Synthesis and glycosidase inhibitory activity of novel (2-phenyl-4H-benzopyrimedo[2,1-b]-thiazol-4-yliden)acetonitrile derivatives

被引：16

作者：

Patil, Vijay S. ^{[2
,4
]}

Nandre, Kamalakar P. ^{[3
]}

Ghosh, Sougata ^{[1
]}

Rao, Vaidya Jayathirtha ^{[4
]}

Chopade, Balu A. ^{[1
]}

Bhosale, Sheshanath V. ^{[5
]}

Bhosale, Sidhanath V. ^{[2
,3
]}

机构：

[1] Univ Pune, Inst Bioinformat & Biotechnol, Pune 411007, Maharashtra, India

[2] N Maharashtra Univ, Dept Organ Chem, Jalgaon 425001, India

[3] CSIR Indian Inst Chem Technol, Polymers & Funct Mat Div, Hyderabad 500607, Andhra Pradesh, India

[4] CSIR Indian Inst Chem Technol, Div Crop Protect Chem, Hyderabad 500607, Andhra Pradesh, India

[5] RMIT Univ, Sch Appl Sci, Melbourne, Vic 3001, Australia

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2012年 / 22卷 / 23期

关键词：

2-Aminobenzothiazoles; Glycosidase inhibitors; Porcine pancreatic alpha-amylase; Murine intestinal glycosidase; ALPHA-GLUCOSIDASE; ACARBOSE; AGENTS;

D O I：

10.1016/j.bmcl.2012.10.025

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of (2-phenyl-4H-benzopyrimodo[2,1-b][1,3]thiazol-4-yliden-4-yliden)acetonitrile derivatives have been prepared by ring transformation reaction of 4-(methylthio)-2-oxo-6-aryl-2H-pyrane-3-carbonitriles. The yield of ring transformation product is moderate to good. Furthermore the glycosidase inhibitory activities were tested by using a-amylase and a-glucosidase pancreatic, intestinal and liver enzymes, responsible for hyperglycemia in type II diabetes. The results revealed that all compounds exhibit significant glycosidase inhibitory activity. (C) 2012 Elsevier Ltd. All rights reserved.

引用

页码：7011 / 7014

页数：4

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