Novel factor Xa inhibitors based on a 2-carboxyindole scaffold: SAR of P4 substituents in combination with a neutral P1 ligand.
Bioorg Med Chem Lett
; 14(16): 4197-201, 2004 Aug 16.
Article
en En
| MEDLINE
| ID: mdl-15261269
ABSTRACT
A series of novel, highly potent 2-carboxyindole-based factor Xa inhibitors is described. Structural requirements for P4 ligands in combination with a neutral biaryl P1 ligand were investigated with the 2-carboxyindole scaffold. A diverse set of P4 substituents was identified, which, in conjunction with a biaryl P1 ligand, gave highly potent factor Xa inhibitors, which were also selective versus other proteases and efficacious in various antithrombotic secondary assays.
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Colección:
01-internacional
Base de datos:
MEDLINE
Asunto principal:
Inhibidores de Serina Proteinasa
/
Inhibidores del Factor Xa
/
Indoles
Tipo de estudio:
Prognostic_studies
Idioma:
En
Revista:
Bioorg Med Chem Lett
Asunto de la revista:
BIOQUIMICA
/
QUIMICA
Año:
2004
Tipo del documento:
Article
País de afiliación:
Alemania