Synthesis and evaluation of amino acid ester prodrugs of penciclovir

Dae Kee Kim, Namkyu Lee, Guang Jin Im, Young Woo Kim, Kieyoung Chang, Hun Taek Kim, Yong Baik Cho, Won Son Choi, Inho Jung, Key H. Kim

Research output: Contribution to journalArticlepeer-review

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The synthesis, aqueous solubility and stability, in vitro antiviral activity, and oral bioavailability of the amino acid ester prodrugs of penciclovir, 13-20, 23, and 24, are described. All of the prodrugs were highly soluble (> 100 mg/mL) and sufficiently stable in aqueous solution. The oral bioavailability of O-acetyl-O-L-valylpenciclovir (13) (34%) in mice was comparable to that of famciclovir (33%) and approximately 4-fold higher than that of penciclovir.

Original languageEnglish
Pages (from-to)1849-1854
Number of pages6
JournalBioorganic and Medicinal Chemistry Letters
Issue number15
StatePublished - 6 Aug 1996


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