Design, synthesis, and SAR of amino acid derivatives as factor Xa inhibitors

Bioorg Med Chem Lett. 2001 Nov 19;11(22):2947-50. doi: 10.1016/s0960-894x(01)00585-6.

Abstract

A series of potent and selective factor Xa inhibitors was synthesized using various readily available amino acids as central templates. The most potent compound displays IC(50) of 3 nM.

MeSH terms

  • Drug Design
  • Factor Xa Inhibitors*
  • Inhibitory Concentration 50
  • Models, Molecular
  • Serine Proteinase Inhibitors / chemical synthesis
  • Serine Proteinase Inhibitors / chemistry
  • Serine Proteinase Inhibitors / pharmacology*
  • Structure-Activity Relationship

Substances

  • Factor Xa Inhibitors
  • Serine Proteinase Inhibitors