基于结构的设计、合成及新型 N-羧基苯基吡咯衍生物作为针对 HIV 融合蛋白 gp41 的融合抑制剂的生物学评价
Structure-based design, synthesis and biological evaluation of new N-carboxyphenylpyrrole derivatives as HIV fusion inhibitors targeting gp41.
机构信息
State Key Laboratory of Respiratory Diseases, Guangzhou Institute of Biomedicine and Health, The Chinese Academy of Sciences, Guangzhou 510663, China.
出版信息
Bioorg Med Chem Lett. 2010 Jan 1;20(1):189-92. doi: 10.1016/j.bmcl.2009.10.139. Epub 2009 Nov 5.
Abstract
A new series of N-carboxyphenylpyrrole ligands were designed using GeometryFit based on an X-ray crystal structure of gp41. The synthesized ligands showed significant inhibitory activities against HIV gp41 6-helix bundle formation, HIV-1 mediated cell-cell fusion and HIV-1 replication.
摘要
设计了一系列新的 N-羧基苯基吡咯配体，使用 GeometryFit 根据 gp41 的 X 射线晶体结构。合成的配体对 HIV gp41 6 螺旋束形成、HIV-1 介导的细胞-细胞融合和 HIV-1 复制具有显著的抑制活性。
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