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ID: ALA1130640

Journal: Bioorg Med Chem Lett

Title: Lactate cannot substitute for alanine in d4T-based anti-HIV nucleotide prodrugs--despite efficient esterase-mediated hydrolysis.

Authors: McGuigan C, Cahard D, Ballatore C, Siddiqui A, De Clercq E, Balzarini J.

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.

CiteXplore: 9873653

DOI: 10.1016/s0960-894x(98)00530-7