含环丙甲酸类活性片段的新型二酰胺衍生物的设计、合成及生物活性  

Design,synthesis and biological activities of novel diamide derivatives containing bioactive cyclopropanecarboxylic acid fragments

作　　者：陈睿嘉 冯婷婷 王港澳 徐晓勇[1] 李忠[1] CHEN Ruijia;FENG Tingting;WANG Gang'ao;XU Xiaoyong;LI Zhong(Shanghai Key Laboratory of Chemical Biology,School of Pharmacy,East China University of Science and Technology,Shanghai 200237,China)

机构地区：[1]华东理工大学药学院,上海市化学生物学(芳香杂环)重点实验室,上海200237

出　　处：《农药学学报》2022年第2期248-259,共12页Chinese Journal of Pesticide Science

基　　金：国家重点研发计划(2017YFD0200505)。

摘　　要：为探索具有新颖结构的杀虫剂先导,将多种含环丙甲酸的活性片段引入二酰胺类杀虫剂,设计并合成了21个新型的二酰胺类衍生物,其结构均经过核磁共振波谱(NMR)及高分辨质谱(HRMS)表征。测试了所有目标衍生物对苜蓿蚜Aphis craccivora、东方黏虫Mythimna separate、小麦赤霉病菌Fusarium graminearum及小麦白粉病菌Blumeria graminis的生物活性。结果显示:大部分邻位二酰胺类衍生物的对两种供试病原菌的杀菌活性不够理想,而对两种害虫靶标均有良好的杀虫活性。在500 mg/L质量浓度下,衍生物10h对苜蓿蚜的致死率为90%,10k对东方黏虫的致死率达100%,这两个衍生物均可作为潜在的杀虫先导衍生物加以进一步研究。In order to discover insecticide leads with novel structures,a variety of cyclopropanecarboxylic acid-containing active fragments were introduced into diamide insecticides.21 novel diamide derivatives were designed and synthesized.Their structures were characterized by nuclear magnetic resonance spectroscopy(NMR)and high resolution mass spectrometry(HRMS).And their biological activities against Aphis craccivora,Mythimna separate,Fusarium graminearum and Blumeria graminis were evaluated.The results suggestted that most of our anthranilic diamides had low fungicidal activities on the two fungi and good insecticidal activities against the two insect targets.And at the concentration of 500 mg/L,10h exhibited a mortality rate of 90%against A.craccivora,while 10k possessed a rate of 100%against M.separate.Both two derivatives could be further optimized as potential insecticide leads.

关 键 词：环丙甲酸 活性片段 二酰胺 杀虫活性 

分 类 号：O624.5[理学—有机化学] O623.626[理学—化学]