HCV NS5A replication complex inhibitors. Part 3: discovery of potent analogs with distinct core topologies.
Bioorg Med Chem Lett
; 23(3): 779-84, 2013 Feb 01.
Article
en En
| MEDLINE
| ID: mdl-23273521
ABSTRACT
In a recent disclosure, we described the discovery of dimeric, prolinamide-based NS5A replication complex inhibitors exhibiting excellent potency towards an HCV genotype 1b replicon. That disclosure dealt with the SAR exploration of the peripheral region of our lead chemotype, and herein is described the SAR uncovered from a complementary effort that focused on the central core region. From this effort, the contribution of the core region to the overall topology of the pharmacophore, primarily vector orientation and planarity, was determined, with a set of analogs exhibiting <10 nM EC(50) in a genotype 1b replicon assay.
Texto completo:
1
Bases de datos:
MEDLINE
Asunto principal:
Antivirales
/
Proteínas no Estructurales Virales
Idioma:
En
Revista:
Bioorg Med Chem Lett
Asunto de la revista:
BIOQUIMICA
/
QUIMICA
Año:
2013
Tipo del documento:
Article
País de afiliación:
Estados Unidos