Novel 3-carboxamide-coumarins as potent and selective FXIIa inhibitors.
Recently, FXIIa was highlighted as an original attractive target for the development of new anticoagulant drugs with low rates of therapy-related hemorrhages. In this work, we describe the development of a new series of 3-carboxamide-coumarins that are the first potent and selective nonpeptidic inhibitors of FXIIa.
Robert
Séverine
S
Department of Pharmacy, Drug Design and Discovery Center, FUNDP, University of Namur, Namur, Belgium.
Bertolla
Carine
C
Masereel
Bernard
B
Dogné
Jean-Michel
JM
Pochet
Lionel
L
D000577:Amides / Q000138:chemical synthesis* / Q000737:chemistry; D000925:Anticoagulants / Q000138:chemical synthesis* / Q000737:chemistry; D003374:Coumarins / Q000138:chemical synthesis* / Q000737:chemistry; D015956:Factor XIIa / Q000037:antagonists & inhibitors* / Q000737:chemistry; D013329:Structure-Activity Relationship
D000577:Amides; D000925:Anticoagulants; D003374:Coumarins; D015956:Factor XIIa