Exploratory solid-phase synthesis of factor Xa inhibitors: discovery and application of p3-heterocyclic amides as novel types of non-basic arginine surrogates.
Bioorg Med Chem Lett
; 9(24): 3459-64, 1999 Dec 20.
Article
en En
| MEDLINE
| ID: mdl-10617091
ABSTRACT
A series of novel FXa inhibitors 2a-m and 3a-f was discovered that feature heterocyclic carboxamides tethered to a d-diaminobutyric acid sidechain. These neutral amide derivatives serve as novel P3 d-arginine mimics. Pyrazine carboxamide scaffolds afforded the most potent FXa inhibitors (e.g., 2b IC50 = 4.6 nM). The synthesis and biological activity of two focused libraries are reported.
Buscar en Google
Colección:
01-internacional
Base de datos:
MEDLINE
Asunto principal:
Arginina
/
Inhibidores de Serina Proteinasa
/
Inhibidores del Factor Xa
/
Amidas
/
Compuestos Heterocíclicos
Idioma:
En
Revista:
Bioorg Med Chem Lett
Asunto de la revista:
BIOQUIMICA
/
QUIMICA
Año:
1999
Tipo del documento:
Article
País de afiliación:
Estados Unidos