Synthesis and SAR of pyridothiazole substituted pyrimidine derived HCV replication inhibitors.
Bioorg Med Chem Lett
; 22(17): 5652-7, 2012 Sep 01.
Article
en En
| MEDLINE
| ID: mdl-22858143
ABSTRACT
Introduction of a nitrogen atom into the benzene ring of a previously identified HCV replication (replicase) benzothiazole inhibitor 1, resulted in the discovery of the more potent pyridothiazole analogues 3. The potency and PK properties of the compounds were attenuated by the introductions of various functionalities at the R(1), R(2) or R(3) positions of the molecule (compound 3). Inhibitors 38 and 44 displayed excellent potency, selectivity (GAPDH/MTS CC(50)), PK parameters in all species studied, and cross genotype activity.
Texto completo:
1
Banco de datos:
MEDLINE
Asunto principal:
Antivirales
/
Pirimidinas
/
Replicación Viral
/
Hepacivirus
Límite:
Animals
/
Humans
Idioma:
En
Revista:
Bioorg Med Chem Lett
Asunto de la revista:
BIOQUIMICA
/
QUIMICA
Año:
2012
Tipo del documento:
Article
País de afiliación:
Estados Unidos