发现 N-苄基-N'-(4-哌啶基)脲 CCR5 拮抗剂作为抗 HIV-1 药物 (I): 胺部分的优化。
Discovery of N-benzyl-N'-(4-pipyridinyl)urea CCR5 antagonists as anti-HIV-1 agents (I): optimization of the amine portion.
机构信息
Infectious Diseases Center for Excellence in Drug Discovery, GlaxoSmithKline, Research Triangle Park, NC 27709, USA.
出版信息
Bioorg Med Chem Lett. 2010 Dec 15;20(24):7397-400. doi: 10.1016/j.bmcl.2010.10.033. Epub 2010 Oct 12.
PMID:21035337
Abstract
Several series of carbamate, urea and carboxamide-based CCR5 antagonists have been discovered via optimizations at the amine portion of lead compound 2. All compounds were evaluated for their antiviral activities. Lead urea 29 showed good pharmacokinetic properties, justifying further development of this series.
摘要
通过对先导化合物 2 胺部分的优化，发现了几系列氨基甲酸酯、脲和酰胺基 CCR5 拮抗剂。所有化合物均进行了抗病毒活性评价。先导脲 29 表现出良好的药代动力学特性，证明了该系列的进一步开发是合理的。
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