为了寻找更多高活性化合物和进行先导结构的衍生,利用Ugi反应设计合成了18个4-甲基-1,2,3-噻二唑新化合物(I-1～I-18),其结构均经核磁共振氢谱、红外光谱和高分辨质谱的表征和确认。杀菌、抗病毒以及诱导活性的筛选结果表明:目标化合物I-3和I-11抗烟草花叶病毒(TMV)的半叶法活性高于对照药剂病毒唑,I-6的保护活性和钝化活性高于病毒唑,I-12的治疗活性高于病毒唑,I-16的诱导活性高于对照药剂噻酰菌胺;氟原子的引入有利于保持和提高新化合物的抗病毒活性,4-甲基-1,2,3-噻二唑和氟原子是新化合物抗病毒的重要活性亚结构单元。Ugi反应是新农药创制中先导优化的绿色手段。 In order to find out more active compounds and to derivatize the leading structure, 18 novel 4-methyl-1,2,3-thiadiazoles (1-1-1-18) were designed and synthesized by Ugi reaction. The structures Characterization and confirmation by 1H NMR, IR and HRMS. The screening results of bactericidal, antiviral and inducible activity showed that the half-leaf activity of the target compounds I-3 and I-11 against tobacco mosaic virus (TMV) was higher than that of the control drug ribavirin and the protective activity and passivation of I-6 The activity of I-12 is higher than that of ribavirin, and the induction activity of I-16 is higher than that of the reference drug thiacetamol. The introduction of fluorine atom helps to maintain and improve the antiviral activity of the new compound. 4- Methyl-1,2,3-thiadiazoles and fluorine atoms are important active antiviral substructural units of new compounds. The Ugi reaction is a green means of leading optimization in the creation of new pesticides.