title: Solid-phase synthesis of naphthylamidines as factor VIIa/tissue factor inhibitors.
abstract: Reductive amination followed by acylation of polymer-linked formyl aryl amidines generate combinatorial libraries of aryl amidines 8-13. Potent small molecule naphthylamidine inhibitors 12 (Ki<100 nM) of FVIIa/TF have been discovered and their activity against other serine proteases in the coagulation cascade is reported.
authors.affiliation: Berlex Biosciences, 2600 Hilltop Drive, Richmond, CA 94804, USA. brad_buckman@berlex.com
authors.forename: Brad O
authors.initials: BO
authors.lastname: Buckman
authors.forename: Yuo-Ling
authors.initials: YL
authors.lastname: Chou
authors.forename: Meg
authors.initials: M
authors.lastname: McCarrick
authors.forename: Amy
authors.initials: A
authors.lastname: Liang
authors.forename: Dao
authors.initials: D
authors.lastname: Lentz
authors.forename: Raju
authors.initials: R
authors.lastname: Mohan
authors.forename: Michael M
authors.initials: MM
authors.lastname: Morrissey
authors.forename: Kenneth J
authors.initials: KJ
authors.lastname: Shaw
authors.forename: Lan
authors.initials: L
authors.lastname: Trinh
authors.forename: David R
authors.initials: DR
authors.lastname: Light
mesh_terms: D000578:Amidines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D001665:Binding Sites; D015942:Factor VIIa / Q000037:antagonists & inhibitors*; D006801:Humans; D007700:Kinetics; D008958:Models, Molecular; D008968:Molecular Conformation; D009284:Naphthols / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D013329:Structure-Activity Relationship; D013925:Thromboplastin / Q000037:antagonists & inhibitors*
chemical_list: D000578:Amidines; D009284:Naphthols; D013925:Thromboplastin; D015942:Factor VIIa