Synthesis and antidiabetic activity of 2,5-disubstituted-3-imidazol-2-yl-pyrrolo[2,3-b]pyridines and thieno[2,3-b]pyridines

被引：90

作者：

Bahekar, Rajesh H. ^{[1
]}

Jain, Mukul R. ^{[1
]}

Jadav, Pradip A. ^{[1
]}

Prajapati, Vijay M. ^{[1
]}

Patel, Dipam N. ^{[1
]}

Gupta, Arun A. ^{[1
]}

Sharma, Ajay ^{[1
]}

Tom, Robby ^{[1
]}

Bandyopadhya, Debdutta ^{[1
]}

Modi, Honey ^{[1
]}

Patel, Pankaj R. ^{[1
]}

机构：

[1] Cadila Healthcare Ltd, Zydus Res Ctr, Ahmadabad 382210, Gujarat, India

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2007年 / 15卷 / 21期

关键词：

arylimidazoline; type; 2; diabetes; pyrrolo[2,3-b]pyridine; thieno[2,3-b]pyridine; insulinotropic; antidiabetic;

D O I：

10.1016/j.bmc.2007.08.005

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：

In the present investigation, two series of 2,5-disubstituted-3-imidazol-2-yl-pyrrolo[2,3-b]pyridines (2a-1) and thieno[2,3-b]pyridines (3a-1) were designed as analogs of BL 11282 (1). The in vitro glucose dependent insulinotropic activity of all the test compounds was evaluated using RIN5F cell based assay and all the test compounds showed glucose and concentration dependent insulin secretion. The in vivo antidiabetic activities of most potent compounds from each series (2c and 3c) were assessed in C57BL/6J mice. Compounds 2c and 3c showed dose dependent insulin secretion and significant glucose reduction in vivo. In general, compounds 2c and 3c were found to be equipotent at all the three different doses selected and with respect to BL 11282, both the test compounds were found to be more potent, at all the time points. (C) 2007 Elsevier Ltd. All rights reserved.

引用

页码：6782 / 6795

页数：14

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