新型异喹啉 CXCR4 拮抗剂的合成及 SAR 研究及其具有很强的抗 HIV 活性。
Synthesis and SAR of novel isoquinoline CXCR4 antagonists with potent anti-HIV activity.
机构信息
Department of Medicinal Chemistry, Infectious Diseases Center for Excellence in Drug Discovery, GlaxoSmithKline Research and Development, Research Triangle Park, NC 27709-3398, USA.
出版信息
Bioorg Med Chem Lett. 2010 May 15;20(10):3026-30. doi: 10.1016/j.bmcl.2010.03.118.
Using AMD070 as a starting point for structural modification, a novel series of isoquinoline CXCR4 antagonists was developed. A structure-activity scan of alternate lower heterocycles led to the 3-isoquinolinyl moiety as an attractive replacement for benzimidazole. Side chain optimization in the isoquinoline series led to a number of compounds with low nanomolar anti-HIV activities and promising rat PK properties.
以 AMD070 为起点进行结构修饰，开发了一系列新型异喹啉类 CXCR4 拮抗剂。对替代的较低杂环的结构活性扫描导致 3-异喹啉基部分成为苯并咪唑的有吸引力的替代品。异喹啉系列中的侧链优化导致了一些具有低纳摩尔抗 HIV 活性和有前途的大鼠 PK 性质的化合物。
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