Identification of 4H,6H-[2]benzoxepino[4,5-c][1,2]oxazoles as novel squalene synthase inhibitors

Bioorg Med Chem Lett. 2011 Jun 15;21(12):3648-53. doi: 10.1016/j.bmcl.2011.04.092. Epub 2011 Apr 29.

Abstract

Novel squalene synthase inhibitors are disclosed. The design, synthesis, SAR and pharmacological profile of the compounds are discussed.

MeSH terms

  • Binding Sites
  • Crystallography, X-Ray
  • Drug Design*
  • Enzyme Activation / drug effects
  • Enzyme Inhibitors / chemistry*
  • Enzyme Inhibitors / pharmacology*
  • Farnesyl-Diphosphate Farnesyltransferase / antagonists & inhibitors*
  • Inhibitory Concentration 50
  • Molecular Structure
  • Oxazoles / chemistry*
  • Oxazoles / pharmacology*
  • Structure-Activity Relationship

Substances

  • Enzyme Inhibitors
  • Oxazoles
  • Farnesyl-Diphosphate Farnesyltransferase