2-氨基和 2,4-二氨基嘧啶对体内具有抗布氏锥虫活性的 SAR 研究。
SAR of 2-amino and 2,4-diamino pyrimidines with in vivo efficacy against Trypanosoma brucei.
机构信息
SCYNEXIS Inc., PO Box 12878, Research Triangle Park, NC 27709-2878, USA.
出版信息
Bioorg Med Chem Lett. 2011 May 15;21(10):2816-9. doi: 10.1016/j.bmcl.2011.03.097. Epub 2011 Apr 1.
PMID:21507639
Abstract
A series of 2,4-diaminopyrimidines was investigated and compounds were found to have in vivo efficacy against Trypanosoma brucei in an acute mouse model. However, in vitro permeability data suggested the 2,4-diaminopyrimidenes would have poor permeability through the blood brain barrier. Consequently a series of 4-desamino analogs were synthesized and found to have improved in vitro permeability.
摘要
研究了一系列 2,4-二氨基嘧啶类化合物，发现其中一些化合物在急性小鼠模型中对布氏锥虫具有体内疗效。然而，体外渗透数据表明 2,4-二氨基嘧啶类化合物的血脑屏障通透性较差。因此，合成了一系列 4-去氨基类似物，发现它们的体外渗透性得到了改善。
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