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中文摘要：
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。
英文摘要：
1,2,3-thiadiazoles possess versatile biological activity.In order to conduct lead derivation and find more active new structures,18 novel 4-methyl-1,2,3-thiadiazoles containing active substructure of 3-fluoro-4-methylphenyl were rationally designed and synthesized via Ugi reaction.All new compounds synthesized were confirmed by 1H NMR,IR and HRMS.Bioassay including fungicidal activity,antivirus activity in vitro and in vivo and systemic acquired resistance of the target compounds indicated that these newly ...
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