有机化学 ›› 2015, Vol. 35 ›› Issue (5): 1112-1122.DOI: 10.6023/cjoc201411033 上一篇    下一篇

研究简报

高异黄酮类化合物的合成及其舒张血管活性研究

郑国勋, 张宗昌, 康博瑞, 于瑞红, 曹永孝, 张三奇   

  1. 西安交通大学医学部 西安 710061
  • 收稿日期:2014-11-20 修回日期:2014-12-30 发布日期:2015-01-14
  • 通讯作者: 张三奇 E-mail:sqzhang@mail.xjtu.edu.cn
  • 基金资助:

    陕西省科技统筹创新工程项目基金(No.2012KPCL03-20)资助项目.

Synthesis and Vasodilatation of Homoisoflavones

Zheng Guoxun, Zhang Zongchang, Kang Borui, Yu Ruihong, Cao Yongxiao, Zhang Sanqi   

  1. Xi'an Jiaotong University Health Science Center, Xi'an 710061
  • Received:2014-11-20 Revised:2014-12-30 Published:2015-01-14
  • Supported by:

    Project supported by the Innovation Project on Science and Technology of Shanxi Province (No.2012KPCL03-20).

采用药物分子设计中的骨架迁跃原理, 设计了作为血管舒张剂的高异黄酮类化合物. 以2-乙酰苯酚和取代的苯甲醛为原料, 通过羟醛缩合、催化氢化、与N,N-二甲基甲酰胺二甲缩醛反应成环三步反应合成了19个高异黄酮类化合物, 其中15个未见文献报道. 采用1H NMR、MS和HRMS对合成的目标化合物进行了结构表征. 离体动脉环张力实验证明, 在浓度为10-5 mol/L时, 部分化合物具有显著的舒张血管活性.

关键词: 高异黄酮, 合成, 血管舒张

Homoisoflavones were designed as vasodilative agents on the basis of scaffold hopping. A series of homoisoflavones were synthesized from 2-acetylphenol and aromatic aldehyde via aldol condensation, hydrogenation and cyclization. The structures of title compounds were characterized by 1H NMR, MS and HRMS. The vasodilative effects of synthesized compounds were evaluated by wire myograph on isolated rat mesenteric arterial ring induced contraction with 60 mmol/L KCl. The results suggest that the title compounds are novel vasodilative agents.

Key words: homoisoflavones, synthesis, vasodilatation