Selective and orally bioavailable phenylglycine tissue factor/factor VIIa inhibitors

Bioorg Med Chem Lett. 2005 Dec 1;15(23):5344-52. doi: 10.1016/j.bmcl.2005.04.079. Epub 2005 Oct 4.

Abstract

We describe the structure-based design and synthesis of highly potent, orally bioavailable tissue factor/factor VIIa inhibitors which interfere with the coagulation cascade by selective inhibition of the extrinsic pathway.

MeSH terms

  • Administration, Oral
  • Animals
  • Anticoagulants / chemical synthesis
  • Anticoagulants / chemistry*
  • Anticoagulants / pharmacology*
  • Biological Availability
  • Crystallography, X-Ray
  • Drug Design
  • Factor VIIa / antagonists & inhibitors*
  • Glycine / analogs & derivatives
  • Glycine / chemistry
  • Humans
  • Molecular Structure
  • Rats
  • Serine Proteinase Inhibitors / chemical synthesis
  • Serine Proteinase Inhibitors / chemistry*
  • Serine Proteinase Inhibitors / pharmacology*
  • Thromboplastin / antagonists & inhibitors*

Substances

  • Anticoagulants
  • Serine Proteinase Inhibitors
  • 2-phenylglycine
  • Thromboplastin
  • Factor VIIa
  • Glycine