Insects have to shed and replace the cuticle exoskeleton to grow, which biological process is commonly called �molting�. In that process, insects have to synthesize a large amount of chitin to make new cuticle. Since the chitin does not exist in mammal, the inhibitors of chitin synthesis can be safe insecticides. About a half century ago a benzoylphenylurea (BPU) was discovered as the novel compound that inhibits insect chitin synthesis, but the mode of action of BPUs is still unknown. Diflubenzuron (DFB) is the first commercialized BPU containing 2,6-difluorobenzoyl and 4-chlorophenyl moieties. Author's group measured the larvicidal activity of various BPUs against rice stem borers Chilo suppressalisand quantitatively analyzed the substituent effects to make clear the physicochemical properties for the higher activity. Then, I joined Matsumura's group to study the mode of action of DFB. We proposed that DFB inhibits the cuticle formation step that is related to the vesicle movement regulated by ion transport systems.

Structure-activity relationship of insect molting inhibitors

248th National Meeting (2014)

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