| 丹皮酚苯磺酰腙类衍生物的合成及杀粘虫活性研究 |
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| 引用本文： | 陈根强,杨进明,孙迪,韩笑笑,田月娥,刘圣明,姜佳,车志平. 丹皮酚苯磺酰腙类衍生物的合成及杀粘虫活性研究[J]. 化学通报, 2020, 83(2): 139-143 |
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| 作者姓名： | 陈根强 杨进明 孙迪 韩笑笑 田月娥 刘圣明 姜佳 车志平 |
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| 作者单位： | 河南科技大学林学院农药设计与合成实验室 洛阳471023 |
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| 基金项目： | 国家自然科学基金资助项目(U1604105)；河南省自然科学基金(182300410043,182300410016,152300410082)；河南科技大学SRTP项目(2019406) |
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| 摘 要： | 丹皮酚可作用于乙酰胆碱酯酶、穿过血脑屏障,该作用机理为使其可能开发成为新型杀虫剂。鉴于此,本文合成了5个丹皮酚苯磺酰腙类衍生物(5a～5e),并评价了它们对威胁农作物的害虫的杀虫活性。在1mg/mL浓度下,以川楝素为阳性对照,采用小叶碟添加法测定化合物3和5a～5e的杀粘虫活性。其中,化合物5e杀虫活性显著,最终校正死亡率(FMR=50.0%)与商品化植物源杀虫剂川楝素等同。初步构效关系研究表明,丹皮酚羰基位修饰是可行的;中间体3的亚胺位磺化修饰可提高杀虫活性,且磺化取代基不同活性差异显著。此外,实验还发现试虫取食了附有供试化合物的叶片后在幼虫期、化蛹期和羽化期均出现不同程度、不同状况的非正常生长。
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| 关 键 词： | 天然产物 丹皮酚 苯磺酰腙 杀虫活性 构效关系 |
| 收稿时间： | 2019-10-22 |
| 修稿时间： | 2019-10-25 |
Syntheses and Insecticidal Activities of Some Paeonol-Based Phenylsulfonylhydrazone Derivatives Against Mythimna separata In Vivo |
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| Chen Genqiang,Yang Jinming,Sun Di,Han Xiaoxiao,Tian YueE,Liu Shengming,Jiang Jia and Che Zhiping. Syntheses and Insecticidal Activities of Some Paeonol-Based Phenylsulfonylhydrazone Derivatives Against Mythimna separata In Vivo[J]. Chemistry, 2020, 83(2): 139-143 |
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| Authors: | Chen Genqiang Yang Jinming Sun Di Han Xiaoxiao Tian YueE Liu Shengming Jiang Jia Che Zhiping |
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| Affiliation: | Laboratory of Pesticidal Design Synthesis,College of Forestry,Henan University of Science and Technology,Laboratory of Pesticidal Design Synthesis,College of Forestry,Henan University of Science and Technology,Laboratory of Pesticidal Design Synthesis,College of Forestry,Henan University of Science and Technology,Laboratory of Pesticidal Design Synthesis,College of Forestry,Henan University of Science and Technology,Laboratory of Pesticidal Design Synthesis,College of Forestry,Henan University of Science and Technology,Laboratory of Pesticidal Design Synthesis,College of Forestry,Henan University of Science and Technology,Laboratory of Pesticidal Design Synthesis,College of Forestry,Henan University of Science and Technology,Laboratory of Pesticidal Design Synthesis,College of Forestry,Henan University of Science and Technology |
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| Abstract: | Paeonol inhibits acetylcholinesterase (AChE), and across the blood-brain barrier (BBB), which lays a solid foundation for the development of new insecticides. In view of this, five paeonol-based phenylsulfonylhydrazone derivatives were synthesized and evaluated for their insecticidal activity against a crop-threatening agricultural pest, the pre-third-instar larvae of Mythimna separate in vivo at the concentration of 1 mg/mL. Among all the target compounds, compounds 5e exhibited more promising insecticidal activity, and the final mortality rates (FMRs) of 5e and toosendanin were both of 50.0%. Meanwhile, some interesting the structure-activity relationship results of tested compounds were also discovered: modification of carbonyl of paeonol is acceptable; modification of imino group of 3 is important for insecticidal activity, and different sulfonated substituents showed significant difference in activity. In addition, owing to feeding too much compounds coated leaves, some larvae of M. separata showed developmental abnormalities during larve, pupae and adult stages. |
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| Keywords: | Natural product, Paeonol, Phenylsulfonylhydrazone, Insecticidal activity, Structure-activity relationship |
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