Mesoionic pyrido[1,2-a]pyrimidinones: A novel class of insecticides inhibiting nicotinic acetylcholine receptors
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- 作者：Wenming Zhang ; wenming.zhang@dupont.com" class="auth_mail" title="E-mail the corresponding author ; Caleb W. Holyoke Jr. ; 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
- 关键词：Mesoionic ; Pyrido[1 ; 2-a]pyrimidinone ; Insecticide ; Acetylcholine receptor ; Inhibitor
- 刊名：Bioorganic & Medicinal Chemistry Letters
- 出版年：2016
- 出版时间：15 November 2016
- 年：2016
- 卷：26
- 期：22
- 页码：5444-5449
- 全文大小：974 K
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, 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.