摘要
以葛根黄豆甙元为先导化合物。设计合成9个衍生物,在结构鉴定的基础上,做了油/水分配系数和抗缺氧活性等测定。按Hansch模型进行拟合,经数学处理,结果得到lg1/C=3.347+0.7375lgP-0.07229(lgp)~2的抛物线形式的定量构效关系方程,初步揭示了这类化合物的结构与其抗缺氧活性之间的定量关系,为进一步筛选最佳化合物作心血管药物提供了重要依据。
This paper reports on the synthesis of 9 derivatives of Pueraria Lobata Isoflavones,in which etherification takes place in the 7 and 4' positions,by using daidzein as a lead compound; The structures of the compounds are proved by UV,IR,NMR and MS.The experimental results of distribution coefficient of oil/water and the effects of anti-hypoxia of parts are also reported.Hansch's model has been adopted to deal with experimental results mathematically,and the equation of QSAR obtained is as follows:lg 1/C=3.347+0.7375 lgP-0.07229 (lg P)2(R2=0.973,F=127.65,n=10)From the above equation it can be seen that lg P is the major cause affecting their activities.When the lg P of derivatives is 5.1,the activity of antihypoxia is most powerful
出处
《同济医科大学学报》
CAS
CSCD
北大核心
1990年第3期188-193,共6页
Acta Universitatis Medicinae Tongji
关键词
葛根
葛根黄豆甙元
定量构效
daidzeiri
isoflavones
structure-activity relationship
antihypoxia
