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Mesoionic pyrido[1,2-a]pyrimidinones: A novel class of insecticides inhibiting nicotinic acetylcholine receptors.

Abstract：

: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.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Zhang W,Holyoke CW Jr,Barry J,Leighty RM,Cordova D,Vincent DR,Hughes KA,Tong MT,McCann SF,Xu M,Briddell TA,Pahutski TF,Lahm GP

doi

10.1016/j.bmcl.2016.10.031

subject

Has Abstract

pub_date

2016-11-15 00:00:00

pages

5444-5449

issue

22

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(16)31059-9

journal_volume

26

pub_type

杂志文章

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