Combinatorial Synthesis of A Series of Paeonol-based Phenylsulfonyl hydrazone Derivatives as Insecticidal Agents

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Author(s): Zhi-Ping Che*, Jin-Ming Yang, Di Sun, Yue-E Tian, Sheng-Ming Liu, Xiao-Min Lin, Jia Jiang, Gen-Qiang Chen.

Journal Name: Combinatorial Chemistry & High Throughput Screening
Accelerated Technologies for Biotechnology, Bioassays, Medicinal Chemistry and Natural Products Research

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Background: Plant secondary metabolites play an important role in novel insecticide discovery for 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 into phenylsulfonylhydrazone derivatives is a potential approach for the development of novel insecticides, which showed more toxicity than paeonol. However, there are no reports on the insecticidal activity of paeonol-based phenylsulfonylhydrazone derivatives to control Mythimna separata.

Methods: We always endeavor to discover biorational natural products-based insecticides, 12 novel paeonol-based phenylsulfonylhydrazone derivatives have been successfully perpared by structural modification of paeonol, and evaluated the insecticidal activity against M. separata by the leaf-dipping method at the concentration of 1 mg/mL.

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: It 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.

Keywords: Paeonol, combinatorial synthesis, phenylsulfonylhydrazone, insecticidal activity, biorational pesticides

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(E-pub Ahead of Print)
DOI: 10.2174/1386207323666200127121129
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