Lei Chao, Geng Li, Xu Xiaoyong, Shao Xusheng, Li Zhong
Shanghai Key Laboratory of Chemical Biology, School of Pharmacy, East China University of Science and Technology, Shanghai 200237, China.
Shanghai Key Laboratory of Chemical Biology, School of Pharmacy, East China University of Science and Technology, Shanghai 200237, China; Shanghai Collaborative Innovation Center for Biomanufacturing Technology, 130 Meilong Road, Shanghai 200237, China.
Bioorg Med Chem Lett. 2018 Feb 15;28(4):831-833. doi: 10.1016/j.bmcl.2017.06.046. Epub 2017 Jun 20.
A series of novel isoxazole-containing neonicotinoids were synthesized from nitromethylene analogues and aromatic aldehydes in the presence of l-proline/KCO. Bioassays indicated that several synthesized compounds showed 40-70% mortality against brown planthopper (Nilaparvata lugens) under the concentration of 4mgL, higher than that of imidacloprid (20%). Against cowpea aphid (Aphis craccivora), the best activity of title compounds reached 90% at the concentration of 20mgL.
在L-脯氨酸/碳酸钾存在的条件下，由硝基亚甲基类似物和芳香醛合成了一系列含异恶唑的新型烟碱类化合物。生物测定表明，几种合成化合物在4mg/L的浓度下对褐飞虱（Nilaparvata lugens）的死亡率为40%-70%，高于吡虫啉（20%）。对于豇豆蚜（Aphis craccivora），目标化合物在20mg/L的浓度下最佳活性达到90%。
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