Antiherpes activity of [E]-5-(1-propenyl)-2'-deoxyuridine and 5-(1-propenyl)-1-beta-D-arabinofuranosyluracil

Antiviral Res. 1981 Nov;1(4):213-23. doi: 10.1016/0166-3542(81)90012-7.

Abstract

5-(1-Propenyl)-1-beta-D-arabinofuranosyluracil has been synthesized, and this compound and [E]-5-(-propenyl)-2'-deoxyuridine have been tested for inhibition of herpes virus multiplication. Only [E]-5-(1-propenyl)-2'-deoxyuridine was found to be an active inhibitor reducing by 50% the plaque formation of herpes simplex virus type 1 (HSV-1) at about 1 muM. A comparison to the bromovinyl derivatives showed the following order of descending activity; [E]-5-(2-bromovinyl)-2'-deoxyuridine greater than 5-(2-bromovinyl)-1-beta-D-arabinofuranosyluracil greater than or equal to [E]-5-(1-propenyl)-2'-deoxyuridine greater than 5-(1-propenyl)-1-beta-arabinofuranosyluracil. HSV-1 mutants lacking thymidine kinase or resistant against acycloguanosine were resistant against [E]-5-(1-propenyl)-2'-deoxyuridine. All compounds seemed to be phosphorylated by HSV-1 thymidine kinase in a cell-free assay. The compounds were phosphorylated to a lower extent by cellular or HSV-2 thymidine kinase, and the HSV-2 strains tested were inhibited by less than 50% at 100 muM in plaque assays. A selective inhibition of HAV-1 DNA synthesis by [E]-5-(1-propenyl)-2'-deoxyuridine was observed in infected cells indicating an effect on viral DNA polymerase. [E]-5-(1-Propenyl)-2'-deoxyuridine had a low cellular toxicity and a therapeutic effect when applied topically to HSV-1-infected guinea pig skin.

MeSH terms

  • Animals
  • Antiviral Agents / pharmacology*
  • Arabinofuranosyluracil* / analogs & derivatives*
  • Arabinonucleosides / pharmacology*
  • Cell Division / drug effects
  • Cell Line
  • Chlorocebus aethiops
  • DNA / biosynthesis
  • DNA, Viral / biosynthesis
  • Deoxyuridine / analogs & derivatives*
  • Deoxyuridine / pharmacology
  • Guinea Pigs
  • Herpes Simplex / drug therapy*
  • Phosphorylation
  • Simplexvirus / drug effects
  • Simplexvirus / growth & development
  • Thymidine / metabolism
  • Uridine / analogs & derivatives*
  • Uridine / pharmacology
  • Viral Plaque Assay

Substances

  • Antiviral Agents
  • Arabinonucleosides
  • DNA, Viral
  • Arabinofuranosyluracil
  • 5-(1-propenyl)-2'-deoxyuridine
  • 5-(1-propenyl)-1-arabinofuranosyluracil
  • DNA
  • Thymidine
  • Deoxyuridine
  • Uridine