磺胺类药物的 HPLC 参数 log k'与生物活性之间的关系
THE RELATIONSHIP BETWEEN HPLC PARAMETER log k'AND BIOLOGICAL ACTIVITY OF SULFA DRUGS
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摘要: 本文研究了磺胺类药物的 HPLC 参数 log k'与辛醇/水分配系数的对数值 log P 的关系以及 log k'与磺胺类药物体外抑制大肠杆菌活性的关系。通过对这两个关系的比较,提出可用色谱参数 log k'代替 Hansch 方程中的iog P 进行磺胺类药物构效关系的研究。同时指出,对于所试验的磺胺类药物来说,log k'可以成为一个较好的疏水性参数。Abstract: The octanol-water partition coefficient,log P and biological activity of sulfadrugs were both correlated with HPLC parameter,log k'(capacity factor).By comparing these two kinds of relationships,it was found that the log P in Hansch'sequation might be substituted by log k'in the correlation of chemical structure with the minimum inhibitory concentration of the tested sulfa drugs against E.coli in vitro, and good correlations were obtained.