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Lactate cannot substitute for alanine in d4T-based anti-HIV nucleotide prodrugs--despite efficient esterase-mediated
C McGuigan1, D Cahard, C Ballatore
1Welsh School of Pharmacy, Cardiff University, UK. mcguigan@cardiff.ac.uk
Bioorganic & Medicinal Chemistry Letters
|January 5, 1999
Abstract:
As part of our on-going effort to deliver masked phosphates of antiviral nucleosides inside living cells we have previously discovered that amino acid-derived phosphoramidates are particularly effective. Here we report that lactate analogues, with a simple change of bridging nitrogen for oxygen, are virtually inactive as antiviral agents and apparently do not achieve intracellular nucleoside phosphate delivery.