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. 2017 Jan 1;27(1):16-20.
doi: 10.1016/j.bmcl.2016.11.042. Epub 2016 Nov 16.

Mesoionic pyrido[1,2-a]pyrimidinones: Discovery of triflumezopyrim as a potent hopper insecticide1

Wenming Zhang  1 , Caleb W Holyoke Jr  2 , Thomas F Pahutski  2 , George P Lahm  2 , James D Barry  2 , Daniel Cordova  2 , Robert M Leighty  2 , Vineet Singh  3 , Daniel R Vicent  2 , My-Hanh T Tong  2 , Kenneth A Hughes  2 , Stephen F McCann  2 , Yewande T Henry  2 , Ming Xu  2 , Twyla A Briddell  2
Affiliations

Mesoionic pyrido[1,2-a]pyrimidinones: Discovery of triflumezopyrim as a potent hopper insecticide1

Wenming Zhang et al. Bioorg Med Chem Lett. .

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.

Keywords: Acetylcholine receptor; Inhibitor; Insecticide; Mesoionic; Pyrido[1,2-a]pyrimidinone; Triflumezopyrim.

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