Identification and optimization of tetrahydro-2H-3-benzazepin-2-ones as squalene synthase inhibitors

Bioorg Med Chem Lett. 2011 Apr 15;21(8):2554-8. doi: 10.1016/j.bmcl.2011.02.004. Epub 2011 Feb 17.

Abstract

Novel squalene synthase inhibitors are disclosed. SAR and pharmacological profile of selected compounds are discussed.

MeSH terms

  • Animals
  • Benzazepines / chemical synthesis
  • Benzazepines / chemistry*
  • Benzazepines / pharmacokinetics
  • Crystallography, X-Ray
  • Enzyme Inhibitors / chemical synthesis
  • Enzyme Inhibitors / chemistry*
  • Enzyme Inhibitors / pharmacokinetics
  • Farnesyl-Diphosphate Farnesyltransferase / antagonists & inhibitors*
  • Farnesyl-Diphosphate Farnesyltransferase / metabolism
  • Humans
  • Mice
  • Microsomes, Liver / metabolism
  • Molecular Conformation
  • Stereoisomerism
  • Structure-Activity Relationship

Substances

  • Benzazepines
  • Enzyme Inhibitors
  • Farnesyl-Diphosphate Farnesyltransferase