Discovery of novel heterocyclic factor VIIa inhibitors.
Structure-activity relationships and binding mode of novel heterocyclic factor VIIa inhibitors will be described. In these inhibitors, a highly basic 5-amidinoindole moiety has been successfully replaced with a less basic 5-aminopyrrolo[3,2-b]pyridine scaffold.
Rai
Roopa
R
Celera, 180 Kimball Way, South San Francisco, CA 94080, USA. roopa.rai@hotmail.com
Kolesnikov
Aleksandr
A
Sprengeler
Paul A
PA
Torkelson
Steven
S
Ton
Tony
T
Katz
Bradley A
BA
Yu
Christine
C
Hendrix
John
J
Shrader
William D
WD
Stephens
Robin
R
Cabuslay
Ronnell
R
Sanford
Ellen
E
Young
Wendy B
WB
D000631:Aminopyridines / Q000737:chemistry* / Q000494:pharmacology; D001665:Binding Sites; D018360:Crystallography, X-Ray; D015195:Drug Design; D015942:Factor VIIa / Q000037:antagonists & inhibitors*; D005343:Fibrinolytic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D006571:Heterocyclic Compounds / Q000138:chemical synthesis* / Q000494:pharmacology; D006801:Humans; D013329:Structure-Activity Relationship; D013925:Thromboplastin / Q000037:antagonists & inhibitors*
D000631:Aminopyridines; D005343:Fibrinolytic Agents; D006571:Heterocyclic Compounds; D013925:Thromboplastin; D015942:Factor VIIa