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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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. |
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ISSN: | 2046-2069 |
DOI: | 10.1039/c5ra09286h |