Mesoionic pyrido[1,2-a]pyrimidinones: Discovery of dicloromezotiaz as a lepidoptera insecticide acting on nicotinic acetylcholine receptors^1,2

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• 作者：Wenming Zhang ; ^{wenming.zhang@dupont.com} ; Caleb W. Holyoke Jr. ; James Barry ; Daniel Cordova ; Robert M. Leighty ; My-Hanh T. Tong ; Kenneth A. Hughes ; George P. Lahm ; Thomas F. Pahutski ; Ming Xu ; Twyla A. Briddell ; Stephen F. McCann ; Yewande T. Henry ; Yuzhong Chen
• 关键词：Mesoionic ; Pyrido[1 ; 2-a]pyrimidinone ; Insecticide ; Dicloromezotiaz ; Acetylcholine receptor ; Inhibitor
• 刊名：Bioorganic & Medicinal Chemistry Letters
• 出版年：2017
• 出版时间：15 February 2017
• 年：2017
• 卷：27
• 期：4
• 页码：911-917
• 全文大小：538 K
• 卷排序：27

文摘

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.