HCV NS5B polymerase inhibitors 3: Synthesis and in vitro activity of 3-(1,1-dioxo-2H-[1,2,4]benzothiadiazin-3-yl)-4-hydroxy-2H-quinolizin-2-one derivatives

Bioorg Med Chem Lett. 2009 Aug 1;19(15):4484-7. doi: 10.1016/j.bmcl.2009.05.021. Epub 2009 May 9.

Abstract

3-(1,1-Dioxo-2H-[1,2,4]benzothiadiazin-3-yl)-4-hydroxy-2H-quinolizin-2-one derivatives as potential anti-HCV drugs targeting NS5B polymerase have been investigated. Their synthesis, HCV NS5B polymerase inhibition, and replicon activity are discussed.

MeSH terms

  • Animals
  • Antiviral Agents / chemical synthesis*
  • Antiviral Agents / pharmacology
  • Benzothiadiazines / chemical synthesis*
  • Benzothiadiazines / pharmacology
  • Chemistry, Pharmaceutical / methods
  • Drug Design
  • Enzyme Inhibitors / chemical synthesis*
  • Enzyme Inhibitors / pharmacology
  • Hepacivirus / metabolism
  • Hepatitis C / drug therapy*
  • In Vitro Techniques
  • Inhibitory Concentration 50
  • Magnetic Resonance Spectroscopy
  • Models, Chemical
  • Molecular Structure
  • Quinolizines / chemical synthesis*
  • Quinolizines / pharmacology
  • Structure-Activity Relationship
  • Viral Nonstructural Proteins / antagonists & inhibitors*
  • Viral Nonstructural Proteins / chemistry

Substances

  • Antiviral Agents
  • Benzothiadiazines
  • Enzyme Inhibitors
  • Quinolizines
  • Viral Nonstructural Proteins
  • NS-5 protein, hepatitis C virus