Discovery of 3-amino-4-chlorophenyl P1 as a novel and potent benzamidine mimic via solid-phase synthesis of an isoxazoline library

Bioorg Med Chem Lett. 2003 May 19;13(10):1795-9. doi: 10.1016/s0960-894x(03)00130-6.

Abstract

In an effort to identify orally bioavailable factor Xa inhibitors, two isoxazolines libraries were prepared to scan for novel P1 ligands. From this work, 4-chloro-3-aniline was identified as a novel and potent benzamidine mimic.

MeSH terms

  • Animals
  • Benzamidines / chemistry
  • Combinatorial Chemistry Techniques*
  • Enzyme Inhibitors / chemical synthesis
  • Factor Xa Inhibitors*
  • Humans
  • Isoxazoles / chemical synthesis*
  • Isoxazoles / pharmacology
  • Molecular Mimicry
  • Structure-Activity Relationship

Substances

  • Benzamidines
  • Enzyme Inhibitors
  • Factor Xa Inhibitors
  • Isoxazoles
  • benzamidine