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

Bioorg Med Chem Lett. 2009 Aug 1;19(15):4476-9. doi: 10.1016/j.bmcl.2009.05.063. Epub 2009 May 23.

Abstract

2-(1,1-Dioxo-2H-[1,2,4]benzothiadiazin-3-yl)-1-hydroxynaphthalene 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*
  • Humans
  • In Vitro Techniques
  • Inhibitory Concentration 50
  • Magnetic Resonance Spectroscopy
  • Models, Chemical
  • Molecular Structure
  • Naphthalenes / antagonists & inhibitors*
  • Naphthalenes / chemistry
  • Naphthols / chemical synthesis*
  • Naphthols / pharmacology
  • Structure-Activity Relationship
  • Viral Nonstructural Proteins / antagonists & inhibitors*

Substances

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