新型含取代噁二唑结构的吡唑肟类化合物的合成与生物活性研究  

Synthesis and Biological Activities of Novel Pyrazole Oximes Containing Substituted Oxadiazole Moiety

作　　者：戴红[1] 丁颖 杜显超 姚炜[1] 陈庆文 王祥龙[1] 仲苏林[2] 曹雄飞[2] 石玉军[1] Dai Hong;Ding Ying;Du Xianchao;Yao Wei;Chen Qingwen;Wang Xianglong;Zhong Sulin;Cao Xiongfei;Shi Yujun(College of Chemistry and Chemical Engineering,Nantong University,Nantong 226019;United Nations Nantong Pesticide Forulation Development Centre,Nantong 226006)

机构地区：[1]南通大学化学化工学院,南通226019 [2]联合国南通农药剂型开发中心,南通226006

出　　处：《有机化学》2018年第7期1755-1762,共8页Chinese Journal of Organic Chemistry

基　　金：南通市科技计划(No.MS22015020);江苏省大学生创新训练计划(No.201710304048)资助项目~~

摘　　要：为了寻找具有较好生物活性的吡唑肟类衍生物,采用活性基团拼接方法,设计合成了一系列新型含取代噁二唑结构的吡唑肟类化合物.利用~1H NMR、^(13)C NMR和元素分析等手段确证了目标化合物的结构.初步的生物活性测试结果表明,部分目标化合物显示出较好的杀虫活性.当测试浓度降为100μg/m L时,3个化合物对粘虫仍具有较好的杀虫效果,杀死率分别为70%,60%和70%.另外,1个化合物在测试浓度为500μg/m L时对蚜虫也表现出一定的杀虫作用,杀死率为60%.In order to find novel pyrazole oximes with good bioactivities, a series of novel pyrazole oxime derivatives containing substituted oxadiazole moiety were designed and synthesized according to the method of active substructure combination. Their structures were confirmed by ^1H NMR, ^13C NMR and elemental analysis. Preliminary bioassay data indicated that some title compounds showed good insecticidal activities. At the concentration of 500 μg/mL, 9 compounds possessed insecticidal activity against Oriental armyworm with 80%~100%. When the concentration was lowered to 100 μg/mL, 3 compounds still displayed significant insecticidal activity against Oriental armyworm with 70%, 60% and 70%. Additionally, one compound had 60% insecticidal activity against Aphis medicaginis at 500 μg/mL.

关 键 词：噁二唑 吡唑肟 合成 生物活性 

分 类 号：O626[理学—有机化学] TQ453[理学—化学]