摘要/Abstract

采用活性单元拼接的方法，以新型吡唑酰胺类杀螨剂吡螨胺为先导结构，在吡唑酰胺分子结构中引入取代噁唑活性单元，设计合成出15个结构新颖的含取代噁唑环的吡唑酰胺类衍生物.目标化合物的结构通过¹H NMR，¹³C NMR和元素分析等进行了表征.初步室内杀虫活性测试结果表明，在500 μg/mL测试浓度下，多数目标化合物对粘虫（Oriental armyworm）有着较高的杀虫活性（致死率≥ 90%）.其中1个目标化合物在500 μg/mL测试浓度下对蚜虫（Aphis medicaginis）的致死率达100%.此外，2个目标化合物在500 μg/mL测试浓度下对朱砂叶螨（Tetranychus cinnabarinus）的致死率都为30%.
关键词: 噁唑, 吡唑酰胺, 合成, 生物活性
In search of new pyrazole amide derivatives with wonderful bioactivities, fifteen novel pyrazole amide compounds were designed and synthesized by introducing substituted oxazole unit into pyrazole amide skeleton based on the lead compound tebufenpyrad. The structures of the title compounds were confirmed by ¹H NMR, ¹³C NMR and elemental analysis. The preliminary bioassay data exhibited that most of target compounds had more than 90% insecticidal activities against Oriental armyworm at the concentration of 500 μg/mL. At the concentration of 500 μg/mL, one compound displayed 100% mortality rate against Aphis medicaginis. In addition, two compounds showed 30% insecticidal activity against Tetranychus cinnabarinus at the concentration of 500 μg/mL.
Key words: oxazole, pyrazole amide, synthesis, biological activity


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