Activity of Mannich bases of 7-hydroxycoumarin against Flaviviridae

Bioorg Med Chem. 2008 Mar 1;16(5):2591-605. doi: 10.1016/j.bmc.2007.11.045. Epub 2007 Nov 22.

Abstract

Some Mannich bases of 7-hydroxycoumarin (2) and their simple derivatives (3 and 4) were prepared and tested against viruses containing single-stranded, positive-sense RNA genomes (ssRNA(+)). This study was directed toward Flaviviridae and, in particular, HCV surrogate viruses (BVDV, YFV). The 7-hydroxy derivatives 2 were generally devoid of activity, but when position 7 was propylated, the resulting 7-propyloxy derivatives 3 were in some cases endowed with an interesting activity against BVDV. The formation of 7-benzoyl derivatives 4 gave compounds generally lacking in activity against Flaviviridae, whereas the appearance of activity against RSV has been observed. Also some unsymmetrical methylene derivatives 5-7 (namely coumarins bridged to chromones or indoles) were found moderately active in antiviral tests. Derivatives 3 were submitted to a molecular modeling study using DNA polymerase of HCV as a target. The good correlation between calculated molecular modeling IC(50) and experimental EC(50) indicates that DNA polymerase is potentially involved in the inhibition of surrogate HCV viruses.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antiviral Agents / chemical synthesis*
  • Antiviral Agents / chemistry
  • Antiviral Agents / pharmacology*
  • Binding Sites
  • Cell Line
  • Cell Survival / drug effects
  • Cricetinae
  • Dogs
  • Flaviviridae / chemistry
  • Flaviviridae / drug effects*
  • Flaviviridae / metabolism
  • Humans
  • Mannich Bases / chemistry
  • Models, Molecular
  • Molecular Structure
  • Protein Binding
  • Structure-Activity Relationship
  • Umbelliferones / chemical synthesis*
  • Umbelliferones / chemistry
  • Umbelliferones / pharmacology*
  • Viral Nonstructural Proteins / chemistry
  • Viral Nonstructural Proteins / metabolism

Substances

  • Antiviral Agents
  • Mannich Bases
  • Umbelliferones
  • Viral Nonstructural Proteins