双酰胺类杀虫剂作用机制及其先导优化研究进展

Research progress on action mechanism and lead optimization of diamide insecticides

双酰胺类超高效杀虫剂的作用靶标新颖,对农业和卫生害虫高效广谱,是解决农药残留危害和害虫抗性问题及保障农业生产发展的重要化合物。综合2008年以来大部分关于双酰胺类杀虫剂合成的文献,详细介绍了双酰胺类杀虫活性物质的分类、优缺点、靶标鱼尼丁受体的晶体结构、作用机制及开发历程,分析了双酰胺类先导优化与合成研究中的构效关系,指出了药剂物理行为对其与靶标互作的影响,阐明了溴虫氟苯双酰胺等新型杀虫剂和鱼尼丁受体靶标对害虫抗性综合治理、新型杀虫剂创制及环境保护的意义,预测了未来双酰胺杀虫剂的研究方向。

Owing to the new targets,efficiency,and broad spectrum,diamide insecticides are regarded as crucial chemicals to resolve residue hazard,reduce pest resistance,as well as promote agriculture production.In this article,most of the literature on synthesis of diamides published since 2008 are reviewed.The detail characters of diamides(e.g.class,advantages and disadvantages,mechanism,development procedure,crystal structure of ryanodine receptor)are introduced,while SAR(structure-activity relationship)in lead optimization and the influence of diamides’physical behaviors on the interaction between ryanodine receptor(RyR)and insecticides are also analyzed.The RyR targets and new diamide compounds such as broflanilide are of importance in many fields(comprehensive governance of pest resistance,structure design of new insecticides,environment protection,and etc.).Besides,future hotspots of diamide insecticides research are predicted.