| 4"-脱氧阿维菌素脲类及硫脲类衍生物的合成与杀虫活性 |
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| 引用本文： | 张娜,成丕乐,南祥,吴小兵,刘映前,余海涛,张健,杨程杰,胡冠芳.4"-脱氧阿维菌素脲类及硫脲类衍生物的合成与杀虫活性[J].农药学学报,2016,18(5):556-566. |
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| 作者姓名： | 张娜 成丕乐 南祥 吴小兵 刘映前 余海涛 张健 杨程杰 胡冠芳 |
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| 作者单位： | 1.兰州大学 药学院药物化学研究所, 兰州 730000 |
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| 基金项目： | 国家自然科学基金项目（31371975；30800720）. |
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| 摘 要： | 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LC50值分别为0.100和1.71 μmol/L，表现出很高的毒杀活性，化合物9o对甘蓝蚜的毒性最高，LC50值为1.13 μmol/L。
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| 关 键 词： | 阿维菌素B1a 脲 硫脲 合成 杀虫活性 |
| 收稿时间： | 5/6/2016 12:00:00 AM |
| 修稿时间： | 7/3/2016 12:00:00 AM |
Synthesis and insecticidal activity of 4"-deoxy-abamectin urea and thioure analogues |
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| ZHANG N,CHENG Pile,NAN Xiang,WU Xiaobing,LIU Yingqian,YU Haitao,ZHANG Jian,YANG Chengjie and HU Guanfang.Synthesis and insecticidal activity of 4"-deoxy-abamectin urea and thioure analogues[J].Chinese Journal of Pesticide Science,2016,18(5):556-566. |
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| Authors: | ZHANG N CHENG Pile NAN Xiang WU Xiaobing LIU Yingqian YU Haitao ZHANG Jian YANG Chengjie and HU Guanfang |
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| Institution: | 1.School of Pharmacy, Lanzhou University, Lanzhou 730000, China2.Institute of Plant Protection, Gansu Academy of Agricultural Sciences, Lanzhou 730000, China |
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| Abstract: | Based on SAR investigation, two series of abamectin analogues containing urea and acyl thiourea groups were designed according to analog synthesis and sub-structure. Their structures were confirmed by1H NMR, MS and elemental analysis. Their insecticidal activity was tested against Tetranychus cinnabarinus andBrevicoryne brassicae. All the tested compounds showed significant inhibitory activity against the above two insect species. Notably, the majority of those compounds exhibited high selectivity againstB. brassicae, some of which were much better in comparison to abamectin. Especially, compound9h displayed more potent activity than abamectin against the above two insect species, namely,T. cinnabarinus (LC50 = 0.100 μmol/L) andB. brassicae (LC50 = 1.71 μmol/L).Moreover, compound9o showed superior activity againstB. brassicae, with LC50 value of 1.13 μmol/L. |
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| Keywords: | abamectin urea acyl thiourea synthesis insecticidal activity |
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