Synthesis and antiviral properties of 5-vinylpyrimidine nucleoside analogs

Pharmacol Ther. 1984;26(1):1-44. doi: 10.1016/0163-7258(84)90049-4.

Abstract

5-Vinylpyrimidine nucleosides can be readily synthesized via organometallic intermediates from commercially available nucleosides. Highly potent and selective inhibitors of herpes simplex virus type 1 (HSV-1) and varicella-zoster virus (VZV) are (E)-5-(2-bromovinyl)-2'-deoxyuridine (BVDU) and some related analogs such as (E)-5-(2-iodovinyl)-2'-deoxyuridine (IVDU), 1-beta-D-arabinofuranosyl-(E)-5-(2-bromovinyl)uracil (BVaraU) and (E)-5-(2-bromovinyl)-2'-deoxycytidine (BVDC). The selective antiviral action of BVDU is based upon a specific phosphorylation by the virus-encoded deoxythymidine kinase (TK), inhibition of the viral DNA polymerase and/or incorporation into viral DNA. The efficacy of BVDU against HSV-1 and VZV infections has been demonstrated in animal models and phase I clinical trials. Possible limitations in the clinical usefulness of 5-vinylpyrimidine nucleosides in general and BVDU in particular are discussed.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Animals
  • Antiviral Agents / chemical synthesis*
  • Antiviral Agents / therapeutic use
  • Bromodeoxyuridine / analogs & derivatives
  • Bromodeoxyuridine / chemical synthesis
  • Bromodeoxyuridine / pharmacology
  • Bromodeoxyuridine / therapeutic use
  • Cell Line
  • Chemical Phenomena
  • Chemistry
  • Disease Models, Animal
  • Drug Resistance, Microbial
  • Fibroblasts
  • Herpesvirus 3, Human / drug effects
  • Humans
  • Mice
  • Pyrimidine Nucleosides / chemical synthesis*
  • Pyrimidine Nucleosides / pharmacology
  • Pyrimidine Nucleosides / therapeutic use
  • Rabbits
  • Simplexvirus / drug effects
  • Structure-Activity Relationship

Substances

  • Antiviral Agents
  • Pyrimidine Nucleosides
  • brivudine
  • Bromodeoxyuridine