摘要
在黄豆甙元化学结构的基础上,合成了一系列异黄酮衍生物。由相应的脱氧安息香与N,N-二甲基甲酰胺缩二甲醇环合而得相应的异黄酮或与醋酐醋酸钠环合而为2-甲基异黄酮,再进行Mannich反应和醚化而得目的物。初筛表明化合物Ⅰ_(1～3),Ⅰ_5,Ⅱ_1,Ⅲ_2有明显耐缺氧作用。Ⅰ_1,Ⅰ_5还有显著的扩张冠脉作用。
On the basis of the chemical structure of daidzein, a series of isoflavones have been synthesized. The intermediates, 7-methoxy-4'-hydroxyisoflavone(V) and 7-hydroxy-4'-methoxyisoflavone(Ⅸ) were prepared by condensation of corresponding desoxybenzoin with dimethylformamide dimethylacetal. 7-Methoxy-2-methyl-4'-hydroxyisoflavone (Ⅶ) was also prepared from desoxybenzoin Ⅳ by reacting with acetic anhydride and anhydrous sodium acetate and followed by hydrolysis.Compounds Ⅰ_(1～5) were obtained by Mannich reaction and compounds Ⅱ_(1,2) Ⅲ_(1,2) were obtained by etherification of corresponding isoflavones.All compounds were tested for resistance to hypoxia in mice and Ⅰ_(1～3), Ⅰ_5, Ⅱ_1 and Ⅲ_2 were shown to have significant effect. Compound Ⅰ_1 and Ⅰ_5 were also found to increase coronary blood flow.
出处
《药学学报》
CAS
CSCD
北大核心
1989年第12期906-912,共7页
Acta Pharmaceutica Sinica
关键词
异黄酮衍生物
心血管药物
Isoflavones
Resistance to hypoxia
Dilation of coronary artery
