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Substituted piperazines as novel dipeptidyl peptidase IV inhibitors

被引：89
作者：
Brockunier, LL
He, JF
Colwell, LF
Habulihaz, B
He, HB
Leiting, B
Lyons, KA
Marsilio, F
Patel, RA
Teffera, Y
Wu, JK
Thornberry, NA
Ann, 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 / 18期
关键词：
D O I：
10.1016/j.bmcl.2004.06.065
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Incorporation of a fluorophenyl beta-amino amide moiety into piperazine screening lead 2 has resulted in the discovery of a structurally novel series of potent and selective DP-IV inhibitors. Simplification of the molecule and incorporation of multiple fluorine atoms on the phenyl ring has provided low molecular weight analogs such as compound 32, which is a 19 nM DP-IV inhibitor with >4000-fold selectivity over QPP. (C) 2004 Elsevier Ltd. All rights reserved.
引用
收藏
页码：4763 / 4766
页数：4
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