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

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 g...

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

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.