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
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
收藏
页码:2469 / 2473
页数:5
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