含“-S=N-CN”结构的三氟甲基吡啶酰胺衍生物的合成及杀菌活性

Synthesis and Bactericidal Activity of Trifluoromethyl Pyridinamide Derivatives Containing a Structure of"-S=N-CN"

合成了系列结构新颖的含“—S=N—CN”结构的三氟甲基吡啶酰胺衍生物,采用1H NMR、13C NMR、19F NMR及HRMS对其结构进行了表征。杀菌活性测试结果表明,部分化合物对水稻白叶枯病菌(Xanthomonas oryzae pv.Oryzae)、柑橘溃疡病菌(Xanthomonas axonopodis pv.Citri)和烟草青枯病菌(Ralstonia solanacearum)均具有一定的抑制作用,在质量浓度为200 mg/L时,化合物E1、E2、E4、E10、E11、E13、E14对水稻白叶枯病菌的抑制率均高于80%,化合物E9、E11、E13、E14对柑橘溃疡病菌的抑制作用在50%以上;质量浓度为100 mg/L时,化合物E1、E4、E7、E8、E11、E14、E15对水稻白叶枯病菌的抑制率均高于60%,其中化合物E11为78.7%。研究结果表明该类化合物可作为先导化合物作进一步优化。

A series of novel trifluoromethyl pyridinamide derivatives with-S=N-CN structure were designed and synthesized.Their chemical structures were confirmed by 1H NMR,13C NMR,19F NMR and HR-MS.The results of investigation for bactericidal activity indicated that some of the compounds showed a certain inhibitory effect against Xanthomonas oryzae pv.Oryzae(Xoo),Xanthomonas axonopodis pv.Citri(Xac)and Ralstonia solanacearum(Rs).Such as the activities of compounds E1,E2,E4,E10,E11,E13 and E14 on Xoo were over 80%at 200 mg/L,and compounds E9,E11,E13 and E14 showed over 50%activity against Xac.The activities of compounds E1,E4,E7,E8,E11,E14 and E15 on Xoo was higher than 60%at 100 mg/L,particularly,compound E11 showed 78.7%against Xoo.The results indicated some of the compounds could be used as the leading compounds for further study.