Citation
Cr. Wagner et al., Antiviral nucleoside drug delivery via amino acid phosphoramidates, NUCLEOS NUC, 18(4-5), 1999, pp. 913-919
Citations number
10
Categorie Soggetti
Biochemistry & Biophysics
Journal title
NUCLEOSIDES & NUCLEOTIDES
ISSN journal
07328311
→ ACNP
Volume
18
Issue
4-5
Year of publication
1999
Pages
913 - 919
Database
ISI
SICI code
0732-8311(1999)18:4-5<913:ANDDVA>2.0.ZU;2-C
Abstract
Stable and water soluble amino acid phosphomonoester amidates of AZT were s
ynthesized and shown to have potent anti-HIV-1 activity. Intracellular and
cell extract metabolism studies revealed that these compounds are likely to
be enzymatically converted to the corresponding monophosphates. In additio
n, we have shown that the half life and tissue distribution of a phosphoram
idate of AZT is 5 and 10-fold greater, respectively, than AZT.