Zhang Renfeng, Deng Peng, Dai Ali, Guo Shengxin, Wang Ya, Wei Panpan, Wu Jian
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.
ACS Omega. 2021 Oct 8;6(41):27561-27567. doi: 10.1021/acsomega.1c04644. eCollection 2021 Oct 19.
A total of 34 novel ferulic amide Ac5c derivatives were designed and synthesized and their antipest activities were investigated. The results showed that some compounds exhibited excellent antibacterial activity against pv. () and pv. (), such as compounds and demonstrated excellent activity against , with EC values of 4.0, and 1.9 μg/mL, respectively. Compounds , , , , , and had significant activities against , with EC values of 12.5, 13.9, 9.8 15.0, 9.2, and 19.8 μg/mL, respectively. Moreover, the antibacterial activity against rice bacterial leaf blight was also evaluated. Scanning electron microscopy (SEM) showed that compound significantly reduced the cell membrane of , and resulted in cell surface wilting, deformation, breakage, and increased porous attributes. In addition, some of the target compounds also showed moderate biological activity against fungi and acted as potential insecticides.
共设计合成了34种新型阿魏酸酰胺Ac5c衍生物，并对其抗虫活性进行了研究。结果表明，部分化合物对丁香假单胞菌番茄致病变种（Pseudomonas syringae pv. tomato）和丁香假单胞菌辣椒致病变种（Pseudomonas syringae pv. maculicola）表现出优异的抗菌活性，如化合物1和2对丁香假单胞菌番茄致病变种表现出优异的活性，其EC50值分别为4.0和1.9 μg/mL。化合物3、4、5、6、7和8对丁香假单胞菌辣椒致病变种具有显著活性，其EC50值分别为12.5、13.9、9.8、15.0、9.2和19.8 μg/mL。此外，还评估了其对水稻白叶枯病的抗菌活性。扫描电子显微镜（SEM）显示，化合物1显著破坏了水稻白叶枯病菌的细胞膜，导致细胞表面萎蔫、变形、破裂，并增加了多孔性。此外，部分目标化合物对真菌也表现出中等生物活性，并具有潜在的杀虫活性。
