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.