Imidazopiperidine amides as dipeptidyl peptidase IV inhibitors for the treatment of diabetes

被引：22

作者：

Chen, Ping

Caldwell, Charles G.

Mathvink, Robert J.

Leiting, Barbara

Marsilio, Frank

Patel, Reshma A.

Wu, Joseph K.

He, Hualbing

Lyons, Kathryn A.

Thornberry, Nancy A.

Weber, Ann E.

机构：

[1] Merck Res Lab, Dept Med Chem, Rahway, NJ 07065 USA

[2] Mol Therapeut Lab, Dept Metab Dis Diabet, Rahway, NJ 07065 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2007年 / 17卷 / 21期

关键词：

dipeptidyl peptidase IV inhibitors; diabetes; glucagon-like; peptide-1 (GLP-1); incretin hormones; imidazopiperidine amides;

D O I：

10.1016/j.bmcl.2007.08.030

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of substituted imidazopiperidine amides has been prepared and evaluated for inhibition of dipeptidyl peptidase IV (PP-4). Substitution at the 1- and 3-positions produced increased selectivity for DPP-4 relative to DPP-8 and DPP-9. Compounds in this series had IC50 values as low as 5.8 nM for inhibition of DPP-4. Published by Elsevier Ltd.

引用

收藏

页码：5853 / 5857

页数：5

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