Anti-HBV specific beta-L-2'-deoxynucleosides

Nucleosides Nucleotides Nucleic Acids. 2001 Apr-Jul;20(4-7):597-607. doi: 10.1081/NCN-100002336.

Abstract

A unique series of simple unnatural L-nucleosides that specifically inhibit hepatitis B virus (HBV) replication has been discovered. These molecules have in common a hydroxyl group in the 3'-position (3'-OH) of the beta-L-2'-deoxyribose sugar that confers antiviral activity specifically against hepadnaviruses. Replacement of the 3'-OH broadens activity to other viruses. Substitution in the base decreases antiviral potency and selectivity. Human DNA polymerases and mitochondrial function are not effected. Plasma viremia is reduced up to 8 logs in a woodchuck model of chronic HBV infection. These investigational drugs, used alone or in combination, are expected to offer new therapeutic options for patients with chronic HBV infection.

Publication types

  • Review

MeSH terms

  • Animals
  • Antiviral Agents / chemistry
  • Antiviral Agents / pharmacology*
  • Deoxyadenosines / chemistry
  • Deoxyadenosines / pharmacology
  • Deoxycytidine / chemistry
  • Deoxycytidine / pharmacology
  • Deoxyribonucleosides / chemistry
  • Deoxyribonucleosides / pharmacology*
  • Hepatitis B Virus, Woodchuck / drug effects
  • Hepatitis B Virus, Woodchuck / physiology
  • Hepatitis B virus / drug effects*
  • Hepatitis B virus / physiology
  • Hepatitis B, Chronic / drug therapy
  • Humans
  • Structure-Activity Relationship
  • Substrate Specificity
  • Thymidine / chemistry
  • Thymidine / pharmacology
  • Virus Replication / drug effects

Substances

  • Antiviral Agents
  • Deoxyadenosines
  • Deoxyribonucleosides
  • Deoxycytidine
  • Thymidine