中氮茚吡啶并[1,2-a]嘧啶酮：作为一种作用于烟碱型乙酰胆碱受体的鳞翅目杀虫剂的二氯美唑噻的发现。
Mesoionic pyrido[1,2-a]pyrimidinones: Discovery of dicloromezotiaz as a lepidoptera insecticide acting on nicotinic acetylcholine receptors.
作者信息
Zhang Wenming, Holyoke Caleb W, Barry James, Cordova Daniel, Leighty Robert M, Tong My-Hanh T, Hughes Kenneth A, Lahm George P, Pahutski Thomas F, Xu Ming, Briddell Twyla A, McCann Stephen F, Henry Yewande T, Chen Yuzhong
机构信息
DuPont Crop Protection, Stine-Haskell Research Center, 1094 Elkton Road, Newark, DE 19711, USA.
DuPont Crop Protection, Stine-Haskell Research Center, 1094 Elkton Road, Newark, DE 19711, USA.
出版信息
Bioorg Med Chem Lett. 2017 Feb 15;27(4):911-917. doi: 10.1016/j.bmcl.2017.01.002. Epub 2017 Jan 5.
A novel class of mesoionic pyrido[1,2-a]pyrimidinones has been discovered with exceptional insecticidal activity controlling a number of insect species. In this communication, we report the part of the optimization program that led to the identification of dicloromezotiaz as a potent insecticide to control a broad range of lepidoptera. Our efforts in discovery, synthesis, 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。在本通讯中，我们报告了优化计划的一部分，该计划导致鉴定出二氯美唑噻作为一种有效的杀虫剂，可控制多种鳞翅目昆虫。我们还介绍了在发现、合成、构效关系阐明和生物活性评估方面所做的工作。
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