摘要
根据电子等排原理,合成了5个2,4-二氨基-5-烷氧基苯氨嘧啶类化合物,它们对大肠杆菌1515的抗菌活性均弱于TMP。与以前合成的20个化合物一起进行Hansch相关分析,结果表明抑菌作用与取代基的MR呈线性相关。2-位取代基与3,4-位及5-位取代基对化合物抑菌活性的贡献各不相同。
On the basis of isosteric principle, five compounds of 2,4-diamino-5-alkoxylanilinopyrirnidines were synthesized by condensation of 5-bromouracil with corresponding alkoxyl anilines, followed by chlorination with POC1, and animation under high pressure. The antibacterial activities growth inhibition to E.coli 1515 of these compounds were also reported. The results showed that the their in vitro activity are less potent than trimethoprim.Quantitative structure-activity relationship studies utilizing Hansch approach with the previously reported 20 compounds show that the inhibitory activity in linearly correlated with MR of substitue-nts on benzene ring. Substituents on 2-position, 3, 4-position and 5 -position gine different contribution to the inhibitory activity.
出处
《北京医科大学学报》
CSCD
1989年第4期311-313,共3页
Journal of Peking University(Health Sciences)
基金
中国科学院科学基金
关键词
嘧啶
合成
定量构效关系
2,4-diamino-5-alkoxyl anilino pyrimidine Quantitative structure-activity relationship (QSAR)
