title: Solid-phase parallel synthesis of azarene pyrrolidinones as factor Xa inhibitors.
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.
authors.affiliation: Department of Medicinal Chemistry, Rhone-Poulenc Rorer, Collegeville, PA 19426, USA.
authors.forename: Y
authors.initials: Y
authors.lastname: Gong
authors.forename: M
authors.initials: M
authors.lastname: Becker
authors.forename: Y M
authors.initials: YM
authors.lastname: Choi-Sledeski
authors.forename: R S
authors.initials: RS
authors.lastname: Davis
authors.forename: J M
authors.initials: JM
authors.lastname: Salvino
authors.forename: V
authors.initials: V
authors.lastname: Chu
authors.forename: K D
authors.initials: KD
authors.lastname: Brown
authors.forename: H W
authors.initials: HW
authors.lastname: Pauls
mesh_terms: D000925:Anticoagulants / Q000138:chemical synthesis* / Q000378:metabolism / Q000494:pharmacology*; D020650:Combinatorial Chemistry Techniques; D065427:Factor Xa Inhibitors; D011760:Pyrrolidinones / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology; D013329:Structure-Activity Relationship
chemical_list: D000925:Anticoagulants; D065427:Factor Xa Inhibitors; D011760:Pyrrolidinones