Anthranilic diamides have been proven to be a class of efficacious and safe insecticides targeting ryanodine receptors (RyRs) during the last decade. In order to develop innovative scaffolds with high insecticidal act...Anthranilic diamides have been proven to be a class of efficacious and safe insecticides targeting ryanodine receptors (RyRs) during the last decade. In order to develop innovative scaffolds with high insecticidal activity, two series of N-pyridylpyrazole derivatives containing N-(tert-butyl)benzohydrazide substructures were designed and synthesized. Their insecticidal activities against oriental armyworm (Mythimna separata) and diamondback moth (Plutella xylostella) were evaluated. Preliminary bioassay results revealed that some of the new compounds exhibited good insecticidal activity against the oriental armyworm and diamondback moth. The mode of action of these compounds were verified using calcium-imaging technique and the results showed that some new compounds could effectively modulate the insect cytosolic Ca^2+ level, and break the cellular calcium homeostasis, indicating some of these compounds were potent activators of the RyRs.展开更多
基金the NSFC/China (No.21502229)Tianjin Natural Science Foundation (No.16JCYBJC29400).
文摘Anthranilic diamides have been proven to be a class of efficacious and safe insecticides targeting ryanodine receptors (RyRs) during the last decade. In order to develop innovative scaffolds with high insecticidal activity, two series of N-pyridylpyrazole derivatives containing N-(tert-butyl)benzohydrazide substructures were designed and synthesized. Their insecticidal activities against oriental armyworm (Mythimna separata) and diamondback moth (Plutella xylostella) were evaluated. Preliminary bioassay results revealed that some of the new compounds exhibited good insecticidal activity against the oriental armyworm and diamondback moth. The mode of action of these compounds were verified using calcium-imaging technique and the results showed that some new compounds could effectively modulate the insect cytosolic Ca^2+ level, and break the cellular calcium homeostasis, indicating some of these compounds were potent activators of the RyRs.
