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
王翀 1吴心阳 1杨奇隆 1杨岩 1崔培培1
作者信息
- 1. 太原理工大学生物医学工程学院 晋中 030060
- 折叠
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.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和先导化合物L2.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对TMV的保护活性(36.4％)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.
Abstract
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 exhibit high anti-TMV activities.The inactivation,curative and protective activites of compound 4n(43.5％,40.1％,38.7％)are superior to ribavirin and lead compound L2.The inactivation activities of compounds 4d(40.8％)and 4f(42.0％)are higher than that of ribavirin(38.6％)and lead compound L2(40.5％).The inactivation activity of compound 4I(38.4％)is equivalent to ribavirin(38.6％).The protective activity of compound 4f(36.4％)is equivalent to ribavirin(37.2％).Compound 4n is expected to become a potential antiviral pesticide.
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Key words
Natural product/Echinopsine/Acylhydrazone/Indole/Anti-plant viral activity/Tobacco mosaic virus(TMV)引用本文复制引用
基金项目
国家自然科学基金(22001190)
山西省基础研究计划(20210302123180)
出版年
2024
NETL
NSTL
万方数据