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

页码：2475 / 2479

页数：5

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