Guo S X, He F, Dai A L, Zhang R F, Chen S H, Wu J
State Key Laboratory Breeding Base of Green Pesticide and Agricultural Bioengineering, Key Laboratory of Green Pesticide and Agricultural Bioengineering, Ministry of Education, Research and Development Center for Fine Chemicals, Guizhou University Huaxi District Guiyang 550025 P. R. China
RSC Adv. 2020 Sep 28;10(59):35658-35670. doi: 10.1039/d0ra07301f.
A series of trifluoromethylpyridine amide derivatives containing sulfur moieties (thioether, sulfone and sulfoxide) was designed and synthesized. Their antibacterial activities against pv. (), () and insecticidal activities against were evaluated. Notably, the half-maximal effective concentration (EC) value of sulfone-containing compound F10 is 83 mg L against , which is better than that of commercial thiodiazole copper (97 mg L) and bismerthiazol (112 mg L). Thioether-containing compounds E1, E3, E5, E6, E10, E11 and E13 showed much higher activities against with the EC value from 40 to 78 mg L, which are much lower than that of thiodiazole copper (87 mg L) and bismerthiazol (124 mg L). Generally, most of the sulfone-containing compounds and sulfoxide-containing compounds showed higher activities against than that of the corresponding thioether-containing compound, but most of the thioether-containing compounds contributed higher antibacterial activities against . Furthermore, title compounds E3, E11, E24 and G2 showed good insecticidal activities of 75%, 70%, 70% and 75%, respectively.
设计并合成了一系列含硫部分（硫醚、砜和亚砜）的三氟甲基吡啶酰胺衍生物。评估了它们对（）、（）的抗菌活性以及对的杀虫活性。值得注意的是，含砜化合物F10对的半数有效浓度（EC）值为83 mg/L，优于市售的噻菌铜（97 mg/L）和噻霉酮（112 mg/L）。含硫醚的化合物E1、E3、E5、E6、E10、E11和E13对显示出更高的活性，EC值为40至78 mg/L，远低于噻菌铜（87 mg/L）和噻霉酮（124 mg/L）。一般来说，大多数含砜化合物和含亚砜化合物对的活性高于相应的含硫醚化合物，但大多数含硫醚化合物对具有更高的抗菌活性。此外，标题化合物E3、E11、E24和G2分别显示出75%、70%、70%和75%的良好杀虫活性。
