华南农业大学学报2018，Vol.39Issue(2)：75-81,7.DOI:10.7671/j.issn.1001-411X.2018.02.012
新型芳基吡唑脲类化合物的合成及活性评价
Synthesis and bioactivity evaluation of novel urea derivatives of arylpyrazoles
摘要
Abstract
[Objective]To explore new active compounds targeting the central nervous system of insects via structural modification of fipronil, and provide practical experience and theoretical guidance for development of new insecticides.[Method]Using fipronil as the primary material, six new urea derivatives of arylpyrazoles (2a–2f) were synthesized through two step reactions according to intermediate derivatization strategy. The structures were identified by MS,1H NMR and13C NMR. The bioactivities of the target compounds on third instar larvae of Plutella xylostella were evaluated by the leaf immersion method. The toxic effects of these target compounds on central olfactory neurons in P. xylostella were detected by patch clamp technique.[Result]The preliminary bioassay showed that compound 2a had the most toxicity with 6.17 μg·mL–1 LC50 after 12 hours. Electrophysiological data showed that compounds 2b, 2d, 2e and 2f acted on the neurons in a different manner compared to the parent compounds. The membrane potential of the neurons displayed a transient depolarization, and gradually hyperpolarized accompanying with the inhibition of self-generation activities.[Conclusion]Introducing urea structure to bioactive molecules is a potential strategy to change the way pesticides act on the central nervous system of insects, and provides a guidance for the development of new pesticides.关键词
芳基吡唑/脲类衍生物/生物活性/中枢嗅觉神经元/杀虫剂/浸叶法/膜片钳技术Key words
arylpyrazoles/urea derivative/bioactivity/central-olfactory neurons/insecticide/leaf immersion method/patch clamp technique分类
农业科技引用本文复制引用
盛情情,赵晨,燕颍,徐汉虹..新型芳基吡唑脲类化合物的合成及活性评价[J].华南农业大学学报,2018,39(2):75-81,7.基金项目
广东省自然科学基金(2017A030310490,2014A030311044) （2017A030310490,2014A030311044）
广州市科技计划项目(201510010299) （201510010299）
