Design, synthesis and insecticidal activities of N-(4-cyano-1-phenyl-1H-pyrazol-5-yl)-1,3-diphenyl-1H-pyrazole-4-carboxamide derivativesElectronic supplementary information (ESI) available. See DOI: 10.1039/c5ra09286h

Insect ryanodine receptor is one of the promising targets for the development of novel insecticides. In order to search for potent insecticides targeting the ryanodine receptor (RyR), a series of novel diphenyl-1 H -pyrazole derivatives with cyano substituent were designed and synthesized. Their ins...

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Hauptverfasser: Lv, Xian-Hai, Xiao, Jin-Jing, Ren, Zi-Li, Chu, Ming-Jie, Wang, Peng, Meng, Xiang-Feng, Li, Dong-Dong, Cao, Hai-Qun
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Sprache:eng
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Zusammenfassung:Insect ryanodine receptor is one of the promising targets for the development of novel insecticides. In order to search for potent insecticides targeting the ryanodine receptor (RyR), a series of novel diphenyl-1 H -pyrazole derivatives with cyano substituent were designed and synthesized. Their insecticidal activities against diamondback moth ( Plutella xylostella ) indicated that most of the compounds showed moderate to high activities at the four concentrations. Among these compounds, N -(4-cyano-1-(4-fluorophenyl)-1 H -pyrazol-5-yl)-1-(4-fluorophenyl)-3-phenyl-1 H -pyrazole-4-carboxamide ( 5g ) showed 84% larvicidal activity against Plutella xylostella at the concentration of 0.1 mg L −1 . Molecular docking showed the predicted binding mode between 5g and protein receptor, which could suggest that the title compounds were the possible activators of insect RyR. Twenty novel diphenyl-1 H -pyrazole derivatives with cyano substituent were designed and synthesized, and their insecticidal activities were evaluated.
ISSN:2046-2069
DOI:10.1039/c5ra09286h