1.
Bioorg Med Chem Lett
; 11(14): 1797-800, 2001 Jul 23.
Article
in English
| MEDLINE
| ID: mdl-11459634
ABSTRACT
The development of potent and selective small molecule inhibitors of factor Xa is described.
Subject(s)
Amidines/pharmacology , Antithrombin III/chemical synthesis , Antithrombin III/pharmacology , Indoles/pharmacology , Thrombin/drug effects , Urokinase-Type Plasminogen Activator/drug effects , Amidines/chemistry , Crystallography , Drug Design , Enzyme Inhibitors/chemistry , Enzyme Inhibitors/pharmacology , Fibrinolysin/drug effects , Indoles/chemistry , Structure-Activity Relationship , Trypsin/drug effects
2.
Bioorg Med Chem Lett
; 11(14): 1801-4, 2001 Jul 23.
Article
in English
| MEDLINE
| ID: mdl-11459635
ABSTRACT
A neutral inhibitor of the serine protease factor Xa was identified via a high-throughput screen of a commercial library. The initial lead 1 demonstrated reversible and competitive inhibition kinetics for factor Xa and possessed a high degree of selectivity versus other related serine proteases. Initial modeling efforts and the generation of a series of analogues of 1 are described.
