大豆黄素-4’-甲氧基-7-萘磺酸酯的微波合成及药学性质研究

Microwave Synthesis and Pharmacological Properties of Daidzein-4’-methoxy-7-naphthalenesulfonate

以改善大豆黄素(D1)的药学性质,根据药动团变换原理对D1进行了结构修饰。利用微波加热法高效合成未见报道的大豆黄素-4’-甲氧基-7-萘磺酸酯(D3)。通过对D3的药学性质的考察,分析其构性关系。结果表明,与D1相比,D3在乙酸乙酯中的溶解度提高了3.42×105倍,表观脂水分配系数(lgP)为2.07±0.01。构性关系的研究表明,药物药学性质与其结构密不可分,合适的溶解度预示药物的生物利用度会有所提高。

The novel daidzein napsylate derivative(daidzein-4’-methoxy-7-naphthalenesulfonate)was synthesized in high yield by microwave irradiation to improve its pharmacological properties,according to structural modification of daidzein(D1)using the principle of pharmacokinetic transformation.The pharmaceutical properties of D3 were investigated to analyze the structure-property relationship.The results showed that the solubility of D3 was increased by 3.42×105 times relative to D1 in ethyl acetate,and the apparent lipid water partition coefficient(lg P)was 2.07±0.01.The results showed that the absorption and utilization of drugs were closely related to their physicochemical properties.