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Design, synthesis and insecticidal activity of benzenesulfonamide derivatives containing various alkynyl, alkenyl and cyclopropyl groups in para position. | LitMetric

AI Article Synopsis

  • Celangulin V, a natural sesquiterpene polyester, has shown anti-insect activity through a unique mechanism targeting the H subunit of V-ATPase in insect midguts.
  • Researchers synthesized thirty-two benzene sulfonamide derivatives to find cost-effective insecticides, with several compounds (C2, C4, C5, C6, and C8) demonstrating significantly higher efficacy than Celangulin V, with lower LC50 values.
  • Molecular docking studies suggest that these new sulfonamide compounds effectively interact with the H subunit of V-ATPase, making them promising candidates for developing efficient insecticidal agents.

Article Abstract

Celangulin V is a natural -dihydrofuran sesquiterpene polyester with anti activity and unique mechanism of action. Further study showed that its target was the H subunit of V-ATPase in the midgut of . Thus, combined with the previous work, thirty-two benzene sulfonamide derivatives were systematically synthesised to discover efficient and low-budget insecticidal candidates for the H subunit of V-ATPase. Screening results showed that compounds C2, C4, C5, C6 and C8 could significantly cause death of tested third-instar larvae of , and provided the corresponding LC50 values of 0.844, 0.953, 0.705, 0.599 and 0.887 mg/mL, which were extremely better than Celangulin V (LC50 = 11.5 mg/mL). The docking results indicated that this novel framework might target H subunit of V-ATPase. Given these excellent bioactivity results, this kind of sulfonamide framework could provide a suitable point for exploring highly efficient insecticidal agents.

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Source
http://dx.doi.org/10.1080/14786419.2022.2130303DOI Listing

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