An analogue of AICAR with dual inhibitory activity against WNV and HCV NTPase/helicase: synthesis and in vitro screening of 4-carbamoyl-5-(4,6-diamino-2,5-dihydro-1,3,5-triazin-2-yl)imidazole-1-beta-D-ribofuranoside

Bioorg Med Chem Lett. 2007 Apr 15;17(8):2285-8. doi: 10.1016/j.bmcl.2007.01.074. Epub 2007 Jan 27.

Abstract

The title compound (4) was synthesized by the reaction of ethyl 1-(2,3,5-tri-O-benzoyl-beta-d-ribofuranosyl)-5-formylimidazole-4-carboxylate with excess guanidine in ethanol at reflux. Compound 4 was evaluated in vitro against NTPases/helicases of four different viruses of the Flaviviridae family, including the West Nile virus (WNV), hepatitis C virus (HCV), dengue virus (DENV), and the Japanese encephalitis virus (JEV), employing both an RNA and a DNA substrate. The compound showed activity against NTPase/helicase of WNV and HCV with an IC(50) of 23 and 37 microM, respectively, when a DNA substrate was employed, while no activity was observed when an RNA substrate was used. There was no activity against the NTPase/helicase of either DENV or JEV irrespective of whether an RNA or a DNA substrate was employed. Considering that Flaviviridae are RNA viruses, the observed absence of activity against an RNA substrate, but the presence of activity against a DNA substrate is intriguing and somewhat surprising. The preliminary studies show that compound 4 does not form a tight complex with either an RNA or a DNA substrate, suggesting that its mechanism of action may involve direct interaction with the enzyme.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Aminoimidazole Carboxamide / analogs & derivatives
  • Aminoimidazole Carboxamide / chemistry
  • Aminoimidazole Carboxamide / pharmacology
  • Antiviral Agents / chemical synthesis*
  • Antiviral Agents / pharmacology
  • Flaviviridae
  • Hepacivirus / drug effects*
  • Hepacivirus / enzymology
  • Humans
  • Inhibitory Concentration 50
  • Nucleoside-Triphosphatase / antagonists & inhibitors*
  • RNA Helicases / antagonists & inhibitors*
  • Ribonucleosides / chemistry*
  • Ribonucleosides / pharmacology
  • Ribonucleotides / chemistry
  • Ribonucleotides / pharmacology
  • West Nile virus / drug effects*
  • West Nile virus / enzymology

Substances

  • Antiviral Agents
  • Ribonucleosides
  • Ribonucleotides
  • Aminoimidazole Carboxamide
  • Nucleoside-Triphosphatase
  • RNA Helicases
  • AICA ribonucleotide