Novel N-substituted 4-hydrazino piperidine derivative as a dipeptidyl peptidase IV inhibitor

被引：7

作者：

Gupta, Ramesh C. ^{[1
]}

Chhipa, Laxmikant ^{[1
]}

Mandhare, Appaji B. ^{[1
]}

Zambad, Shitalkumar P. ^{[2
]}

Chauthaiwale, Vijay ^{[3
]}

Nadkarni, Sunil S.

Dutt, Chaitanya

机构：

[1] Torrent Pharmaceut Ltd, Torrent Res Ctr, Med Chem, Gandhinagar 382428, Gujarat, India

[2] Torrent Pharmaceut Ltd, Torrent Res Ctr, Pharmacology, Gandhinagar 382428, Gujarat, India

[3] Torrent Pharmaceut Ltd, Torrent Res Ctr, Discovery Res, Gandhinagar 382428, Gujarat, India

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2009年 / 19卷 / 17期

关键词：

DPP IV inhibitors; GLP-1; N-Substituted 4-hydrazino piperidine; Type-2; diabetes; POTENT; DISCOVERY;

D O I：

10.1016/j.bmcl.2009.07.058

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A novel class of N-substituted 4-hydrazino piperidine derivatives were designed, synthesized and evaluated for DPP IV inhibition. The SAR studies on the N-substituted piperidine led to the discovery of compound 22e as a potent DPP IV inhibitor (IC(50) 88 nM), which is highly selective over other peptidases. In vivo efficacy indicates that compound 22e stimulates insulin release in response to glucose load and improves glucose tolerance in n5-STZ and Zucker Diabetic Fatty (ZDF) rats. (C) 2009 Elsevier Ltd. All rights reserved.

引用

页码：5021 / 5025

页数：5

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