Antagonists of the human CCR5 receptor as anti-HIV-1 agents.: Part 3:: A proposed pharmacophore model for 1-[N-(methyl)-N-(phenylsulfonyl)amino]-2-(phenyl)4-[4-(substituted)piperidin-1yl]butanes

被引：44

作者：

Finke, PE

Meurer, LC

Oates, B

Shah, SK

Loebach, JL

Mills, SG

MacCoss, M

Castonguay, L

Malkowitz, L

Springer, MS

Gould, SL

DeMartino, JA

机构：

[1] Merck Res Labs, Dept Med Chem, Rahway, NJ 07065 USA

[2] Merck Res Labs, Dept Mol Syst, Rahway, NJ 07065 USA

[3] Merck Res Labs, Dept Immunol Res, Rahway, NJ 07065 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2001年 / 11卷 / 18期

关键词：

D O I：

10.1016/S0960-894X(01)00491-7

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Structure-activity relationship studies directed toward the optimization of (2S)-2-(3-chlorophenyl)-1-[N-(methyl)-N-(phenylsulfonyl)amino]-4-[-(substituted)piperidin-1-yl]butanes as CCR5 antagonists resulted in the synthesis of the spiro-indanone derivative 8c (IC50 = 5 nM). These and previous results are summarized in a proposed pharmacophore model for this class of CCR5 antagonist. (C) 2001 Elsevier Science Ltd. All rights reserved.

引用

页码：2469 / 2473

页数：5

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