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Design, Synthesis, Insecticidal Activities and Molecular Docking of Sulfonamide Derivatives Containing Propargyloxy
Jian-Jun Zhu1, Tao Guo1, Zi-Wei Zhang1
1College of Chemistry & Pharmacy, Northwest A&F University, Xian Yang Shi, Yangling, 712100, China.
Researchers synthesized novel sulfonamide derivatives to discover effective pesticides targeting the Mythimna separate insect. Several compounds demonstrated superior insecticidal activity compared to Celangulin V, offering promising leads for new insecticide development.
Area of Science:
- Agricultural Chemistry
- Organic Chemistry
- Insecticide Development
Background:
- Natural products are a key source for discovering new, highly active pesticide molecules.
- Celangulin V shows significant insecticidal activity against Mythimna separate by targeting the V-ATPase H subunit.
Purpose of the Study:
- To synthesize and evaluate novel sulfonamide derivatives as potential insecticides.
- To identify cost-effective and highly efficient compounds targeting the V-ATPase H subunit of Mythimna separate.
Main Methods:
- Systematic synthesis of thirty-seven sulfonamide derivatives with propargyloxy or pyridine groups.
- Bioactivity assays were conducted on third-instar larvae of Mythimna separate.
- Molecular docking experiments were performed to predict the binding mechanism.
Main Results:
- Compounds A2-A4 and A6-A7 displayed enhanced insecticidal activity against M. separate larvae.
- The LC50 values for these compounds ranged from 2.48 to 3.54 mg/mL, outperforming Celangulin V (LC50 = 18.1 mg/mL).
- Molecular docking suggested these derivatives interact with the V-ATPase H subunit.
Conclusions:
- The synthesized sulfonamide derivatives show significant potential as novel insecticides.
- These compounds offer a promising foundation for developing new pest control agents targeting the V-ATPase H subunit.
- Further research into these derivatives could lead to more efficient and selective insecticides.
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