含氟异喹啉二酮衍生物的合成及其抗马铃薯 Y 病毒活性分析

    Synthesis of Fluorinated Isoquinolindione Derivatives and Analysis of Its Antiviral Activity Against Potato Virus Y

    • 摘要: 为了探索更高抗植物病毒活性的新药物分子,采用较廉价的原料、较温和的反应条件合成了12个含氟基团异喹啉二酮衍生物,并采用半叶枯斑法对合成的目标化合物进行抗马铃薯 Y 病毒(PVY)活性测定。结果表明:含氟异喹啉二酮衍生物对马铃薯 Y 病毒(PVY)具有较好的抑制活性,其中化合物3e的治疗活性(43.5%)、保护活性(47.1%)、钝化活性(51.9%)都表现出较好的效果,与阳性对照农用抗病毒药物病毒唑活性相当,在其结构基础上进行一定的结构修饰,有望得到具有更高抗病毒活性的化合物。

       

      Abstract: In order to explore new drug molecules with higher antiviral activity against plant viruses, 12 fluorinated isoquinolinedione derivatives were synthesized by using cheaper raw materials and milder reaction conditions, and the anti-Potato virus Y (PVY) activity of the synthesized target compounds was determined by using the half-leaf necrosis method. The results showed that the fluorinated isoquinolinedione derivatives had good inhibitory activity against potato virus Y (PVY). Among them, the compound 3e showed good effects in the therapeutic activity (43.5%), protective activity (47.1%) and inactivate activity (51.9%), which was comparable to the positive control agricultural antiviral drug ribavirin. It was expected that the compounds with higher antiviral activity could be obtained by some structural modification on the basis of its structure.

       

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