发现 N-苄基-N'-(4-哌啶基)脲 CCR5 拮抗剂作为抗 HIV-1 药物（二）：酰基部分的修饰。
Discovery of N-benzyl-N'-(4-pipyridinyl)urea CCR5 antagonists as anti-HIV-1 agents (II): modification of the acyl portion.
机构信息
Infectious Diseases Center for Excellence in Drug Discovery, GlaxoSmithKline, Research Ttriangle Park, NC 27709, USA.
出版信息
Bioorg Med Chem Lett. 2010 Dec 15;20(24):7401-4. doi: 10.1016/j.bmcl.2010.10.042. Epub 2010 Oct 21.
PMID:21055933
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.
摘要
对 CCR5 先导分子 2 的酰基部分进行修饰，鉴定出了几类新的 CCR5 拮抗剂。评估了合成化合物的抗病毒活性和药代动力学性质。从这些研究中得出的构效关系 (SAR) 进一步指导了优化工作，最终发现了具有可接受的类药性的 36。
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