【摘要】 用大肠杆菌(1515)测定了二十二个5-取代苄基-2,4-二氨基嘧啶类化合物的80%最低抑菌浓度,采用Hansch方法导出的定量构效相关式所表明苄基苯环上3,4,5-位取代基的立体参数(MR)之和与抑菌活性呈Kubinyi双线性关系。取代基的疏水性参数(π)未能改进这种相关。取代基的电性参数σR~-对定量相关式有不很明显的改善。更多还原

【Abstract】 The 80% minimum inhibitory concentration of 22 5-(substitutedbenzyl)-2, 4-diamino-pyrimidines (16 of them are not reported in literatures) were tested using Escherichia coli bacteria (1515). The quantitative structure-activity relationships analysis shows that the sum of the steric parameter (ΣMR) of 3,4,5-substituents on phenyl group of benzylpyrimidines are bilinearly correlated with the inhibitory activity (n=20, r=0.84, s=0.345). The hydrophobicparameter(π)of the substituent cannot improve the correlation and the electronic parameter σR- of substituent gives slight contribution to the correlation.更多还原