高异黄酮类化合物的合成及其舒张血管活性研究  

Synthesis and Vasodilatation of Homoisoflavones

作　　者：郑国勋[1] 张宗昌[1] 康博瑞[1] 于瑞红[1] 曹永孝[1] 张三奇[1] 

机构地区：[1]西安交通大学医学部,西安710061

出　　处：《有机化学》2015年第5期1112-1122,共11页Chinese Journal of Organic Chemistry

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

摘　　要：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.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.

关 键 词：高异黄酮 合成 血管舒张 

分 类 号：O621.3[理学—有机化学] TQ460.1[理学—化学]