Discovery of N-benzyl-N'-(4-pipyridinyl)urea CCR5 antagonists as anti-HIV-1 agents (II): modification of the acyl portion期刊界 All Journals 搜尽天下杂志传播学术成果专业期刊搜索期刊信息化学术搜索

Discovery of N-benzyl-N'-(4-pipyridinyl)urea CCR5 antagonists as anti-HIV-1 agents (II): modification of the acyl portion

Authors:	Duan Maosheng Peckham Jennifer Edelstein Mark Ferris Robert Kazmierski Wieslaw M Spaltenstein Andrew Wheelan Pat Xiong Zhiping

Affiliation:	Infectious Diseases Center for Excellence in Drug Discovery, GlaxoSmithKline, Research Ttriangle Park, NC 27709, USA. maosheng.a.duan@gsk.com

Abstract:	Modification of the acyl moiety in the CCR5 lead molecule 2 led to identification of several new classes of CCR5 antagonists. Antiviral activity and pharmacokinetic properties of the synthesized compounds were evaluated. Structure-activity relationship (SAR) derived from these studies further guided the optimization efforts, ultimately leading to the discovery of 36 with an acceptable drug-like profile.

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