Potent 4-amino-5-azaindole factor VIIa inhibitors.
The 4-amino-5-azaindole as an amidino-benzimidazole replacement is described. A series of potent and selective analogs were discovered and showed desirable ex vivo efficacy as measured by PT.
Hu
Huiyong
H
Celera Genomics, South San Francisco, CA 94080, USA. huiyong.hu@yahoo.com
Kolesnikov
Aleksandr
A
Riggs
Jennifer R
JR
Wesson
Kieron E
KE
Stephens
Robin
R
Leahy
Ellen M
EM
Shrader
William D
WD
Sprengeler
Paul A
PA
Green
Michael J
MJ
Sanford
Ellen
E
Nguyen
Margaret
M
Gjerstad
Erik
E
Cabuslay
Ronnel
R
Young
Wendy B
WB
D015942:Factor VIIa / Q000037:antagonists & inhibitors* / Q000378:metabolism; D007211:Indoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D015394:Molecular Structure; D011725:Pyridines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship
D007211:Indoles; D011725:Pyridines; D015942:Factor VIIa