1,3,4 trisubstituted pyrrolidine CCR5 receptor antagonists bearing 4-aminoheterocycle substituted piperidine side chains

被引：34
作者：
Willoughby, CA
Rosauer, KG
Hale, JJ
Budhu, RJ
Mills, SG
Chapman, KT
MacCoss, M
Malkowitz, L
Springer, MS
Gould, SL
DeMartino, JA
Siciliano, SJ
Cascieri, MA
Carella, A
Carver, G
Holmes, K
Schleif, WA
Danzeisen, R
Hazuda, D
Kessler, J
Lineberger, J
Miller, M
Emini, EA
机构：
[1] Merck Res Labs, Dept Med Chem, Rahway, NJ 07065 USA
[2] Merck Res Labs, Dept Immunol Res, Rahway, NJ 07065 USA
[3] Merck Res Labs, Dept Antiviral Res, W Point, PA 19486 USA
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2003年 / 13卷 / 03期
关键词：
D O I：
10.1016/S0960-894X(02)00988-5
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
A new class of 4-(aminoheterocycle)piperidine derived 1,3,4 trisubstituted pyrrolidine CCR5 antagonists is reported. Compound 4a is shown to have good binding affinity (1.8 nM) and antiviral activity in PBMC's (IC95 = 50 nM). Compound 4a also has improved PK properties relative to 1. (C) 2002 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码：427 / 431
页数：5
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