title: Design, synthesis, and in vitro biological activity of indole-based factor Xa inhibitors.
abstract: A series of indole and carbazole based inhibitors of factor Xa (FXa) has been investigated. The most potent compound inhibits FXa with a Ki of 0.2 nM and has 900- and 750-fold selectivity over thrombin and trypsin, respectively.
authors.affiliation: Discovery Research, Berlex Biosciences, Richmond, CA 94804, USA. damian_arnaiz@berlex.com
authors.forename: D O
authors.initials: DO
authors.lastname: Arnaiz
authors.forename: Z
authors.initials: Z
authors.lastname: Zhao
authors.forename: A
authors.initials: A
authors.lastname: Liang
authors.forename: L
authors.initials: L
authors.lastname: Trinh
authors.forename: M
authors.initials: M
authors.lastname: Witlow
authors.forename: S K
authors.initials: SK
authors.lastname: Koovakkat
authors.forename: K J
authors.initials: KJ
authors.lastname: Shaw
mesh_terms: D000578:Amidines / Q000737:chemistry*; D000925:Anticoagulants / Q000138:chemical synthesis* / Q000494:pharmacology*; D002227:Carbazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D055598:Chemical Phenomena; D002627:Chemistry, Physical; D018360:Crystallography, X-Ray; D065427:Factor Xa Inhibitors; D006801:Humans; D007211:Indoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D008958:Models, Molecular; D008968:Molecular Conformation; D011725:Pyridines / Q000737:chemistry*; D013329:Structure-Activity Relationship; D013917:Thrombin / Q000037:antagonists & inhibitors; D014361:Trypsin Inhibitors / Q000138:chemical synthesis / Q000494:pharmacology
chemical_list: D000578:Amidines; D000925:Anticoagulants; D002227:Carbazoles; D065427:Factor Xa Inhibitors; D007211:Indoles; D011725:Pyridines; D014361:Trypsin Inhibitors; C114592:Fidexaban; D013917:Thrombin