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Solid-phase parallel synthesis of azarene pyrrolidinones as factor Xa inhibitors
Y Gong1, M Becker, Y M Choi-Sledeski
1Department of Medicinal Chemistry, Rhone-Poulenc Rorer, Collegeville, PA 19426, USA.
Bioorganic & Medicinal Chemistry Letters
|June 8, 2000
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.