高等学校化学学报

高等学校化学学报

• 研究论文 • 上一篇    下一篇

氨基烷基萘酚类化合物的合成及其抑菌和杀线虫活性研究

张琦璘1，2，3，史衍常2，3，高 堃2，3，王林松2，3，宋亚东2，3，王郁森2，3，李鹏程2，3，刘 松2，3，邢荣娥2，3，宋 琳1，秦玉坤2，3   

  1. 1. 青岛科技大学生物工程学院 2. 中国科学院海洋研究所，实验海洋生物学重点实验室 3. 青岛海洋科技中心，海洋药物与生物制品功能实验室
  • 收稿日期:2025-01-28 修回日期:2025-03-28 网络首发:2025-03-29 发布日期:2025-03-29
  • 通讯作者: 秦玉坤 E-mail:ykqin@qdio.ac.cn
  • 基金资助:
    国家自然科学基金(批准号: 42076126)、山东省重点研发计划重大科技创新项目(批准号: 2022CXGC020413)、青岛市科技惠民示范专项(批准号: 25-1-5-xdny-7-nsh)和现代农业产业技术体系专项(批准号: CARS-49)资助

Synthesis of aminoalkyl naphthol analogues and their anti-fungal and nematicidal activities

ZHANG Qilin1,2,3, SHI Yanchang2,3, GAO Kun2,3, WANG Linsong2,3, SONG Yadong2,3, WANG Yusen2,3, LI Pengcheng2,3, LIU Song2,3, XING Ronge2,3, SONG Lin1, QIN Yunkun2,3   

  1. 1. Bioengineering College, Qingdao University of Science and Technology

    2.Key Laboratory of Experimental Marine Biology, Institute of Oceanology, Chinese Academy of Sciences

    3. Functional laboratory for Marine Drugs and Bioproducts, Qingdao Marine Science and Technology Center

  • Received:2025-01-28 Revised:2025-03-28 Online First:2025-03-29 Published:2025-03-29
  • Contact: QIN Yunkun E-mail:ykqin@qdio.ac.cn
  • Supported by:
    Supported by the National Natural Science Foundation of China (No. 42076126), Shandong Key R&D Plan, Major Scientific and Technological Innovation Project (No. 2022CXGC020413), Qingdao Science and Technology Benefit the People Demonstration Project (No. 25-1-5-xdny-7-nsh), Special Project on Modern Agricultural Industry Technology System (No. CARS-49)

PDF (PC)

补充材料

1

摘要： 随着现代农业的快速发展，植物真菌病害和线虫问题日益凸显，对农业生产构成了严重威胁。因此，寻找一种新型、高效且环境友好的农药活性物质，成为当前农业科学研究的重要课题。为了发现一类兼具抑菌和杀线虫活性的新型农药活性物质，本研究通过一锅法三组分由醛、乙腈/乙酰胺/尿素和2-萘酚，首次设计并合成了一系列氨基烷基萘酚类化合物，并对其抗植物病原真菌和杀线虫活性进行了试验。在 200 μg/mL 至 25 μg/mL 的浓度范围内，化合物 10 对链格孢菌的抑制活性约为 50%，且无明显的浓度依赖性。此外，活体抑菌实验发现，化合物10在50 μg/mL浓度下的治疗作用与阳性对照嘧菌酯相当。同时，在温室试管试验中，合成化合物对南方根结线虫有显著的防治效果，化合物 14 在 10 μg/mL 浓度下可显著减少根结数量，抑制率约为 90.91%，与阳性对照氟吡菌酰胺相当。本研究成功合成了一系列具有潜在农药活性的氨基烷基萘酚类化合物，为新型农药的研发奠定了基础。

关键词: 一锅法, 氨基烷基萘酚, 抗植物病原真菌活性, 杀线虫活性

Abstract: With the rapid development of modern agriculture, the problems of plant fungal diseases and nematodes are becoming more and more prominent, seriously threatening agricultural production. Therefore, the search for a new, efficient and environmentally friendly pesticide active substance has become an important issue in current agricultural scientific research. In this study, in order to discover a new class of pesticide active substances with both anti-fungal and nematicidal activities, a series of aminoalkyl naphthol analogs were designed and synthesized for the first time by a one-pot, three-component method consisting of aldehyde, acetonitrile/amide/urea and 2-naphthol and their anti-pathogenic fungal and nematicidal activities were tested. The inhibitory activity of compound 10 against Alternaria alternata was about 50 % within the concentration range of 200 μg/mL to 25 μg/mL, with no significant concentration dependence. In addition, in vivo curative experiment against A. alternate found that compound 10 had comparable therapeutic action to the positive control azoxystrobin at 50 μg/mL. Meanwhile, target compound had signi?cant control e?cacy on Meloidogyne incognita under the greenhouse test-tube assay. Compound 14 could signi?cantly reduce the number of root knots at 10 μg/mL, at which the inhibition rate was about 90.91 %, which was comparable to that of the positive control fluopyram. The present work indicates that amidoalkyl naphthol can be used as promising candidates for the development of anti-phytopathogenic fungal and nematicidal activity agents.

Key words: One pot method, Amidoalkyl naphthol, Anti-fungal activity, Nematicidal activity

中图分类号: 

TrendMD: