Development of potent and selective factor Xa inhibitors.
The development of potent and selective small molecule inhibitors of factor Xa is described.
Rai
R
R
Departments of Medicinal Chemistry, Structural Chemistry and Enzymology, Axys Pharmaceuticals, Inc., 385 Oyster Point Blvd., 94080, South San Francisco, CA, USA.
Kolesnikov
A
A
Li
Y
Y
Young
W B
WB
Leahy
E
E
Sprengeler
P A
PA
Verner
E
E
Shrader
W D
WD
Burgess-Henry
J
J
Sangalang
J C
JC
Allen
D
D
Chen
X
X
Katz
B A
BA
Luong
C
C
Elrod
K
K
Cregar
L
L
D000578:Amidines / Q000737:chemistry / Q000494:pharmacology*; D000990:Antithrombin III / Q000138:chemical synthesis* / Q000494:pharmacology*; D003461:Crystallography; D015195:Drug Design; D004791:Enzyme Inhibitors / Q000737:chemistry / Q000494:pharmacology; D005341:Fibrinolysin / Q000187:drug effects; D007211:Indoles / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D013917:Thrombin / Q000187:drug effects*; D014357:Trypsin / Q000187:drug effects; D014568:Urokinase-Type Plasminogen Activator / Q000187:drug effects*
C433825:2-(3-bromo-2-hydroxy-5-methylphenyl)-1H-indole-5-carboxamidine; D000578:Amidines; D004791:Enzyme Inhibitors; D007211:Indoles; D000990:Antithrombin III; D014357:Trypsin; D013917:Thrombin; D005341:Fibrinolysin; D014568:Urokinase-Type Plasminogen Activator