Wenming Zhang, Caleb W Holyoke, 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
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.
January 5, 2017: Bioorganic & Medicinal Chemistry Letters