含噻唑和噁唑部分的 Nortopsentin 类似物的优化、构效关系和作用模式。
Optimization, Structure-Activity Relationship, and Mode of Action of Nortopsentin Analogues Containing Thiazole and Oxazole Moieties.
机构信息
Tianjin Key Laboratory of Structure and Performance for Functional Molecules, MOE Key Laboratory of Inorganic-Organic Hybrid Functional Material Chemistry, College of Chemistry , Tianjin Normal University , Tianjin 300387 , China.
State Key Laboratory of Elemento-Organic Chemistry, Research Institute of Elemento-Organic Chemistry, College of Chemistry, Collaborative Innovation Center of Chemical Science and Engineering (Tianjin) , Nankai University , Tianjin 300071 , China.
出版信息
J Agric Food Chem. 2019 Sep 11;67(36):10018-10031. doi: 10.1021/acs.jafc.9b04093. Epub 2019 Sep 3.
Plant diseases seriously endanger plant health, and it is very difficult to control them. A series of nortopsentin analogues were designed, synthesized, and evaluated for their antiviral activities and fungicidal activities. Most of these compounds displayed higher antiviral activities than ribavirin. Compounds , , and , with excellent antiviral activities, emerged as novel antiviral lead compounds, among which was selected for further antiviral mechanism research. The mechanism research results indicated that these compounds may play an antiviral role by aggregating viral particles to prevent their movement in plants. Further fungicidal activity tests revealed that nortopsentin analogues displayed broad-spectrum fungicidal activities. Compounds and displayed higher antifungal activities against than the commercial fungicides carbendazim and chlorothalonil. Current research has laid a foundation for the application of nortopsentin analogues in plant protection.
植物病害严重危害植物健康，防治难度较大。本研究设计、合成了一系列诺托普西汀类似物，并对其抗病毒活性和杀菌活性进行了评价。这些化合物大多数表现出比利巴韦林更高的抗病毒活性。化合物 、 、 和 表现出优异的抗病毒活性，成为新型抗病毒先导化合物，其中 被选为进一步的抗病毒机制研究。机制研究结果表明，这些化合物可能通过聚集病毒颗粒来阻止它们在植物体内移动，从而发挥抗病毒作用。进一步的杀菌活性测试表明，诺托普西汀类似物具有广谱杀菌活性。化合物 和 对 的杀菌活性高于商业杀菌剂多菌灵和百菌清。目前的研究为诺托普西汀类似物在植物保护中的应用奠定了基础。
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