P4 capped amides and lactams as HCV NS3 protease inhibitors with improved potency and DMPK profile.
Bioorg Med Chem Lett
; 20(2): 567-70, 2010 Jan 15.
Article
en En
| MEDLINE
| ID: mdl-20004570
ABSTRACT
SAR studies on the extension of P3 unit of Boceprevir (1, SCH 503034) with amides and lactams and their synthesis is described. Extensive SAR studies resulted in the identification of 36 bearing 4, 4-dimethyl lactam as the new P4 cap unit with improved potency (K(i)( *)=15nM, EC 90=70nM) and pharmacokinetic properties (Rat AUC (PO)=3.52microMh) compared to 1.
Texto completo:
1
Colección:
01-internacional
Base de datos:
MEDLINE
Asunto principal:
Antivirales
/
Oligopéptidos
/
Inhibidores de Proteasas
/
Proteínas no Estructurales Virales
/
Amidas
/
Lactamas
Límite:
Animals
Idioma:
En
Revista:
Bioorg Med Chem Lett
Asunto de la revista:
BIOQUIMICA
/
QUIMICA
Año:
2010
Tipo del documento:
Article
País de afiliación:
Estados Unidos