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含噻吩嘧啶的二硫缩醛衍生物的设计、合成、抗番茄斑萎病毒活性及作用机制。

Design, Synthesis, Anti-Tomato Spotted Wilt Virus Activity, and Mechanism of Action of Thienopyrimidine-Containing Dithioacetal Derivatives.

机构信息

State Key Laboratory Breeding Base of Green Pesticide and Agricultural Bioengineering, Key Laboratory of Green Pesticide and Agricultural Bioengineering, Ministry of Education, Guizhou University, Huaxi District, Guiyang 550025, China.

出版信息

J Agric Food Chem. 2022 May 25;70(20):6015-6025. doi: 10.1021/acs.jafc.2c00773. Epub 2022 May 16.

Abstract

Currently, there is insufficient viricide to effectively control tomato spotted wilt virus (TSWV). To address this pending issue, a series of thienopyrimidine-containing dithioacetal derivatives were prepared and tested for their anti-TSWV activities. A subsequent three-dimensional quantitative structure-activity relationship was constructed to indicate the development of optimal compound . The obtained compound had excellent anti-TSWV curative, protective, and inactivating activities (63.0, 56.6, and 74.1%, respectively), and the EC values of protective and inactivating activities of compound were 252.8 and 113.5 mg/L, respectively, better than those of ningnanmycin (284.8 and 144.7 mg/L) and xiangcaoliusuobingmi (624.9 and 300.0 mg/L). In addition, the anti-TSWV activity of compound was associated with defense-related enzyme activities, enhanced photosynthesis, and reduced stress response, thereby enhancing disease resistance.

摘要

目前,用于有效控制番茄斑萎病毒(TSWV)的杀病毒剂还不够。为了解决这一待解决的问题,合成了一系列含噻吩嘧啶的二硫缩醛衍生物,并对其抗 TSWV 活性进行了测试。随后构建了三维定量构效关系,以指示最佳化合物的开发。得到的化合物具有优异的抗 TSWV 治疗、保护和失活活性(分别为 63.0%、56.6%和 74.1%),化合物的保护和失活活性的 EC 值分别为 252.8 和 113.5mg/L,优于宁南霉素(284.8 和 144.7mg/L)和香豆素硫冰(624.9 和 300.0mg/L)。此外,化合物的抗 TSWV 活性与防御相关酶活性、增强光合作用和减轻应激反应有关,从而提高了抗病性。

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