Lactate cannot substitute for alanine in d4T-based anti-HIV nucleotide prodrugs--despite efficient esterase-mediated hydrolysis
- Bioorg Med Chem Lett. 1998 Nov 3;8(21):2949-54. doi: 10.1016/S0960-894X(98)00530-7.
- 1. Welsh School of Pharmacy, Cardiff University, UK. [email protected]
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.