1.
Bioorg Med Chem Lett
; 16(14): 3829-32, 2006 Jul 15.
Article
in English
| MEDLINE
| ID: mdl-16650987
ABSTRACT
Efforts toward developing orally bioavailable factor VIIa inhibitors starting from parenteral lead compound 1 are described. SAR resulted in improved physicochemical properties, leading to enhanced oral absorption in rat.
Subject(s)
Anticoagulants/chemical synthesis , Anticoagulants/pharmacology , Factor VIIa/antagonists & inhibitors , Thrombosis/drug therapy , Administration, Oral , Animals , Biological Availability , Rats , Structure-Activity Relationship , Thrombin/antagonists & inhibitors
2.
Bioorg Med Chem Lett
; 16(8): 2270-3, 2006 Apr 15.
Article
in English
| MEDLINE
| ID: mdl-16460932
ABSTRACT
Structure-activity relationships and binding mode of novel heterocyclic factor VIIa inhibitors will be described. In these inhibitors, a highly basic 5-amidinoindole moiety has been successfully replaced with a less basic 5-aminopyrrolo[3,2-b]pyridine scaffold.
