1.
Bioorg Med Chem Lett
; 16(12): 3197-200, 2006 Jun 15.
Article
in English
| MEDLINE
| ID: mdl-16621549
ABSTRACT
The discovery and development of 5-azaindole factor VIIa inhibitors will be described.
Subject(s)
Aza Compounds/chemical synthesis , Aza Compounds/pharmacology , Factor VIIa/antagonists & inhibitors , Indoles/chemical synthesis , Indoles/pharmacology , Aza Compounds/chemistry , Crystallography, X-Ray , Factor VIIa/chemistry , Factor VIIa/metabolism , Indoles/chemistry , Models, Molecular , Molecular Structure , Structure-Activity Relationship
2.
Bioorg Med Chem Lett
; 16(10): 2796-9, 2006 May 15.
Article
in English
| MEDLINE
| ID: mdl-16487703
ABSTRACT
Synthesis and biological data of a novel selective and efficacious factor IXa inhibitor are described along with its crystal structure in factor VIIa.
Subject(s)
Factor IXa/antagonists & inhibitors , Pyrazoles/pharmacology , Serine Proteinase Inhibitors/pharmacology , Factor IXa/chemistry , Humans , Models, Molecular
3.
Bioorg Med Chem Lett
; 16(3): 710-3, 2006 Feb.
Article
in English
| MEDLINE
| ID: mdl-16257204
ABSTRACT
Inhibition of coagulation proteases such as thrombin, fXa, and fVIIa has been a focus of ongoing research to produce safe and effective antithrombotic agents. Herein, we describe a unique zinc-mediated chelation strategy to streamline the discovery of potent inhibitors of fIIa, fXa, and fVIIa. SAR studies that led to the development of selective inhibitors of fXa will also be detailed.
Subject(s)
Anticoagulants/chemistry , Blood Coagulation/drug effects , Chelating Agents/chemistry , Protease Inhibitors/chemical synthesis , Zinc/chemistry , Anticoagulants/pharmacology , Blood Coagulation/physiology , Crystallography, X-Ray , Factor VII/antagonists & inhibitors , Factor Xa Inhibitors , Protease Inhibitors/pharmacology , Structure-Activity Relationship , Thrombin/antagonists & inhibitors
4.
Retina
; 24(3): 458-9, 2004 Jun.
Article
in English
| MEDLINE
| ID: mdl-15187673
