Design, synthesis, and SAR of amino acid derivatives as factor Xa inhibitors.
A series of potent and selective factor Xa inhibitors was synthesized using various readily available amino acids as central templates. The most potent compound displays IC(50) of 3 nM.
Su
T
T
COR Therapeutics, Inc., 256 East Grand Avenue, South San Francisco, CA 94080, USA. tsu@corr.com
Wu
Y
Y
Doughan
B
B
Jia
Z J
ZJ
Woolfrey
J
J
Huang
B
B
Wong
P
P
Park
G
G
Sinha
U
U
Scarborough
R M
RM
Zhu
B Y
BY
D015195:Drug Design; D065427:Factor Xa Inhibitors; D020128:Inhibitory Concentration 50; D008958:Models, Molecular; D015842:Serine Proteinase Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship
D065427:Factor Xa Inhibitors; D015842:Serine Proteinase Inhibitors