Antiviral activities of 5-ethynyl-1-beta-D-ribofuranosylimidazole-4- carboxamide and related compounds

Antimicrob Agents Chemother. 1991 Apr;35(4):679-84. doi: 10.1128/AAC.35.4.679.

Abstract

A series of novel compounds, 5-alkynyl-1-beta-D-ribofuranosylimidazole-4- carboxamides, have been identified as broad-spectrum antiviral agents. 5-Ethynyl-1-beta-D-ribofuranosylimidazole-4- carboxamide (EICAR), the most potent congener of the group, showed antiviral potency about 10- to 100-fold greater than that of ribavirin. Similar in spectrum to ribavirin, EICAR was particularly active (50% inhibitory concentration, 0.2 to 4 micrograms/ml) against poxviruses (vaccinia virus), togaviruses (Sindbis and Semliki forest viruses), arenaviruses (Junin and Tacaribe viruses), reoviruses (reovirus type 1), orthomyxoviruses (influenza A and B viruses), and paramyxoviruses (parainfluenza virus type 3, measles virus, subacute sclerosing panencephalitis virus, and respiratory syncytial virus). EICAR was also cytostatic for rapidly growing cells (50% inhibitory concentration, 0.2 to 0.9 microgram/ml). EICAR inhibited vaccinia virus tail lesion formation at doses that were not toxic to the host. EICAR is a candidate antiviral drug for the treatment of pox-, toga-, arena-, reo-, orthomyxo, and paramyxovirus infections.

Publication types

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

MeSH terms

  • Adenosylhomocysteinase
  • Animals
  • Antimetabolites
  • Antiviral Agents / pharmacology*
  • Cell Line
  • Cell Survival / drug effects
  • DNA, Viral / biosynthesis
  • Hydrolases / antagonists & inhibitors
  • Mice
  • RNA, Viral / biosynthesis
  • Ribavirin / pharmacology
  • Ribonucleosides / pharmacology*
  • Tail / microbiology
  • Vaccinia virus / drug effects
  • Viral Proteins / biosynthesis
  • Virus Diseases / drug therapy
  • Virus Diseases / microbiology
  • Viruses / drug effects

Substances

  • Antimetabolites
  • Antiviral Agents
  • DNA, Viral
  • RNA, Viral
  • Ribonucleosides
  • Viral Proteins
  • 5-ethynyl-1-ribofuranosylimidazole-4-carboxamide
  • Ribavirin
  • Hydrolases
  • Adenosylhomocysteinase