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Discovery of novel indole derivatives containing dithioacetal as potential antiviral agents for plants
Pesticide Biochemistry and Physiology ( IF 4.7 ) Pub Date : 2020-06-01 , DOI: 10.1016/j.pestbp.2020.104568
Chunle Wei 1 , Lei Zhao 1 , Zhongrong Sun 1 , Deyu Hu 1 , Baoan Song 1
Affiliation  

Thirty unreported indole derivatives containing dithioacetal moiety were synthesized and evaluated for anti-plant viral activity. Bioassay results displayed that some of the target compounds showed better activities against tobacco mosaic virus (TMV) than the commercial Ribavirin in vivo. In particular, anti-TMV curative, protective and inactivating activity of 4p were 55.1, 57.2, and 80.3%, respectively, and EC50 value for inactivating activity was 88.5 μg/mL. The observation of transmission electron microscope showed that 4p may have a certain destructive effect on TMV particles. To further study, microscale thermophoresis analysis result also demonstrated that 4p powerfully interacted with TMV coat protein in vitro. Hence, this study provides a strong evidence suporting that indole derivatives might be applied as new antiviral agents.

中文翻译:

发现含有二硫缩醛的新型吲哚衍生物作为潜在的植物抗病毒剂

合成了三十种未报道的含有二硫缩醛部分的吲哚衍生物,并评估了其抗植物病毒活性。生物测定结果表明,一些目标化合物在体内表现出比商业病毒唑更好的抗烟草花叶病毒 (TMV) 活性。特别是4p的抗TMV治疗、保护和灭活活性分别为55.1%、57.2%和80.3%,灭活活性的EC50值为88.5 μg/mL。透射电镜观察表明4p可能对TMV颗粒有一定的破坏作用。为了进一步研究,微尺度热泳分析结果还表明4p在体外与TMV外壳蛋白有很强的相互作用。因此,这项研究提供了强有力的证据,支持吲哚衍生物可能用作新的抗病毒药物。
更新日期:2020-06-01
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