Design, Synthesis, Insecticidal Activities and Molecular Docking of Sulfonamide Derivatives Containing Propargyloxy or Pyridine Groups

The discovery of new highly active molecules from natural products is a common method to create new pesticides. Celangulin V targeting Mythimna separate (M. separate) midgut V‐ATPase  H subunit, has received considerable attention for its excellent insecticidal activity and unique mechanism of actio...

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Veröffentlicht in:Chemistry & biodiversity 2023-02, Vol.20 (2), p.e202201020-n/a
Hauptverfasser: Zhu, Jian‐Jun, Guo, Tao, Zhang, Zi‐Wei, Qian, Hao, Tian, Peng, Yu, Ke‐Yin, Wu, Wen‐Jun, Zhang, Ji‐Wen
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Sprache:eng
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Zusammenfassung:The discovery of new highly active molecules from natural products is a common method to create new pesticides. Celangulin V targeting Mythimna separate (M. separate) midgut V‐ATPase  H subunit, has received considerable attention for its excellent insecticidal activity and unique mechanism of action. Therefore, combined with our preliminary work, thirty‐seven sulfonamide derivatives bearing propargyloxy or pyridine groups were systematically synthesized to search for insecticidal candidate compounds with low cost and high efficiency on the  H subunit of V‐ATPase. Bioactive results showed that compounds A2‐A4 and A6‐A7 exhibited a better bioactivity with median effective concentration (LC50) values (2.78, 3.11, 3.34, 3.54 and 2.48 mg/mL, respectively) against third‐instar larvae of M. separate than Celangulin V (LC50=18.1 mg/mL). Additionally, molecular docking experiments indicated that these molecules may act on the H subunit of V‐ATPase. Based on the above results, these compounds provide new ideas for the discovery of insecticides.
ISSN:1612-1872
1612-1880
DOI:10.1002/cbdv.202201020