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S-芳基三唑环核苷类似物:针对丙型肝炎病毒的合成与生物学评价。

S-aryltriazole acyclonucleosides: synthesis and biological evaluation against hepatitis C virus.

机构信息

State Key Laboratory of Virology, College of Chemistry and Molecular Sciences, Wuhan University, Wuhan, PR China.

出版信息

Bioorg Med Chem Lett. 2010 Jun 15;20(12):3610-3. doi: 10.1016/j.bmcl.2010.04.115. Epub 2010 Apr 28.

Abstract

Novel S-aryltriazole acyclonucleosides were designed as structural analogs based on the previously identified antiviral aryltriazole acyclonucleosides in our laboratories. These S-aryltriazole nucleosides were synthesized in excellent yields via S(N)Ar-mediated S-arylation, followed by subsequent ammonolysis. X-ray structural analysis revealed special structural feature brought by the S-linkage, which may represent an unfavorable factor contributing to the lack of anti-HCV activity for this family of triazole nucleosides.

摘要

新型 S-芳基三唑环戊核苷类似物是根据我们实验室先前鉴定的具有抗病毒活性的芳基三唑环戊核苷类似物设计的。这些 S-芳基三唑核苷通过 S(N)Ar 介导的 S-芳基化反应以极好的收率合成,然后进行氨解。X 射线结构分析揭示了 S-键带来的特殊结构特征,这可能是该类三唑核苷缺乏抗 HCV 活性的一个不利因素。

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