【摘要】 报道了10个5-取代苯氨基-2,4-二氨基嘧啶对大肠杆菌MB-1428二氢叶酸还原酶的抑制活性,并采用Hansch方程对它们的定量构效关系进行研究。其定量相关式与5-取代苄基-2,4-二基氨嘧啶类的不同,可能是由于-NH-的疏水性与-CH₂-不同,使它们与二氢叶酸还原酶活性部位的结合与5-取代苄基-2,4-二氨基嘧啶类的不同的关系更多还原

【Abstract】 Inhibitory activities to Escherichia coli MB-1428 dihydrofolate reductase of 10 5-（substituted-anilino）-2,4-diamino pyrimidines have been reported （see table）. Quantitative structure-activityrelationships utilizing Hansch approach has been studied. The correlation equation of 5-（substituted-anilino）-2,4-diamino pyrimidines is different with that of 5-（substituted-benzyl）-2,4-diaminopyrimidines. The hydrophobicity of-NH-group is different from that of -CH₂-group, in addition, thebond length and bond angle of C-NH-C and C-CH₂-C are different. It is guested that the bindingsite of substitued anilino moity with dihydrofolate reductase is probably different from that ofsubstituted benzyl moity. It might be the reason of the difference of the correlation equations ofthese two kinds of compound.更多还原