新型 N-取代苯并咪唑 CXCR4 拮抗剂作为潜在的抗 HIV 药物。
Novel N-substituted benzimidazole CXCR4 antagonists as potential anti-HIV agents.
机构信息
Department of Medicinal Chemistry, Infectious Diseases Center for Excellence in Drug Discovery, GlaxoSmithKline Research and Development, Five Moore Drive, Research Triangle Park, NC 27709-3398, USA.
出版信息
Bioorg Med Chem Lett. 2010 Apr 1;20(7):2125-8. doi: 10.1016/j.bmcl.2010.02.053. Epub 2010 Feb 14.
PMID:20207537
Abstract
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.
摘要
描述了一系列 N-取代苯并咪唑 CXCR4 拮抗剂的先导优化。侧链修饰和立体化学优化导致效力的显著提高，并使化合物发生蛋白位移，从而获得具有低纳摩尔抗 HIV 活性的化合物。
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