Efforts toward oral bioavailability in factor VIIa inhibitors

Bioorg Med Chem Lett. 2006 Jul 15;16(14):3829-32. doi: 10.1016/j.bmcl.2006.04.018. Epub 2006 May 2.

Abstract

Efforts toward developing orally bioavailable factor VIIa inhibitors starting from parenteral lead compound 1 are described. SAR resulted in improved physicochemical properties, leading to enhanced oral absorption in rat.

MeSH terms

  • Administration, Oral
  • Animals
  • Anticoagulants / chemical synthesis*
  • Anticoagulants / pharmacology*
  • Biological Availability
  • Factor VIIa / antagonists & inhibitors*
  • Rats
  • Structure-Activity Relationship
  • Thrombin / antagonists & inhibitors
  • Thrombosis / drug therapy*

Substances

  • Anticoagulants
  • Factor VIIa
  • Thrombin