Rational design of a new series of pronucleotide

Bioorg Med Chem Lett. 2001 Jul 9;11(13):1775-7. doi: 10.1016/s0960-894x(01)00299-2.

Abstract

A new pronucleotide series is described involving a two-step degradation process mediated by, respectively, carboxylesterase and phosphoramidase. Taking AZT as nucleosidyl moiety, it is shown that most of the compounds inhibit HIV replication in TK(-) cell line, which proves 5'-AZTMP delivery.

MeSH terms

  • Anti-HIV Agents / chemical synthesis*
  • Anti-HIV Agents / chemistry
  • Anti-HIV Agents / pharmacology
  • Chromatography, High Pressure Liquid
  • Drug Design*
  • HIV / physiology
  • Nucleotides / chemistry*
  • Nucleotides / pharmacology
  • Prodrugs / chemistry
  • Prodrugs / pharmacology
  • Virus Replication / drug effects

Substances

  • Anti-HIV Agents
  • Nucleotides
  • Prodrugs