有机化学 ›› 2023, Vol. 43 ›› Issue (4): 1584-1590.DOI: 10.6023/cjoc202212021 上一篇    下一篇

研究简报

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

孙洋, 王杨, 张紫婵, 钱烨, 骆桂成, 周贝贝, 缪丽沙, 陈雨蝶, 戴红*(), 徐宝琳, 吴正光*()   

  1. 南通大学化学化工学院 江苏南通 226019
  • 收稿日期:2022-12-15 修回日期:2023-01-31 发布日期:2023-02-06
  • 通讯作者: 戴红, 吴正光
  • 作者简介:
    共同第一作者.
  • 基金资助:
    国家自然科学基金(22177057); 江苏省大学生创新训练计划(202210304022Z)

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

Yang Sun, Yang Wang, Zichan Zhang, Ye Qian, Guicheng Luo, Beibei Zhou, Lisha Miao, Yudie Chen, Hong Dai(), Baolin Xu, Zhengguang Wu()   

  1. College of Chemistry and Chemical Engineering, Nantong University, Nantong, Jiangsu 226019
  • Received:2022-12-15 Revised:2023-01-31 Published:2023-02-06
  • Contact: Hong Dai, Zhengguang Wu
  • About author:
    These authors contributed equally to this work.
  • Supported by:
    National Natural Science Foundation of China(22177057); Science and Technology Innovation Foundation for the College Students of Jiangsu Province(202210304022Z)

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500 μg/mL的浓度下对粘虫均有100%的防效, 其中5种目标化合物在100 μg/mL的浓度下对粘虫表现出80%~100%的杀虫效果. 同时, 在500 μg/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100 μg/mL时对蚜虫的防效在70%~100%. 此外, 在500 μg/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.

关键词: 1,3,4-噁二唑, 吡唑肟, 合成, 生物活性

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 500 μg/mL, of which 5 target compounds possessed 80%~100% insecticidal activities against Mythimna separata at 100 μg/mL. Moreover, at concentration of 500 μg/mL, mortality rates against Aphis medicaginis of 9 target compounds were 100%, those of 3 compounds were 70%~100% at 100 μg/mL. Additionally, 4 target compounds exhibited more than 80% mortality rates against Tetranychus cinnabarinus at 500 μg/mL.

Key words: 1,3,4-oxadiazole, pyrazole oxime, synthesis, bioactivity