Yang Dongyan, Wan Chuan, Xiao Yumei, Che Chuanliang, Rui Changhui, Qin Zhaohai
College of Science, China Agricultural University Beijing 100193 China
Institute of Plant Protection, Chinese Academy of Agricultural Sciences Beijing 100193 China.
RSC Adv. 2018 Jan 8;8(4):1838-1845. doi: 10.1039/c7ra11454k. eCollection 2018 Jan 5.
In searching for new insecticidal lead compounds, a series of novel 1-alkoxy-2-nitroguanidine, guadipyr analogues bearing alkoxy groups were designed, synthesized and confirmed by H NMR, C NMR, high-resolution mass spectrometry and X-ray diffraction. The primary bioassays showed that most of these compounds exhibited moderate to good insecticidal activity against and . Especially, the precise insecticidal assay showed that compounds 4-02, 4-07 and 4-08 displayed excellent activity with IC values lower than 10 μg mL to which is comparable to guadipyr. On the other hand, the toxicity of compound 4-07 and guadipyr against honey bees was much lower than imidacloprid. The results indicated that the flexible chain on the nitrogen atom was the most crucial factor on honey bee toxicity, which existed in both neonicotinoids and guadipyr series.
在寻找新型杀虫先导化合物的过程中，设计、合成了一系列新型的1-烷氧基-2-硝基胍，即带有烷氧基的胍双吡类似物，并通过氢核磁共振（H NMR）、碳核磁共振（C NMR）、高分辨率质谱和X射线衍射对其进行了确证。初步生物测定表明，这些化合物中的大多数对[具体害虫1]和[具体害虫2]表现出中等至良好的杀虫活性。特别是，精确杀虫测定表明，化合物4-02、4-07和4-08表现出优异的[杀虫活性名称]活性，其半数抑制浓度（IC）值低于10μg/mL，与胍双吡相当。另一方面，化合物4-07和胍双吡对蜜蜂的毒性远低于吡虫啉。结果表明，氮原子上的柔性链是对蜜蜂毒性的最关键因素，新烟碱类和胍双吡系列中均存在该因素。
