高等学校化学学报

高等学校化学学报

• 研究论文 • 上一篇    

蛇床子素肟醚衍生物的合成与抗菌活性研究

陈阳密，佘慧娴，汪  晴，杨家强   

  1. 遵义医科大学药学院, 贵州省化学药物创制全省重点实验室
  • 收稿日期:2025-05-20 修回日期:2025-06-22 网络首发:2025-06-24 发布日期:2025-06-24
  • 通讯作者: 杨家强 E-mail:yjqcn@126.com
  • 基金资助:
    贵州省科技计划项目(批准号：黔科合基础-ZK[2024]一般265)和国家级大学生创新创业训练计划项目(批准号：202310661006)资助

Synthesis and Antibacterial Activities of Osthole Oxime Ether Derivatives

CHEN Yangmi, SHE Huixian, WAN Qing, YANG Jiaqiang   

  1. Guizhou Provincial Key Laboratory of Innovation and Manufacturing for Pharmaceuticals, School of Pharmacy, Zunyi Medical University
  • Received:2025-05-20 Revised:2025-06-22 Online First:2025-06-24 Published:2025-06-24
  • Contact: YANG Jiaqiang E-mail:yjqcn@126.com
  • Supported by:
    Supported by the Guizhou Provincial Science and Technology Plan Project of China(No. Qiankehe Foundation ZK[2024]265) and the National College Students' innovation and entrepreneurship training program(No. 202310661006)

PDF (PC)

补充材料

1

摘要： 在前期研究的基础上，运用骨架跃迁原理，对抗革兰氏阳性菌活性化合物A进行结构优化，设计合成了18个蛇床子素肟醚衍生物，经1H NMR、13C NMR和元素分析确证其结构. 抗菌活性测试结果显示，该类化合物对金黄色葡萄球菌(S. aureus)和大肠杆菌(E. coli)的活性不显著，但意外地发现对脆弱拟杆菌(B. fragilis)和厌氧消化链球菌(P. anaerobius)有较好抑制作用，尤以化合物5d和5g最为显著，对B. fragilis的最小抑菌浓度(MIC)分别为1 μg/mL和2 μg/mL，与对照药甲硝唑相当，可作为先导化合物深入研究.

关键词: 蛇床子素衍生物, 肟醚, 合成, 抗菌活性

Abstract: Based on previous research, The structure of antibacterial active compound A were optimized using the scaffold hopping principle. Eighteen osthole oxime ether derivatives were designed and synthesized, and confirmed by 1H NMR, 13C NMR and elemental analysis. The antibacterial activities test results revealed that these compounds had insignificant activity against S. aureus and E. coli. However, they unexpectedly exhibited good inhibitory effects against B. fragilis and P. anaerobius. Notably, the compounds 5d and 5g demonstrated the most significant activity, with minimum inhibitory concentrations(MIC) of 1 μg/mL and 2 μg/mL against B.fragilis, respectively. Its antibacterial activities are comparable to the control drug metronidazole, which will be extensively studied as novel antibacterial lead compounds.

Key words: Osthole derivatives, Oxime ether, Synthesis, Antibacterial activity

中图分类号: 

TrendMD: