| 二氢叶酸还原酶抑制剂:5-取代苄基-2,4-二氨基嘧啶类化合物选择性作用的研究 |
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| 引用本文： | 李仁利,方肇霞.二氢叶酸还原酶抑制剂:5-取代苄基-2,4-二氨基嘧啶类化合物选择性作用的研究[J].药学学报,1986(10). |
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| 作者姓名： | 李仁利 方肇霞 |
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| 作者单位： | 北京医科大学药化教研室
(李仁利)，北京医科大学药化教研室(方肇霞) |
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| 摘 要： | 以47个5-取代苄基-2,4-二氨基嘧啶类化合物(其中四个为新合成的化合物)对乳酪菌二氢叶酸还原酶及鸡肝二氢叶酸还原酶的表现抑制常数(Ki app)研究这类化合物的结构与选择性作用的关系。以取代基的van der Waals体积(Vw)代替MR得到和以前结果相似的定量构效相关式。在此基础上讨论了5-取代苄基-2,4-二氨基嘧啶类化合物的选择性作用。
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| 关 键 词： | 5-取代苄基-2 4-二氨基嘧啶 二氢叶酸还原酶抑制剂 选择性作用 定量构效关系 |
INVESTIGATION OF THE SELECTIVITY OF DIHYDROFOLATE REDUCTASE INHIBITOR 5-SUBSTITUTEDBENZYL-2, 4-DIAMINO-PYRIMIDINES |
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| LI Ren-Li and FANG Zhao-Xia.INVESTIGATION OF THE SELECTIVITY OF DIHYDROFOLATE REDUCTASE INHIBITOR 5-SUBSTITUTEDBENZYL-2, 4-DIAMINO-PYRIMIDINES[J].Acta Pharmaceutica Sinica,1986(10). |
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| Authors: | LI Ren-Li and FANG Zhao-Xia |
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| Abstract: | The apparent inhibitory constants (Ki app) obtained from the action on dihydrofolate reductases from Lactobacillus casei bacteria and chicken liver of fourty-seven 5-subtituted-benzyl-2,4-diaminopyrimidines (among them 4 compounds are newly synthesized)have been used for investigation of the selectivity of this kind of compound. Similar QSAR equations as the results obtained in author's previous reports are correlated using van der Waals volume of substituents (V_w) instead of MR. The selectivity of this kind of compound is disscused on the basis of QSAR correlations. |
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| Keywords: | 5-Substitutedbenzyl-2 4-diaminopyrimidines Dihydrofolate reductase inhibitor Selectivity QSAR |
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