title: Heterocyclic thrombin inhibitors. Part 2: quinoxalinone derivatives as novel, potent antithrombotic agents.
abstract: Quinoxalinone derivatives as prototypes of dual thrombin and factor Xa inhibitors have been discovered. Nanomolar inhibition of both coagulation enzymes resulted in very potent antithrombotic activity in vitro.
authors.affiliation: Department of Chemical Research, Boehringer Ingelheim Pharma KG, Birkendorfer Strasse 65, D-88397, Biberach/Riss, Germany. uwe.ries@bc.boehringer-ingelheim.com
authors.forename: Uwe J
authors.initials: UJ
authors.lastname: Ries
authors.forename: Henning W M
authors.initials: HW
authors.lastname: Priepke
authors.forename: Norbert H
authors.initials: NH
authors.lastname: Hauel
authors.forename: Sandra
authors.initials: S
authors.lastname: Handschuh
authors.forename: Gerhard
authors.initials: G
authors.lastname: Mihm
authors.forename: Jean M
authors.initials: JM
authors.lastname: Stassen
authors.forename: Wolfgang
authors.initials: W
authors.lastname: Wienen
authors.forename: Herbert
authors.initials: H
authors.lastname: Nar
mesh_terms: D000818:Animals; D001777:Blood Coagulation / Q000187:drug effects; D018360:Crystallography, X-Ray; D065427:Factor Xa Inhibitors; D005341:Fibrinolysin / Q000037:antagonists & inhibitors; D005343:Fibrinolytic Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D008958:Models, Molecular; D008968:Molecular Conformation; D010314:Partial Thromboplastin Time; D011810:Quinoxalines / Q000138:chemical synthesis* / Q000494:pharmacology*; D051381:Rats; D013329:Structure-Activity Relationship; D013917:Thrombin / Q000037:antagonists & inhibitors*; D014361:Trypsin Inhibitors / Q000138:chemical synthesis / Q000494:pharmacology
chemical_list: D065427:Factor Xa Inhibitors; D005343:Fibrinolytic Agents; D011810:Quinoxalines; D014361:Trypsin Inhibitors; D013917:Thrombin; D005341:Fibrinolysin