Synthesis and antiviral activity of novel HCV NS3 protease inhibitors with P4 capping groups.
Bioorg Med Chem Lett
; 22(24): 7351-6, 2012 Dec 15.
Article
em En
| MEDLINE
| ID: mdl-23142614
ABSTRACT
We have synthesized and evaluated a series of novel HCV NS3 protease inhibitors with various P4 capping groups, which include urea, carbamate, methoxy-carboxamide, cyclic carbamate and amide, pyruvic amide, oxamate, oxalamide and cyanoguanidine. Most of these compounds are remarkably potent, exhibiting single-digit to sub-nanomolar activity in the enzyme assay and cell-based replicon assay. Selected compounds were also evaluated in the protease-inhibitor-resistant mutant transient replicon assay, and they were found to show quite different potency profiles against a panel of HCV protease-inhibitor-resistant mutants.
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Antivirais
/
Inibidores de Serina Proteinase
/
Proteínas não Estruturais Virais
/
Hepacivirus
Limite:
Animals
Idioma:
En
Ano de publicação:
2012
Tipo de documento:
Article