Amine substituted N-(1H-benzimidazol-2ylmethyl)-5,6,7,8-tetrahydro-8-quinolinamines as CXCR4 antagonists with potent activity against HIV-1

被引：48
|
作者：
Gudmundsson, Kristjan S. [1 ]
Sebahar, Paul R. [1 ]
Richardson, Leah D'Aurora [1 ]
Miller, John F. [1 ]
Turner, Elizabeth M. [1 ]
Catalano, John G. [1 ]
Spaltenstein, Andrew [1 ]
Lawrence, Wendell [2 ]
Thomson, Michael [2 ]
Jenkinson, Stephen [3 ]
机构：
[1] GlaxoSmithKline Res & Dev Ltd, Metab & Virol Ctr Excellence Drug Discovery, Dept Med Chem, Res Triangle Pk, NC 27709 USA
[2] GlaxoSmithKline Res & Dev Ltd, Metab & Virol Ctr Excellence Drug Discovery, Dept Virol, Res Triangle Pk, NC 27709 USA
[3] GlaxoSmithKline Res & Dev Ltd, Metab & Virol Ctr Excellence Drug Discovery, Dept Biochem & Analyt Pharmacol, Res Triangle Pk, NC 27709 USA
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2009年 / 19卷 / 17期
关键词：
CHEMOKINE RECEPTOR CXCR4; PHARMACOKINETICS; MICROENVIRONMENT; INHIBITORS; AMD070; SAFETY; CELLS; ENTRY;
D O I：
10.1016/j.bmcl.2009.07.037
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Several novel amine substituted N-(1H-benzimidazol-2ylmethyl)-5,6,7,8-tetrahydro-8-quinolinamines were synthesized which had potent activity against HIV-1. The synthetic approaches adopted allowed for variation of the substitution pattern and resulting changes in antiviral activity are highlighted. This led to the identification of compounds with low and sub-nanomolar anti-HIV-1 activity. (C) 2009 Elsevier Ltd. All rights reserved.
引用
收藏
页码：5048 / 5052
页数：5
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