College of Agricultural Science and Engineering, Liaocheng University, Liaocheng 252000, P. R. China.
College of Chemical Engineering and Materials Science, Zhejiang University of Technology, Hangzhou 310014, P. R. China.
J Agric Food Chem. 2023 Aug 16;71(32):12333-12345. doi: 10.1021/acs.jafc.3c03937. Epub 2023 Aug 3.
In this project, quinoline and quinolone-containing hydrazide compounds were designed and synthesized by introducing a bioactive hydrazide group into the skeleton of waltherione F. The fungicidal activity revealed that some hydrazide compounds exhibited excellent and broad-spectrum fungicidal activity; especially, compounds , , and showed more than 90% or even 100% inhibition rates against most pathogens at 50 μg·mL. The fungicidal mechanism indicated that compound may affect the normal function of the plasma membrane, further generating changes in the morphology and subcellular structure of mycelia. Simultaneously, may resist the -treated stress through the metabolic pathways related to l-glutamate, l-glutamine, and glutathione. Finally, the effect of compound on wheat seedling's growth and the toxicity to zebrafish were accomplished. These results will provide important guidance to discover novel fungicidal lead compounds and explore new targets, which are effective ways to alleviate the increasingly severe drug resistance.
在本项目中，通过将生物活性的酰腙基团引入到 Waltherione F 的骨架中，设计并合成了含喹啉和喹诺酮的酰腙类化合物。杀菌活性研究表明，一些酰腙类化合物表现出优异和广谱的杀菌活性；特别是化合物 、 、 对大多数病原菌在 50μg·mL 时的抑制率均超过 90%，甚至达到 100%。杀菌机制表明，化合物 可能影响质膜的正常功能，进一步导致菌丝形态和亚细胞结构的变化。同时，化合物 可能通过与 l-谷氨酸、l-谷氨酰胺和谷胱甘肽相关的代谢途径来抵抗 -处理的应激。最后，完成了化合物 对小麦幼苗生长的影响和对斑马鱼的毒性实验。这些结果将为发现新型杀菌先导化合物和探索新靶标提供重要指导，这是缓解日益严重的药物抗性的有效途径。
