Phenyltriazolinones as potent factor Xa inhibitors.
Bioorg Med Chem Lett
; 20(4): 1373-7, 2010 Feb 15.
Article
en En
| MEDLINE
| ID: mdl-20100660
ABSTRACT
We have discovered that phenyltriazolinone is a novel and potent P1 moiety for coagulation factor Xa. X-ray structures of the inhibitors with a phenyltriazolinone in the P1 position revealed that the side chain of Asp189 has reoriented resulting in a novel S1 binding pocket which is larger in size to accommodate the phenyltriazolinone P1 substrate.
Texto completo:
1
Colección:
01-internacional
Base de datos:
MEDLINE
Asunto principal:
Pirazoles
/
Piridonas
/
Sulfonas
/
Diseño de Fármacos
/
Inhibidores del Factor Xa
/
Isoxazoles
/
Anticoagulantes
Tipo de estudio:
Prognostic_studies
Límite:
Humans
Idioma:
En
Revista:
Bioorg Med Chem Lett
Asunto de la revista:
BIOQUIMICA
/
QUIMICA
Año:
2010
Tipo del documento:
Article
País de afiliación:
Estados Unidos
