Heterocyclic thrombin inhibitors. Part 2: quinoxalinone derivatives as novel, potent antithrombotic agents.
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.
Ries
Uwe J
UJ
Department of Chemical Research, Boehringer Ingelheim Pharma KG, Birkendorfer Strasse 65, D-88397, Biberach/Riss, Germany. uwe.ries@bc.boehringer-ingelheim.com
Priepke
Henning W M
HW
Hauel
Norbert H
NH
Handschuh
Sandra
S
Mihm
Gerhard
G
Stassen
Jean M
JM
Wienen
Wolfgang
W
Nar
Herbert
H
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
D065427:Factor Xa Inhibitors; D005343:Fibrinolytic Agents; D011810:Quinoxalines; D014361:Trypsin Inhibitors; D013917:Thrombin; D005341:Fibrinolysin