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1Synthesis and Bioactivities Evaluation of Novel Anthranilic Diamides Containing N-(tert-Butyl)benzohydrazide Moiety as Potent Ryanodine Receptor Activator显示文摘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.Yunyun Zhou Wei Wei Liangliang Zhu Yuxin Li 2019Chinese Journal of Chemistry2019,37,6:1
2Design, Synthesis, and Evaluation of Fungicidal Activity of Novel Pyrazole-Containing Strobilurin Derivatives显示文摘In searching for novel fungicidal leads,a series of pyrazole-containing strobilurins were rationally designed,synthesized and charac-terized.Bioassay indicated that compound 1-7 displayed excellent fungicidal activity against a broad spectrum of plant pathogens such as Gibberella zeae,Rhizoctonia cereolis,Sclerotinia sclerotiorum,Phytophthora infestans,Physolosporo piricola and Pellicularia sosakii with EC_(50) of 0.16,0.02,0.72,0.07,0.77 and 0.65μg/mL,respectively,which were 3-10 times more potent than the positive control azoxystrobin against the corresponding pathogens.Moreover,like azoxystrobin and kresoxim methyl,1-7,displayed excellent protec-tive activity against P.sorghi.Molecular docking validated that 1-7 and azoxystrobin would share a similar binding mode with cytochrome bc_(1) complex.This study demonstrates that 1-7 is a promising fungicidal candidate for further development.Zesheng Hao Weibo Wang Bin Yu Xin Qi You Lv Xiaoyu Liu Haoyin Chen Tatiana A.Kalinina Tatiana V.Glukhareva Zhijin Fan 2021Chinese Journal of Chemistry2021,39,6:1
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