SYNTHESIS AND EVALUATION OF AMINO-ACID ESTER PRODRUGS OF PENCICLOVIR

Authors
KIM DK LEE N IM GJ KIM YW CHANG K KIM HT CHO YB CHOI WS JUNG I KIM KH
Citation
Dk. Kim et al., SYNTHESIS AND EVALUATION OF AMINO-ACID ESTER PRODRUGS OF PENCICLOVIR, Bioorganic & medicinal chemistry letters, 6(15), 1996, pp. 1849-1854
Citations number
13
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
6
Issue
15
Year of publication
1996
Pages
1849 - 1854
Database
ISI
SICI code
0960-894X(1996)6:15<1849:SAEOAE>2.0.ZU;2-C
Abstract
The synthesis, aqueous solubility and stability, in vitro antiviral ac tivity, and oral bioavailability of the amino acid ester prodrugs of p enciclovir, 13-20, 23, and 24, are described. All of the prodrugs were highly soluble (>100 mg/mL) and sufficiently stable in aqueous soluti on. The oral bioavailability of O-acetyl-O-L-valylpenciclovir (13) (34 %) in mice was comparable to that of famciclovir (33%) and approximate ly 4-fold higher than that of penciclovir. Copyright (C) 1996 Elsevier Science Ltd