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首页> 外文期刊>Bioorganic and Medicinal Chemistry Letters >Design and synthesis of spirocyclic compounds as HCV replication inhibitors by targeting viral NS4B protein
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Design and synthesis of spirocyclic compounds as HCV replication inhibitors by targeting viral NS4B protein

机译：通过靶向病毒NS4B蛋白设计和合成作为HCV复制抑制剂的螺环化合物

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摘要

Two novel series of spirocyclic piperidine analogs appended to a pyrazolo[1,5-a]pyridine core were designed, synthesized and evaluated for their anti-HCV activity. A series of piperidine ketals afforded dispiro 6p which showed excellent in vitro anti-HCV activities (EC50 of 1.5 nM and 1.2 nM against genotype 1a and 1b replicons, respectively). A series of piperidine oxazolidinones afforded 27c which showed EC50's of 10.9 nM and 6.1 nM against 1a and 1b replicons, respectively. Both compounds 6p and 27c bound directly to non-structural NS4B protein in vitro (IC50's = 10.2 and 30.4 nM, respectively) and exhibited reduced potency in replicons containing resistance mutations encoding changes in the NS4B protein.
机译：设计，合成和评估了两个新的螺环哌啶类似物系列，它们附加到吡唑并[1,5-a]吡啶核上，并评估其抗HCV活性。一系列哌啶缩酮提供了dispiro 6p，该化合物具有出色的体外抗HCV活性（针对基因型1a和1b复制子的EC50分别为1.5 nM和1.2 nM）。一系列哌啶恶唑烷酮提供27c，相对于1a和1b复制子，其EC50分别为10.9 nM和6.1 nM。化合物6p和27c在体外都直接与非结构NS4B蛋白结合（分别为IC50's = 10.2和30.4 nM），并且在包含编码NS4B蛋白变化的抗性突变的复制子中显示出降低的效价。

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