Synthesis of new acylsulfamoyl benzoxaboroles as potent inhibitors of HCV NS3 protease.
Bioorg Med Chem Lett
; 20(24): 7493-7, 2010 Dec 15.
Article
in En
| MEDLINE
| ID: mdl-21041080
ABSTRACT
HCV NS3/4A serine protease is essential for the replication of the HCV virus and has been a clinically validated target. A series of HCV NS3/4A protease inhibitors containing a novel acylsulfamoyl benzoxaborole moiety at the P1' region was synthesized and evaluated. The resulting P1-P3 and P2-P4 macrocyclic inhibitors exhibited sub-nanomolar potency in the enzymatic assay and low nanomolar activity in the cell-based replicon assay. The in vivo PK evaluations of selected compounds are also described.
Full text:
1
Collection:
01-internacional
Database:
MEDLINE
Main subject:
Protease Inhibitors
/
Boron Compounds
/
Viral Nonstructural Proteins
/
Hepacivirus
Limits:
Animals
Language:
En
Journal:
Bioorg Med Chem Lett
Journal subject:
BIOQUIMICA
/
QUIMICA
Year:
2010
Document type:
Article
Affiliation country: