A novel class of mesoionic pyrido[1,2-a]pyrimidinones has been discovered with exceptional insecticidal activity controlling a number of insect species, particularly hemiptera and lepidoptera. Mode-of-action studies showed that they act on nicotinic acetylcholine receptors (nAChRs) primarily as inhibitors. Here we report the discovery, evolution, and preparation of this class of chemistry. Our efforts
已发现一类新型的中离子
吡啶并[1,2-a]
嘧啶酮类,具有优异的杀虫活性,可控制许多昆虫,特别是半翅目和鳞翅目。作用模式研究表明,它们主要作为
抑制剂作用于
烟碱乙酰胆碱受体(nAChRs)。在这里,我们报告这类
化学的发现,演化和制备。还介绍了我们在结构-活性关系阐明和
生物活性评估方面所做的努力。