Mesoionic insecticides: a novel class of insecticides that modulate nicotinic acetylcholine receptors

Pest Manag Sci. 2017 Apr;73(4):796-806. doi: 10.1002/ps.4496. Epub 2017 Feb 1.

Abstract

Background: As the world population grows towards 9 billion by 2050, it is projected that food production will need to increase by 60%. A critical part of this growth includes the safe and effective use of insecticides to reduce the estimated 20-49% loss of global crop yields owing to pests. The development of new insecticides will help to sustain this protection and overcome insecticide resistance.

Results: A novel class of mesoionic compounds has been discovered, with exceptional insecticidal activity on a range of Hemiptera and Lepidoptera. These compounds bind to the orthosteric site of the nicotinic acetylcholine receptor and result in a highly potent inhibitory action at the receptor with minimal agonism. The synthesis, biological activity, optimization and mode of action will be discussed.

Conclusion: Triflumezopyrim insect control will provide a powerful tool for control of hopper species in rice throughout Asia. Dicloromezotiaz can provide a useful control tool for lepidopteran pests, with an underexploited mode of action among these pests. © 2016 Society of Chemical Industry.

Keywords: mesoionic insecticide; nAChR; nicotinic acetylcholine receptor.

MeSH terms

  • Animals
  • Aphids / drug effects
  • Aphids / growth & development
  • Hemiptera / drug effects*
  • Hemiptera / growth & development
  • Insect Proteins / metabolism
  • Insecticides / chemical synthesis
  • Insecticides / pharmacology*
  • Moths / drug effects*
  • Moths / growth & development
  • Nicotinic Antagonists / metabolism
  • Periplaneta / drug effects*
  • Periplaneta / growth & development

Substances

  • Insect Proteins
  • Insecticides
  • Nicotinic Antagonists