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Flavonoid-triazolyl hybrids as potential anti-hepatitis C virus agents: Synthesis and biological evaluation

机译:黄酮类三唑基杂交种作为潜在的抗丙型肝炎病毒剂:合成和生物学评估

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摘要

A series of flavonoid-triazolyl hybrids were synthesized and evaluated as novel inhibitors of hepatitis C virus (HCV). The results of anti-HCV activity assays showed that most of the synthesized derivatives at a concentration of 100 mu g/mL inhibited the generation of progeny virus. Among these derivatives, 10m and 10r exhibited the most potent anti-HCV activity and inhibited the production of HCV in a dose-dependent manner. Interestingly, 10m and 10r had no significant inhibitory effect on viral translation or replication. Additional action mechanism studies revealed that the most potent compounds, 10m and 10r, significantly inhibited viral entry to 34.0% and 52.0%, respectively, at 10 mu M. These results suggest further effective application of 10m and 10r as potential HCV preventive agents. (c) 2021 Elsevier Masson SAS. All rights reserved.
机译:合成了一系列黄酮类三唑基杂化物,并对其作为新型丙型肝炎病毒(HCV)抑制剂进行了评价。抗-HCV活性检测结果表明,大多数合成的衍生物在100μg/mL浓度下抑制子代病毒的产生。在这些衍生物中,10m和10r表现出最强的抗HCV活性,并以剂量依赖性方式抑制HCV的产生。有趣的是,10m和10r对病毒的翻译或复制没有明显的抑制作用。进一步的作用机制研究表明,最有效的化合物10m和10r在10μM浓度下分别显著抑制病毒进入34.0%和52.0%。这些结果表明,10m和10r作为潜在的HCV预防剂可以进一步有效地应用。(c)2021爱思唯尔马松SAS。版权所有。

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