Design, Synthesis, and Antiviral Activities of Coumarin Derivatives Containing Dithioacetal Structures

被引:50
作者
Zhao, Lei [1 ]
Zhang, Jian [1 ]
Liu, Ting [1 ]
Mou, Honglan [1 ]
Wei, Chunle [1 ]
Hu, Deyu [1 ]
Song, Baoan [1 ]
机构
[1] Guizhou Univ, Guiyang, Peoples R China
基金
中国国家自然科学基金;
关键词
coumarin; dithioacetal; tobacco mosaic virus; transmission electron microscopy; molecular docking; TOBACCO-MOSAIC-VIRUS; INHIBITORS; DISCOVERY; MOIETY;
D O I
10.1021/acs.jafc.9b06861
中图分类号
S [农业科学];
学科分类号
09 ;
摘要
In this study, a series of coumarin derivatives containing dithioacetals were synthesized, characterized, and assessed for their anti-tobacco mosaic virus (TMV) activities. Biological tests showed that most of the title compounds exhibited significant anti-TMV biological activities; in particular, compound b21 showed good inactivating activity anti-TMV, with an EC50 of 54.2 mg/L, superior to that of ribavirin (134.2 mg/L). Transmission electron microscopy analyses showed that compound 21 severely ruptured TMV particles. The interaction of compound b21 with TMV coat protein (TMV CP) was investigated using microscale thermophoresis and molecular docking. Compound b21 exhibited a strong binding ability to TMV CP, with a value of 2.9 mu M, superior to ribavirin.
引用
收藏
页码:975 / 981
页数:7
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