新型含1,3,4-噁二唑基团的吡唑肟衍生物的合成与生物活性  

Synthesis and Bioactivities of Novel Pyrazole Oxime Derivatives Containing 1,3,4-Oxadiazole Group

作　　者：孙洋 王杨 张紫婵 钱烨 骆桂成 周贝贝 缪丽沙 陈雨蝶 戴红[1] 徐宝琳 吴正光 Sun Yang;Wang Yang;Zhang Zichan;Qian Ye;Luo Guicheng;Zhou Beibei;Miao Lisha;Chen Yudie;Dai Hong;Xu Baolin;Wu Zhengguang(College of Chemistry and Chemical Engineering,Nantong University,Nantong,Jiangsu 226019)

机构地区：[1]南通大学化学化工学院,江苏南通226019

出　　处：《有机化学》2023年第4期1584-1590,共7页Chinese Journal of Organic Chemistry

基　　金：国家自然科学基金(No.22177057);江苏省大学生创新训练计划(No.202210304022Z)资助项目。

摘　　要：为了探寻新的吡唑肟活性物质,以唑螨酯为农药先导,依据活性片段拼接原理,合成出了16个新型含1,3,4-噁二唑杂环结构的吡唑肟衍生物,并测定了其杀虫活性.初步活性数据显示,所有目标化合物在500μg/mL的浓度下对粘虫均有100%的防效,其中5种目标化合物在100μg/mL的浓度下对粘虫表现出80%~100%的杀虫效果.同时,在500μg/mL浓度下, 9种目标化合物对蚜虫的致死率都为100%, 3种化合物在100μg/mL时对蚜虫的防效在70%~100%.此外,在500μg/mL的浓度下,有4种目标化合物对朱砂叶螨也呈现出80%以上的杀虫效果.In order to explore new pyrazole oxime compounds possessing satisfactory bioactivities,sixteen pyrazole oxime derivatives containing 1,3,4-oxadiazole group were prepared with fenpyroximate selected as lead structure.Their insecticidal activities were determined.Preliminary bioassay demonstrated that all the target compounds displayed 100%insecticidal activities towards Mythimna separata at 500μg/mL,of which 5 target compounds possessed 80%~100%insecticidal activities against Mythimna separata at 100μg/mL.Moreover,at concentration of 500μg/mL,mortality rates against Aphis medicaginis of 9 target compounds were 100%,those of 3 compounds were 70%~100%at 100μg/mL.Additionally,4 target compounds exhibited more than 80%mortality rates against Tetranychus cinnabarinus at 500μg/mL.

关 键 词：1 3 4-噁二唑 吡唑肟 合成 生物活性 

分 类 号：TQ453[化学工程—农药化工] O626[理学—有机化学]