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.
Subject(s)
Hemiptera/drug effects , Insecticides/pharmacology , Moths/drug effects , Periplaneta/drug effects , Animals , Aphids/drug effects , Aphids/growth & development , Hemiptera/growth & development , Insect Proteins/metabolism , Insecticides/chemical synthesis , Moths/growth & development , Nicotinic Antagonists/metabolism , Periplaneta/growth & developmentABSTRACT
A series of quinoline and isoquinoline isoxazolines have been designed as pesticides for crop protection. Herein we reported the chemical synthesis, biological activity and structure-activity relationships. The isoquinoline derivative, such as 3i, is discovered as potent new class of isoxazoline insecticide which is competitive with commercial insecticide Indoxacarb.
Subject(s)
Hemiptera/drug effects , Insecticides/pharmacology , Isoxazoles/pharmacology , Moths/drug effects , Thysanoptera/drug effects , Animals , Dose-Response Relationship, Drug , Insecticides/chemical synthesis , Insecticides/chemistry , Isoquinolines/chemistry , Isoxazoles/chemical synthesis , Isoxazoles/chemistry , Molecular Structure , Quinolines/chemistryABSTRACT
Isoxazoline insecticides have been shown to be potent blockers of insect GABA receptors with excellent activity on a broad pest range, including Lepidoptera and Hemiptera. Herein we report on the synthesis, biological activity and mode-of-action for a class of 4-heterocyclic aryl isoxazoline insecticides.
