2. Academic Validation
  3. Lactate cannot substitute for alanine in d4T-based anti-HIV nucleotide prodrugs--despite efficient esterase-mediated hydrolysis

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.
C McGuigan 1,  D Cahard,  C Ballatore,  A Siddiqui,  E De Clercq,  J Balzarini
Affiliations

Affiliation

PMID: 9873653 DOI: 10.1016/S0960-894X(98)00530-7
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.

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