Mesoionic pyrido[1,2- a ]pyrimidinones: A novel class of insecticides inhibiting nicotinic acetylcholine receptors
作者:Wenming Zhang、Caleb W. Holyoke、James Barry、Robert M. Leighty、Daniel Cordova、Daniel R. Vincent、Kenneth A. Hughes、My-Hanh T. Tong、Stephen F. McCann、Ming Xu、Twyla A. Briddell、Thomas F. Pahutski、George P. Lahm
DOI:10.1016/j.bmcl.2016.10.031
日期:2016.11
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。