Combinatorial Synthesis of A Series of Paeonol-based Phenylsulfonyl hydrazone Derivatives as Insecticidal Agents.
Paeonol
biorational pesticides
combinatorial synthesis
insecticidal activity
insecticides
phenylsulfonylhydrazone.
Journal
Combinatorial chemistry & high throughput screening
ISSN: 1875-5402
Titre abrégé: Comb Chem High Throughput Screen
Pays: United Arab Emirates
ID NLM: 9810948
Informations de publication
Date de publication:
2020
2020
Historique:
received:
18
10
2019
revised:
19
12
2019
accepted:
10
01
2020
pubmed:
28
1
2020
medline:
2
4
2021
entrez:
28
1
2020
Statut:
ppublish
Résumé
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. 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. 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%). 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.
Sections du résumé
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.
Identifiants
pubmed: 31985371
pii: CCHTS-EPUB-103925
doi: 10.2174/1386207323666200127121129
doi:
Substances chimiques
Acetophenones
0
Hydrazones
0
Insecticides
0
Sulfhydryl Compounds
0
paeonol
3R834EPI82
Types de publication
Journal Article
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM
Pagination
232-238Informations de copyright
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