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四种新烟碱类杀虫剂对蜜蜂的急性毒性及初级风险评估
引用本文:谭都, 须志平, 邵旭升, 李忠. N-苯基八元氧桥环新烟碱化合物的合成及其增效活性[J]. 农药学学报, 2024, 26(1): 44-51. DOI: 10.16801/j.issn.1008-7303.2023.0095
作者姓名:谭都  须志平  邵旭升  李忠
作者单位:1.华东理工大学 药学院,上海市化学生物学 (芳香杂环) 重点实验室,上海 200237
基金项目:国家重点研究计划项目 (2017YFD0200500).
摘    要:

杀虫剂增效剂是提高杀虫剂杀虫效果和降低抗药性的关键成分。本文对具有特异性增效活性的八元氧桥环结构进一步衍生,设计合成了15个新型的N-苯基八元氧桥环新烟碱化合物,并测试了目标化合物与吡虫啉联用时对苜蓿蚜Aphis craccivora 的致死率。结果表明:在1 mg/L质量浓度下,大部分目标化合物能使吡虫啉对苜蓿蚜的毒力增加,表现出增效作用,其中苯环上无取代的化合物4a和4-CF3取代的化合物4m增效活性相当,其对吡虫啉毒力的增效倍数分别为3.44和3.58,可作为候选化合物进一步研究。



关 键 词:杀虫剂增效剂  八元氧桥环  新烟碱  吡虫啉  增效活性
收稿时间:2023-09-20

Neonicotinoids-from zero to hero in insecticide chemistry
TAN Du, XU Zhiping, SHAO Xusheng, LI Zhong. Synthesis and synergistic activity of N-phenyl-eight-membered oxabridged neonicotinoid analogues[J]. Chinese Journal of Pesticide Science, 2024, 26(1): 44-51. DOI: 10.16801/j.issn.1008-7303.2023.0095
Authors:TAN Du  XU Zhiping  SHAO Xusheng  LI Zhong
Affiliation:1.Shanghai Key Laboratory of Chemical Biology, School of Pharmacy, East China University of Science and Technology, Shanghai 200237, China
Abstract:Insecticide synergists are key components to improve insecticidal efficacy and reduce resistance. In this work, further derivation of the eight-membered oxabridged structure with specific synergistic effect was conducted, fifteen novel N-phenyl-eight-membered oxabridged neonicotinoid derivatives were designed and synthesized, the mortality of the target compounds combined with imidacloprid against Aphis craccivora was tested. The results indicated that most of the target compounds increased the toxicity of imidacloprid against A. craccivora at the concentration of 1 mg/L. The non-substituted compound 4a and 4-CF3-substituted compound 4m exhibited the comparable synergistic effect, the synergism ratio was 3.44 and 3.58, respectively, which could be regarded as candidate compounds for further study.
Keywords:insecticide synergist  eight-membered oxabridged  neonicotinoid  imidacloprid  synergistic effect
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