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Cercosporin-Photocatalyzed [4+1]- and [4+2]-Annulations of Azoalkenes Under Mild Conditions
Published on: July 17, 2020
Combinatorial Synthesis of A Series of Paeonol-based Phenylsulfonyl hydrazone Derivatives as Insecticidal Agents
Zhi-Ping Che1, Jin-Ming Yang1, Di Sun1
1Laboratory of Pesticidal Design & Synthesis, Department of Plant Protection, College of Forestry, Henan University of Science and Technology, Luoyang 471023, Henan Province, China.
Background:
Plant secondary metabolites play an essential role in the discovery of novel insecticide due to their unique sources and potential target sites. Paeonol, the main phenolic components in Moutan Cortex, is recognized as a safe and potent botanical insecticide to many insects. The structural modification of paeonol in this study into phenylsulfonylhydrazone derivatives is proved an effective approach for the development of novel insecticides, those derivatives being more toxic than paeonol. However, there have been no reports on the insecticidal activity of paeonol-based phenylsulfonylhydrazone derivatives in controlling Mythimna separata.
Methods:
We have been working to discover biorational natural products-based insecticides. Twelve novel paeonol-based phenylsulfonylhydrazone derivatives have been successfully prepared by structural modification of paeonol, and the insecticidal activity against M. separata by the leafdipping method at the concentration of 1 mg/mL has been evaluated.
Results:
Insecticidal activity revealed that out of 12 title compounds, derivatives 5c and 5f displayed the best against M. separate with the FMR both of 53.6% than toosendanin (FMR = 50.0%).
Conclusion:
The results suggested that for the paeonol-based phenylsulfonylhydrazone series derivatives, the proper substituent of arylsulfonyl R at the hydroxyl position of paeonol was very important for their insecticidal activity. These preliminary results will pave the way for further modification of paeonol in the development of potential new insecticides.
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