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李仁利, 倪文升, 赵维璋
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Ren-Li Li, Wen-Sheng Zhang, Wei-Zhang Zhao
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摘要： 根据生物电子等排原理用硫和亚氨基代替甲氧苄氨嘧啶(TMP)分子中苯环与二氨基嘧啶环间的次甲基, 以研究苄基嘧啶分子中桥链部分在抑酶活性中所起的作用。应用Hansch方法研究了定量构效关系。在定量构效关系的基础上讨论了桥链部分在抑制大肠杆菌二氢叶酸还原酶中的作用。
关键词: 5-取代-2,4-二氨基嘧啶, 二氢叶酸还原酶抑制菌, 定量构效关系
Abstract: The methylene group between the phenyl ring and the diaminopyrimidine ring of trimethoprim (TMP) was bioisosteristically displaced by thio or imino groups in order to study the rolein the inhibitory activity of the bridge moiety in the molecule of benzyl pyrimidines. The Hansch approach was used in the study of quantitative structure-activity relationships (QSAR). On the basis of QSAR studies the role of the bridge moiety in inhibiting Escherichia coli dihydrofolate reductase was discussed.
Key words: 5-Substituted-2, 4-diaminopyrimidine, Dihydrofolate reductase inhibitor, Quantita-tive structure-activity relationships (QSAR)
Supporting:
李仁利, 倪文升, 赵维璋. 5-取代-2,4-二氨基嘧啶对大肠杆菌二氢叶酸还原酶抑制作用的定量构效关系的研究[J]. .
Ren-Li Li, Wen-Sheng Zhang, Wei-Zhang Zhao. QSAR Study on the Inhibitory Action of 5-Substituted-2,4-diaminopyrimidines on Escherichia coliDihydrofolateReductase[J]. .
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链接本文: http://jcps.bjmu.edu.cn/CN/
http://jcps.bjmu.edu.cn/CN/Y1994/V3/I1/6
宋怀恩, 沈建华*, 闻韧*, 蒋华良
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