Novel N-substituted benzimidazole CXCR4 antagonists as potential anti-HIV agents

被引：83

作者：

Miller, John F. ^{[1
]}

Turner, Elizabeth M. ^{[1
]}

Gudmundsson, Kristjan S. ^{[1
]}

Jenkinson, Stephen ^{[4
]}

Spaltenstein, Andrew ^{[1
]}

Thomson, Michael ^{[2
]}

Wheelan, Pat ^{[3
]}

机构：

[1] GlaxoSmithKline Res & Dev Ltd, Infect Dis Ctr Excellence Drug Discovery, Dept Med Chem, Res Triangle Pk, NC 27709 USA

[2] GlaxoSmithKline Res & Dev Ltd, Infect Dis Ctr Excellence Drug Discovery, Dept Virol, Res Triangle Pk, NC 27709 USA

[3] GlaxoSmithKline Res & Dev Ltd, Infect Dis Ctr Excellence Drug Discovery, Dept DMPK, Res Triangle Pk, NC 27709 USA

[4] GlaxoSmithKline Res & Dev Ltd, Infect Dis Ctr Excellence Drug Discovery, Dept Biochem & Analyt Pharmacol, Res Triangle Pk, NC 27709 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2010年 / 20卷 / 07期

关键词：

CXCR4; Benzimidazole; Tetrahydroquinoline; HIV; Antiviral; IMMUNODEFICIENCY-VIRUS-INFECTION; ENTRY INHIBITORS; THERAPY; TYPE-1;

D O I：

10.1016/j.bmcl.2010.02.053

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The lead optimization of a series of N-substituted benzimidazole CXCR4 antagonists is described. Side chain modifications and stereochemical optimization led to substantial improvements in potency and protein shift to afford compounds with low nanomolar anti-HIV activity. (C) 2010 Elsevier Ltd. All rights reserved.

引用

页码：2125 / 2128

页数：4

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