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4''-脱氧阿维菌素脲类及硫脲类衍生物的合成与杀虫活性

张娜 成丕乐 南祥 吴小兵 刘映前 余海涛 张健 杨程杰 胡冠芳

农药学学报2016,Vol.18Issue(5):556-566,11.
农药学学报2016,Vol.18Issue(5):556-566,11.DOI:10.16801/j.issn.1008-7303.2016.0080

4''-脱氧阿维菌素脲类及硫脲类衍生物的合成与杀虫活性

Synthesis and insecticidal activity of 4''- deoxy-abamectin urea and thioure analogues

张娜 1成丕乐 1南祥 1吴小兵 1刘映前 1余海涛 2张健 1杨程杰 1胡冠芳2

作者信息

  • 1. 兰州大学药学院药物化学研究所,兰州 730000
  • 2. 甘肃省农业科学院植物保护研究所,兰州 730000
  • 折叠

摘要

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.

关键词

阿维菌素 B1a//硫脲/合成/杀虫活性

Key words

abamectin/urea/acyl thiourea/synthesis/insecticidal activity

分类

农业科技

引用本文复制引用

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):556-566,11.

基金项目

国家自然科学基金项目(31371975;30800720) (31371975;30800720)

农药学学报

OA北大核心CSCDCSTPCD

1008-7303

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