Mesoionic pyrido[1, 2-a]pyrimidinones: Discovery of triflumezopyrim as a potent hopper insecticide1. Issue 1 (1st January 2017)

• Record Type: Journal Article
• Authors: Zhang, Wenming; Holyoke, Caleb W.; Pahutski, Thomas F.; Lahm, George P.; Barry, James D.; Cordova, Daniel; Leighty, Robert M.; Singh, Vineet; Vicent, Daniel R.; Tong, My-Hanh T.; Hughes, Kenneth A.; McCann, Stephen F.; Henry, Yewande T.; Xu, Ming; Briddell, Twyla A.
• Is Part Of: Bioorganic & medicinal chemistry letters. Volume 27:Issue 1(2017)
• Page Start: 16
• Page End: 20
• Publication Date: 2017-01-01
• Subjects: Mesoionic -- Pyrido[1, 2-a]pyrimidinone -- Insecticide -- Triflumezopyrim -- Acetylcholine receptor -- Inhibitor; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1016/j.bmcl.2016.11.042
• Languages: English
• ISSNs: 0960-894X

Abstract

Graphical abstract: Abstract: 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 which led to the discovery of triflumezopyrim as a highly potent insecticide controlling various hopper species. Our efforts in discovery, synthesis, structure-activity relationship elucidation, and biological activity evaluation are also presented.