叶酸拮抗剂。21. 2,4-二氨基-6-(苄基氨基)吡啶并[3,2-d]嘧啶的合成及抗疟特性
Folate antagonists. 21. Synthesis and antimalarial properties of 2,4-diamino-6-(benzylamino)pyrido[3,2-d]pyrimidines.
作者信息
Colbry N L, Elslager E F, Werbel L M
出版信息
J Med Chem. 1985 Feb;28(2):248-52. doi: 10.1021/jm00380a018.
PMID:3881585
Abstract
The synthesis and antimalarial activity of a series of 2,4,6-triaminopyrido[3,2-d]pyrimidines (4) is described. Several 6-substituted benzylmethylamino analogues were more active against trophozoite induced Plasmodium berghei in mice than the corresponding quinazoline analogues. These agents, however, are cross-resistant to other antifolate compounds and are thus of limited potential as human agents.
摘要
描述了一系列2,4,6-三氨基吡啶并[3,2-d]嘧啶（4）的合成及其抗疟活性。几种6-取代苄基甲基氨基类似物对小鼠体内由滋养体诱导的伯氏疟原虫的活性比相应的喹唑啉类似物更高。然而，这些药物对其他抗叶酸化合物具有交叉抗性，因此作为人类用药的潜力有限。
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