Orally bioavailable anti-HBV dinucleotide acyloxyalkyl prodrugs

Bioorg Med Chem Lett. 2010 Mar 1;20(5):1783-6. doi: 10.1016/j.bmcl.2010.01.010. Epub 2010 Jan 11.

Abstract

The acyloxyalkyl derivatives of a model anti-HBV dinucleotide were synthesized and evaluated as orally bioavailable prodrugs. Our studies have led to the identification of the first orally bioavailable dinucleotide prodrugs for further therapeutic development against the hepatitis B virus (HBV).

Publication types

  • Research Support, N.I.H., Extramural

MeSH terms

  • Administration, Oral
  • Animals
  • Antiviral Agents / chemical synthesis
  • Antiviral Agents / chemistry*
  • Antiviral Agents / therapeutic use
  • Cell Line
  • Female
  • Hepatitis B / drug therapy*
  • Hepatitis B virus / genetics*
  • Humans
  • Male
  • Mice
  • Mice, Transgenic
  • Mutation
  • Nucleotides / chemical synthesis
  • Nucleotides / chemistry*
  • Nucleotides / therapeutic use
  • Prodrugs / chemical synthesis
  • Prodrugs / chemistry*
  • Prodrugs / therapeutic use
  • Rats
  • Rats, Sprague-Dawley

Substances

  • Antiviral Agents
  • Nucleotides
  • Prodrugs