Potent and selective proline derived dipeptidyl peptidase IV inhibitors

被引：49

作者：

Edmondson, SD

Mastracchio, A

Beconi, M

Colwell, LF

Habulihaz, B

He, HB

Kumar, SJ

Leiting, B

Lyons, KA

Mao, A

Marsilio, F

Patel, RA

Wu, JK

Zhu, L

Thornberry, NA

Weber, AE

Parmee, ER

机构：

[1] Merck & Co Inc, Dept Med Chem, Rahway, NJ 07065 USA

[2] Merck & Co Inc, Dept Drug Metab, Rahway, NJ 07065 USA

[3] Merck & Co Inc, Dept Metab Disorders, Rahway, NJ 07065 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2004年 / 14卷 / 20期

关键词：

dipeptidyl peptidase IV; selective; proline amide; thiazolidine; type; 2; diabetes;

D O I：

10.1016/j.bmcl.2004.07.056

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

In-house screening of the Merck sample collection identified proline derived homophenylalanine 3 as a DPP-IV inhibitor with modest potency (DPP-IV IC50 = 1.9 muM). Optimization of 3 led to compound 37, which is among the most potent and selective DPP-IV inhibitors discovered to date. (C) 2004 Elsevier Ltd. All rights reserved.

引用

收藏

页码：5151 / 5155

页数：5

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