Synthesis and biological activity of a novel squalene epoxidase inhibitor, FR194738

Bioorg Med Chem Lett. 2004 Feb 9;14(3):633-7. doi: 10.1016/j.bmcl.2003.11.072.

Abstract

The synthesis and biological properties of a novel squalene epoxidase inhibitor, FR194738, are described. This compound displayed potent in vitro inhibitory activities against squalene epoxidase and cholesterol synthesis, and lowered plasma cholesterol and triglyceride levels in dogs.

MeSH terms

  • Animals
  • Benzylamines / chemical synthesis*
  • Benzylamines / pharmacology*
  • Cholesterol / blood*
  • Dogs
  • Enzyme Inhibitors / chemical synthesis*
  • Enzyme Inhibitors / pharmacology*
  • Humans
  • In Vitro Techniques
  • Microsomes, Liver / enzymology*
  • Oxygenases / antagonists & inhibitors*
  • Rats
  • Squalene Monooxygenase
  • Structure-Activity Relationship
  • Triglycerides / blood*
  • Tumor Cells, Cultured

Substances

  • Benzylamines
  • Enzyme Inhibitors
  • FR 194738
  • Triglycerides
  • Cholesterol
  • Oxygenases
  • Squalene Monooxygenase