Structure-based design and synthesis of benzimidazole derivatives as dipeptidyl peptidase IV inhibitors

被引：48

作者：

Wallace, Michael B. ^{[1
]}

Feng, Jun ^{[1
]}

Zhang, Zhiyuan ^{[1
]}

Skene, Robert J. ^{[1
]}

Shi, Lihong ^{[1
]}

Caster, Christopher L. ^{[1
]}

Kassel, Daniel B. ^{[1
]}

Xu, Rongda ^{[1
]}

Gwaltney, Stephen L., II ^{[1
]}

机构：

[1] Takeda San Diego, Drug Discovery, San Diego, CA 92121 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2008年 / 18卷 / 07期

关键词：

dipeptidyl peptidase IV; DPP-4; benzimidazole; diabetes; X-ray structure;

D O I：

10.1016/j.bmcl.2008.02.071

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A novel series of non-covalent, benzimidazole-based inhibitors of DPP-4 has been developed from a small fragment hit using structure-based drug design. A highly versatile synthetic route was created for the development of SAR, which led to the discovery of potent and selective inhibitors with excellent pharmaceutical properties. (C) 2008 Elsevier Ltd. All rights reserved.

引用

页码：2362 / 2367

页数：6

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