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.
出处
《有机化学》
SCIE
CAS
CSCD
北大核心
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~~
关键词
高异黄酮
合成
血管舒张
homoisoflavones
synthesis
vasodilatation
