Structure-based macrocyclization yields hepatitis C virus NS5B inhibitors with improved binding affinities and pharmacokinetic properties

Angew Chem Int Ed Engl. 2012 May 7;51(19):4637-40. doi: 10.1002/anie.201200110. Epub 2012 Mar 30.
No abstract available

MeSH terms

  • Administration, Oral
  • Animals
  • Binding Sites
  • Crystallography, X-Ray
  • Cyclization
  • Dogs
  • Enzyme Inhibitors / chemistry
  • Enzyme Inhibitors / pharmacokinetics*
  • Hepacivirus / metabolism*
  • Indoles / chemistry
  • Male
  • Protein Structure, Tertiary
  • Rats
  • Rats, Sprague-Dawley
  • Viral Nonstructural Proteins / antagonists & inhibitors*
  • Viral Nonstructural Proteins / metabolism

Substances

  • Enzyme Inhibitors
  • Indoles
  • Viral Nonstructural Proteins
  • indole
  • NS-5 protein, hepatitis C virus