中文摘要：

为了提高大豆苷元的抗动脉粥样硬化功效，利用药动团变换原理对大豆苷元进行修饰。文章采用微波法高产率合成了2个大豆苷元磺酸酯衍生物4和5。采用HPLC考察其药学性质，以及利用药物设计软件ChemAxon的计算结果对被试化合物的药代性质进行预测。实验表明，化合物4和5的溶解度相对与原药大豆苷元在乙酸乙酯中分别提高57600和17000倍，表观脂水分配系数LogP分别为2．02和1．67，衍生物5的水溶性相对与原药也得以提高。实验与计算结果表明，衍生物的药学性质相对于原药大豆苷元得到充分优化，预示其良好的药代性质和生物活性。

英文摘要：

To improve the effect of daidzein to inhibit the atherosclerosis, its structure was modified with using the principle of pharmacokinetic group. The two daidzein sulfonic acid ester derivatives （4 and 5） were synthesized in high yield by microwave irradiation. Their pharmaceutical properties were investigated by HPLC and the drug design software ChemAxon. Using the experimental and calculation results, their pharmacokinetic proper- ties were predicted. Experimental results showed that the solubility of compound 4 and 5 were increased by 57600 and 17000 times relative to daidzein in ethyl acetate, and the apparent lipid water partition coefficient LogP were 2.02 and 1.67 respectively. The water--soluble of derivative 5 was improved relative to daidzein also. The experi- mental and calculation results showed that the pharmaceutical properties of derivatives were fully optimized com- pared to the daidzein, and they had good pharmacokinetie properties and biological activity.