The design of phenylglycine containing benzamidine carboxamides as potent and selective inhibitors of factor Xa.
Factor Xa, a critical serine protease in the blood coagulation cascade, has become a target for inhibition as a strategy for the invention of novel anti-thrombotic agents. Here we describe the development of phenylglycine containing benzamidine carboxamides as novel, potent and selective inhibitors of factor Xa.
Jones
S D
SD
Prosthetics Molecular Design, Beechfield House, Macclesfield, UK. stuart.jones@protherics.com
Liebeschuetz
J W
JW
Morgan
P J
PJ
Murray
C W
CW
Rimmer
A D
AD
Roscoe
J M
JM
Waszkowycz
B
B
Welsh
P M
PM
Wylie
W A
WA
Young
S C
SC
Martin
H
H
Mahler
J
J
Brady
L
L
Wilkinson
K
K
D001550:Benzamidines / Q000737:chemistry* / Q000494:pharmacology; D001665:Binding Sites; D020650:Combinatorial Chemistry Techniques; D018360:Crystallography, X-Ray; D015195:Drug Design; D015951:Factor Xa / Q000378:metabolism; D065427:Factor Xa Inhibitors; D005998:Glycine / Q000031:analogs & derivatives / Q000737:chemistry* / Q000494:pharmacology*; D008958:Models, Molecular; D015394:Molecular Structure; D017434:Protein Structure, Tertiary; D012984:Software
D001550:Benzamidines; D065427:Factor Xa Inhibitors; C008852:2-phenylglycine; D015951:Factor Xa; D005998:Glycine