Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 19, Issue 3, Pages 792-796Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2008.12.031
Keywords
Vidarabine; ara-A; Amino acid ester prodrug; Phosphoramidate prodrug; Antiviral activity; Selective protection of nucleoside; Levulinate ester; Oral bioavailability; Adenosine deaminase; Arahypoxanthine; ara-H; Caco-2 permeability
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Funding
- National Institutes of Health [1R43AI071400]
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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. (C) 2008 Elsevier Ltd. All rights reserved.
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