Solid-phase parallel synthesis of azarene pyrrolidinones as factor Xa inhibitors

Bioorg Med Chem Lett. 2000 May 15;10(10):1033-6. doi: 10.1016/s0960-894x(00)00151-7.

Abstract

A focused library (4 x 14) prepared from 4-aminopyridine and 4-, 5-, and 6-azoindole templates was synthesized using 14 polymer supported 4-amido-2,3,5,6-tetrafluorophenyl (TFP) sulfonate esters inputs. Several compounds were identified as factor Xa inhibitors (IC50< or =0.1 microM) helping to establish the SAR among these four series of azarene pyrrolidinones.

MeSH terms

  • Anticoagulants / chemical synthesis*
  • Anticoagulants / metabolism
  • Anticoagulants / pharmacology*
  • Combinatorial Chemistry Techniques*
  • Factor Xa Inhibitors*
  • Pyrrolidinones / chemistry*
  • Pyrrolidinones / metabolism
  • Pyrrolidinones / pharmacology
  • Structure-Activity Relationship

Substances

  • Anticoagulants
  • Factor Xa Inhibitors
  • Pyrrolidinones