Synthesis and evaluation of 2-phenyl-1,4-butanediamine-based CCR5 antagonists for the treatment of HIV-1

被引：10
作者：
Tallant, Matthew D. [1 ]
Duan, Maosheng [1 ]
Freeman, George A. [1 ]
Ferris, Robert G. [2 ]
Edelstein, Mark P. [2 ]
Kazmierski, Wieslaw M. [1 ]
Wheelan, Pat J. [3 ]
机构：
[1] GlaxoSmithKline Inc, Dept Chem, Res Triangle Pk, NC 27709 USA
[2] GlaxoSmithKline Inc, Dept Virol, Res Triangle Pk, NC 27709 USA
[3] GlaxoSmithKline Inc, ID DMPK, Infect Dis Ctr Excellence Drug Discovery, Res Triangle Pk, NC 27709 USA
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2011年 / 21卷 / 05期
关键词：
CCR5; HIV-1; Diaminobutane; Tropane; Benzimidazole; RECEPTOR; INHIBITORS; DISCOVERY; ENTRY;
D O I：
10.1016/j.bmcl.2011.01.030
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
We describe the synthesis and potency of a novel series of N-substituted 2-phenyl- and 2-methyl-2-phenyl-1,4-diaminobutane- based CCR5 antagonists. Compounds 7a and 12f were found to be potent in anti-HIV assays and bioavailable in the low-dose rat PK model. (C) 2011 Elsevier Ltd. All rights reserved.
引用
收藏
页码：1394 / 1398
页数：5
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