新型 5(3,5)-(二)卤代胞苷/烟碱的 N-酰基/磺酰基衍生物的半合成及其对斜纹夜蛾、朱砂叶螨和麦长管蚜的生物活性。
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.
机构信息
Research Institute of Pesticidal Design & Synthesis, College of Plant Protection, Northwest A & F University, Yangling, People's Republic of China.
College of Chemistry and Pharmacy, Northwest A & F University, Yangling, People's Republic of China.
出版信息
Pest Manag Sci. 2019 Oct;75(10):2598-2609. doi: 10.1002/ps.5375. Epub 2019 Apr 22.
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.
背景
为了发现用于作物保护的新型天然产物农药，通过对烟碱/苦参碱进行结构修饰，合成了一系列 N-酰基/磺酰基衍生物。对 3 种典型的农业害虫（粘虫、朱砂叶螨和麦长管蚜）进行了杀虫活性评价。
结果
化合物 5f 对 3 种测试害虫表现出良好的杀虫活性。所有 N-苯磺酰基烟碱衍生物均表现出较强的杀螨活性。化合物 5j 的杀螨活性比烟碱高 2.5 倍，且具有良好的防治效果。中间体 2 和 3/3' 对蚜虫具有显著的杀虫活性。还获得了一些有趣的构效关系结果。
结论
这些结果表明，化合物 5f 和 5j 可进一步作为农药进行修饰。 © 2019 英国化学学会。
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