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
收稿日期: 2022-12-15
修回日期: 2023-01-31
网络出版日期: 2023-02-07
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
Received date: 2022-12-15
Revised date: 2023-01-31
Online published: 2023-02-07
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.
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 . 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[J]. 有机化学, 2023 , 43(4) : 1584 -1590 . DOI: 10.6023/cjoc202212021
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
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