Studies towards the identification of potent, selective and bioavailable thrombin inhibitors.
The application of selection criteria, based on potency and physicochemical parameters, to a candidate library of thrombin inhibitors is described. The utility of the approach is exemplified by the discovery of a potent, selective and bioavailable thrombin inhibitor 62.
Ambler
J
J
Novartis Horsham Research Center, West Sussex.
Baker
E
E
Bentley
D
D
Brown
L
L
Butler
K
K
Butler
P
P
Farr
D
D
Dunnet
K
K
Le Grand
D
D
Hayler
J
J
Janus
D
D
Jones
D
D
Menear
K
K
Mercer
M
M
Smith
G
G
Talbot
M
M
Tweed
M
M
D000925:Anticoagulants / Q000302:isolation & purification / Q000493:pharmacokinetics / Q000494:pharmacology*; D001682:Biological Availability; D013329:Structure-Activity Relationship; D013917:Thrombin / Q000037:antagonists & inhibitors*
D000925:Anticoagulants; D013917:Thrombin