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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.

DOI:10.1016/j.bmcl.2008.12.031
PMID:19097789
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC2642980/
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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Amino acid ester prodrugs of 2-bromo-5,6-dichloro-1-(beta-D-ribofuranosyl)benzimidazole enhance metabolic stability in vitro and in vivo.2-溴-5,6-二氯-1-(β-D-呋喃核糖基)苯并咪唑的氨基酸酯前药在体外和体内均增强代谢稳定性。
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