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  • Title: Semisynthesis of novel N-acyl/sulfonyl derivatives of 5(3,5)-(di)halogenocytisines/cytisine and their pesticidal activities against Mythimna separata Walker, Tetranychus cinnabarinus Boisduval, and Sitobion avenae Fabricius.
    Author: Huang X, Lv M, Xu H.
    Journal: Pest Manag Sci; 2019 Oct; 75(10):2598-2609. PubMed ID: 30740869.
    Abstract:
    BACKGROUND: To discover novel natural product-based pesticidal agents for crop protection, a series of N-acyl/sulfonyl derivatives of 5(3,5)-(di)halogenocytisines/cytisine were prepared by structural modifications of cytisine. Their pesticidal activities were evaluated against three typically crop-threatening agricultural pests, Mythimna separata Walker, Tetranychus cinnabarinus Boisduval, and Sitobion avenae Fabricius. RESULTS: Compound 5f exhibited the promising pesticidal activities against three tested pests. All N-phenylsulfonylcytisine derivatives showed potent acaricidal activity. Compound 5j exhibited 2.5-fold more potent acaricidal activity than cytisine, and showed good control effects. Intermediates 2, and 3/3' displayed pronounced aphicidal activity. Some interesting results of structure-activity relationships were also obtained. CONCLUSION: These results demonstrate that compounds 5f and 5j could be further modified as pesticidal agents. © 2019 Society of Chemical Industry.
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