Design, Synthesis, and Insecticidal Activities of Novel Analogues of Neonicotinoids: Replacement of Nitromethylene with Nitroconjugated System
Design, Synthesis, and Insecticidal Activities of Novel Analogues of Neonicotinoids: Replacement of Nitromethylene with Nitroconjugated System
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新型烟碱类杀虫剂类似物的设计、合成和杀虫活性：用硝基共轭体系取代硝基亚甲基
DOI：
10.1021/jf803305f
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发表时间：
2009-02-11
影响因子：
6.1
通讯作者：
Xu, Xiaoyong
中科院分区：
文献类型：
--
作者：
Shao, Xusheng;Li, Zhong;Xu, Xiaoyong
为了用硝基共轭体系取代硝基亚甲基药效团，设计并合成了一系列含五元杂环的类烟碱类似物。生物活性测定结果表明，部分化合物对豇豆蚜、粘虫、黑尾叶蝉和灰飞虱的杀虫活性均高于吡虫啉。令人兴奋的是，衍生物13a和131的活性水平与吡虫啉的活性水平相当。
To replace nitromethylene pharmacophore with a nitroconjugated system, a series of novel neonicotinoid analogues bearing five-membered aromatic heterocycles were designed and synthesized. Bioassays indicated that some of the synthesized compounds exhibited higher insecticidal activities than imidacloprid against cowpea aphids (Aphis craccivora), armyworm (Pseudaletia separate Walker), Nephotettix bipunctatus (Fabricius), and small brown rice planthopper (Laodelphasx striatellus). Exhilaratingly, the activity levels of derivatives 13a and 131 rivaled that of imidacloprid.