Antagonists of the human CCR5 receptor as anti-HIV-1 agents.: Part 4:: Synthesis and structure-activity relationships for 1-[N(methyl)-N-(phenylsulfonyl)amino]-2-(phenyl)-4-(4-(N-(alkyl)-N- (benzyloxycarbonyl)amino)piperidin-1-yl)butanes

被引：90
|
作者：
Finke, PE
Oates, B
Mills, SG
MacCoss, M
Malkowitz, L
Springer, MS
Gould, SL
DeMartino, JA
Carella, A
Carver, G
Holmes, K
Danzeisen, R
Hazuda, D
Kessler, J
Lineberger, J
Miller, M
Schleif, WA
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 | 2001年 / 11卷 / 18期
关键词：
D O I：
10.1016/S0960-894X(01)00492-9
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
(2S)-2-(3-Chlorophenyl)-1-[N-(methyl)-N-(phenylsulfonyl)amino]-4-[spiro(2,3-dihydrobenzthiophene-3,4 ' -piperidin-1 ' -yl)]butane S-oxide (lb) has been identified as a potent CCR5 antagonist having an IC50 = 10 nM. Herein, structure-activity relationship studies of non-spiro piperidines are described, which led to the discovery of 4-(N-(alkyl)-N-(benzyloxy-carbonyl)amino)piperidine derivatives (3-5) as potent CCR5 antagonists. (C) 2001 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码：2475 / 2479
页数：5
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