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以构效关系为线索,根据类同合成法和活性官能团拼接策略,以阿维菌素为先导分子,在其4’’-位引入硫脲或脲活性结构单元,合成了一系列酰基硫脲(9a~9o)和芳基脲(10a~10i)阿维菌素衍生物,所有目标化合物均经~1H NMR、MS和元素分析确证。室内杀虫活性测定结果表明:所有衍生物对朱砂叶螨Tetranychus cinnabarinus和甘蓝蚜Brevicoryne brassicae均表现出不同程度的毒杀活性,大部分化合物对甘蓝蚜的杀虫活性优于阿维菌素B1a,其中化合物9h对朱砂叶螨和甘蓝蚜的LC_(50)值分别为0.100和1.71μmol/L,表现出很高的毒杀活性,化合物9o对甘蓝蚜的毒性最高,LC_(50)值为1.13μmol/L。
Based on the structure-activity relationship, the avermectin was used as the leading molecule and the thiourea or urea reactive structural unit was introduced into the 4 ’’ - position according to the same synthesis method and active functional group splicing strategy. A series of acylthioureas (9a ~ 9o) and arylurea (10a ~ 10i) avermectin derivatives, all the target compounds were confirmed by ~ 1H NMR, MS and elemental analysis. The indoor insecticidal activity assay results showed that all the derivatives showed different degree of toxicity to tetranychus cinnabarinus and cabbage aphid Brevicoryne brassicae, and most of the compounds had better insecticidal activity against aphid B1a, Among them, the LC_ (50) value of compound 9h for Tetranychus cinnabarinus and cabbage aphid were 0.100 and 1.71μmol / L, respectively, showing high toxicity. Compound 9o had the highest toxicity to B. brassicae with LC 50 value of 1.13 μmol / L.