中离子型吡啶并[1,2-a]嘧啶酮类：一类新型的抑制烟碱型乙酰胆碱受体的杀虫剂。
Mesoionic pyrido[1,2-a]pyrimidinones: A novel class of insecticides inhibiting nicotinic acetylcholine receptors.
作者信息
Zhang Wenming, Holyoke Caleb W, Barry James, Leighty Robert M, Cordova Daniel, Vincent Daniel R, Hughes Kenneth A, Tong My-Hanh T, McCann Stephen F, Xu Ming, Briddell Twyla A, Pahutski Thomas F, Lahm George P
机构信息
DuPont Crop Protection, Stine-Haskell Research Center, 1090 Elkton Road, Newark, DE 19711, USA.
DuPont Crop Protection, Stine-Haskell Research Center, 1090 Elkton Road, Newark, DE 19711, USA.
出版信息
Bioorg Med Chem Lett. 2016 Nov 15;26(22):5444-5449. doi: 10.1016/j.bmcl.2016.10.031. Epub 2016 Oct 13.
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 in structure-activity relationship elucidation and biological activity evaluation are also presented.
已发现一类新型的中氮茚并[1,2-a]嘧啶酮，具有卓越的杀虫活性，可控制多种昆虫物种，尤其是半翅目和鳞翅目昆虫。作用机制研究表明，它们主要作为抑制剂作用于烟碱型乙酰胆碱受体（nAChRs）。在此，我们报告此类化学物质的发现、演变及制备过程。同时还介绍了我们在构效关系阐明和生物活性评估方面所做的工作。
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