| 陈根强,杨进明,孙迪,韩笑笑,田月娥,刘圣明,姜佳,车志平.化学通报,2020,83(2):139-143. |
| 丹皮酚苯磺酰腙类衍生物的合成及杀粘虫活性研究 |
| Syntheses and Insecticidal Activities of Some Paeonol-Based Phenylsulfonylhydrazone Derivatives Against Mythimna separata In Vivo |
| 投稿时间：2019-10-22 修订日期：2019-11-04 |
| DOI： |
| 中文关键词: 天然产物 丹皮酚 苯磺酰腙 杀虫活性 构效关系 |
| 英文关键词:Natural product Paeonol Phenylsulfonylhydrazone Insecticidal activity Structure-activity relationship |
| 基金项目:国家自然科学基金项目（U1604105）、河南省自然科学基金项目（182300410043，182300410016，152300410082）和河南科技大学SRTP项目（2019406）资助 |
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| 中文摘要: |
| 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。 |
| 英文摘要: |
| Paeonol can inhibite 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 (5a~5e) were synthesized and evaluated for their in vivo insecticidal activity against a crop-threatening agricultural pest, the pre-third-instar larvae of Mythimna separate, at the concentration of 1mg/mL. Among all the target compounds, compound 5e exhibited significant insecticidal activity, and the final corrected mortality (FMR=50.0%) was equivalent to toosendanin. Meanwhile, some interesting structure-activity relationship results were also discovered:modification of carbonyl on paeonol is acceptable; modification of imino group of intermediate 3 is important for insecticidal activity, and different sulfonated substituents show significant difference in activity. In addition, the insects fed with leaves containing the test compound showed developmental abnormalities during larve, pupae and adult stages. |
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