| 王翀,吴心阳,杨奇隆,杨岩,崔培培.化学通报,2024,87(5):612-619,539. |
| 含酰腙吲哚片段的蓝刺头碱衍生物的设计、合成及抗烟草花叶病毒活性 |
| Design, Synthesis and Anti-Tobacco Mosaie Virus Activities of Echinopsine Derivatives Containing Acylhydrazone Indole Fragment |
| 投稿时间：2023-12-13 修订日期：2024-01-15 |
| DOI： |
| 中文关键词: 天然产物 蓝刺头碱；酰腙；吲哚 抗植物病毒活性；烟草花叶病毒 |
| 英文关键词:natural product echinopsine acylhydrazone indole anti-plant viral activity tobacco mosaic virus(TMV) |
| 基金项目:国家自然科学基金项目(22001190)和山西省基础研究计划项目(20210302123180)资助 |
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| 中文摘要: |
| 为了发现高活性的抗病毒化合物，以蓝刺头碱为先导，运用骨架跃迁策略，设计合成了15个含有酰腙吲哚片段的蓝刺头碱衍生物，并通过1H NMR、13C NMR和HRMS确证了其结构，研究了其对烟草花叶病毒（TMV）的钝化、治疗和保护活性。研究结果表明，部分化合物具有较高的抗TMV活性。其中，化合物4n（43.5%，40.1%，38.7%）抗TMV的钝化、治疗和保护活性高于病毒唑（38.6%，36.5%，37.2%）和先导化合物L2（40.5%，34.7%，38.3%）。化合物4d（40.8%）、4f（42.0%）对TMV的钝化活性优于病毒唑（38.6%）和先导化合物L2（40.5%）。化合物4I（38.4%）对TMV的钝化活性与病毒唑（38.6%）相当。化合物4f（36.4%）对TMV的保护活性与病毒唑（37.2%）相当。化合物4n有望成为一种潜在的抗病毒农药。 |
| 英文摘要: |
| In order to discover highly active antiviral compounds, echinopsine was used as the lead and 15 echinopsine derivatives containing the acylhydrazone indole fragments were designed and synthesized by scaffold hopping strategy. Their structures were characterized using 1H NMR, 13C NMR and HRMS. The in vivo antiviral activities against tobacco mosaic virus (TMV) were evaluated in three modes (inactivation, curative, and protective). Bioassay results revealed that some compounds exhibited high anti-TMV activities. The inactivation, curative and protective activites of compound 4n (43.5%, 40.1%, 38.7%) were superior to ribavirin (38.6%, 36.5%, 37.2%) and lead compound L2(40.5%, 34.7%, 38.3%). The inactivation activities of compounds 4d (40.8%) and 4f (42.0%)were higher than that of ribavirin (38.6%) and lead compound L2 (40.5%). The inactivation activity of compound 4I (38.4%) was equivalent to ribavirin (38.6%). The protective activity of compound 4f (36.4%) was equivalent to ribavirin (37.2%). Compound 4n was expected to become a potential antiviral pesticide. |
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