设计和合成阿糖腺苷前药作为抗病毒药物。
Design and synthesis of vidarabine prodrugs as antiviral agents.
机构信息
TSRL Inc., 540 Avis Drive Suite A, Ann Arbor, MI 48108, USA.
出版信息
Bioorg Med Chem Lett. 2009 Feb 1;19(3):792-6. doi: 10.1016/j.bmcl.2008.12.031. Epub 2008 Dec 10.
Abstract
5'-O-D- and L-amino acid derivatives and 5'-O-(D- and L-amino acid methyl ester phosphoramidate) derivatives of vidarabine (ara-A) were synthesized as vidarabine prodrugs. Some compounds were equi- or more potent in vitro than vidarabine against two pox viruses and their uptake by cultured cells was improved compared to the parent drug.
摘要
5'-O-D-和 L-氨基酸衍生物以及 5'-O-(D-和 L-氨基酸甲酯膦酸酯)衍生物的阿糖腺苷（ara-A）被合成作为阿糖腺苷前体药物。一些化合物在体外对两种痘病毒的活性与阿糖腺苷相当或更强，并且与母体药物相比，其被培养细胞摄取的能力得到了提高。
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