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  • Title: Design, synthesis and insecticidal activity of benzenesulfonamide derivatives containing various alkynyl, alkenyl and cyclopropyl groups in para position.
    Author: Zhu JJ, Guo T, Liu HX, Tan XR, Zhang ZW, Wu WJ, Zhang JW.
    Journal: Nat Prod Res; 2024; 38(3):549-553. PubMed ID: 36200705.
    Abstract:
    Celangulin V is a natural β-dihydrofuran sesquiterpene polyester with anti Mythimna separate activity and unique mechanism of action. Further study showed that its target was the H subunit of V-ATPase in the midgut of M. separate. 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 M. separate, 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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