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
in 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.
Full text:
1
Collection:
01-internacional
Database:
MEDLINE
Main subject:
Antiviral Agents
/
Serine Proteinase Inhibitors
/
Viral Nonstructural Proteins
/
Hepacivirus
Limits:
Animals
Language:
En
Journal:
Bioorg Med Chem Lett
Journal subject:
BIOQUIMICA
/
QUIMICA
Year:
2012
Document type:
Article
Affiliation country: