有机化学 ›› 2018, Vol. 38 ›› Issue (7): 1755-1762.DOI: 10.6023/cjoc201802015 上一篇    下一篇

研究论文

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

戴红a, 丁颖a, 杜显超a, 姚炜a, 陈庆文a, 王祥龙a, 仲苏林b, 曹雄飞b, 石玉军a   

  1. a 南通大学化学化工学院 南通 226019;
    b 联合国南通农药剂型开发中心 南通 226006
  • 收稿日期:2018-02-08 修回日期:2018-03-01 发布日期:2018-03-29
  • 通讯作者: 石玉军 E-mail:yjshi2015@163.com
  • 基金资助:

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

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

Dai Honga, Ding Yinga, Du Xianchaoa, Yao Weia, Chen Qingwena, Wang Xianglonga, Zhong Sulinb, Cao Xiongfeib, Shi Yujuna   

  1. a College of Chemistry and Chemical Engineering, Nantong University, Nantong 226019;
    b United Nations Nantong Pesticide Forulation Development Centre, Nantong 226006
  • Received:2018-02-08 Revised:2018-03-01 Published:2018-03-29
  • Contact: 10.6023/cjoc201802015 E-mail:yjshi2015@163.com
  • Supported by:

    Project supported by the Science and Technology Project Fund of Nantong City (No. MS22015020) and the Science and Technology Innovation Foundation for the College Students of Jiangsu Province (No. 201710304048).

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、13C 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100 μg/mL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500 μg/mL时对蚜虫也表现出一定的杀虫作用,杀死率为60%.

关键词: 噁二唑, 吡唑肟, 合成, 生物活性

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.

Key words: oxadiazole, pyrazole oxime, synthesis, biological activity