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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