Mesoionic pyrido[1,2- a ]pyrimidinones: Discovery of dicloromezotiaz as a lepidoptera insecticide acting on nicotinic acetylcholine receptors 1,2
| Autor: | Thomas F. Pahutski, Caleb William Holyoke, Twyla A. Briddell, Ming Xu, James D. Barry, Daniel Cordova, My-Hanh Thi Tong, Stephen Frederick Mccann, Yewande T. Henry, Wenming Zhang, Kenneth A. Hughes, Robert M. Leighty, Chen Yuzhong, George Philip Lahm |
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| Rok vydání: | 2017 |
| Předmět: |
010405 organic chemistry
Chemistry Stereochemistry Organic Chemistry Clinical Biochemistry Mesoionic Pharmaceutical Science Biological activity 010402 general chemistry 01 natural sciences Biochemistry 0104 chemical sciences Lepidoptera genitalia chemistry.chemical_compound Nicotinic agonist Pyrimidinones Drug Discovery medicine Molecular Medicine Molecular Biology Acetylcholine medicine.drug |
| Zdroj: | Bioorganic & Medicinal Chemistry Letters. 27:911-917 |
| ISSN: | 0960-894X |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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