Chem, Taleigao Plateau 403206, Goa, India

[2] Goa Univ, Dept Biotechnol, Taleigao Plateau 403206, Goa, India

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2014年 / 24卷 / 13期

关键词：

Biginelli reaction; Multicomponent reaction; Solvent less; Graphite catalysis; Dihydropyrimidinones; alpha-Amylase inhibition; Antidiabetic; ONE-POT SYNTHESIS; BIGINELLI REACTION; EFFICIENT SYNTHESIS; GREEN SYNTHESIS; DIHYDROPYRIMIDINONES; ACID; 3,4-DIHYDROPYRIMIDIN-2(1H)-ONES; INHIBITOR; ALDEHYDES; EXTRACT;

D O I：

10.1016/j.bmcl.2014.04.099

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A solvent free three component condensation reaction between an aldehyde, ethyl acetoacetate and urea catalyzed by graphite, a green catalyst is described for the synthesis of dihydropyrimidin-2(1H)-ones. This protocol is scalable and the catalyst is reusable. This method is also applied for the synthesis of dihydropyrimidin-2(1H)-thiones. alpha-Amylase, a key enzyme in carbohydrate metabolism is generally targeted for management of type 2 diabetes. The therapeutic potential of the dihydropyrimidinones and dihydropyrimidinthiones to inhibit alpha-amylase activity was evaluated by in vitro assay. Of the synthesized compounds 3,4-dihydropyrimidin-2(1H)-thione (1k) demonstrated highest inhibition of a-amylase activity. (C) 2014 Elsevier Ltd. All rights reserved.

引用

页码：2897 / 2899

页数：3

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