High potency improvements to weak aryl uracil HCV polymerase inhibitor leads.
Bioorg Med Chem Lett
; 23(15): 4367-9, 2013 Aug 01.
Article
in En
| MEDLINE
| ID: mdl-23791079
ABSTRACT
Described herein is the development of a potent non-nucleoside, small molecule inhibitor of genotype 1 HCV NS5B Polymerase. A 23 µM inhibitor that was active against HCV polymerase was further elaborated into a potent single-digit nanomolar inhibitor of HCV NS5B polymerase by additional manipulation of the R and R1 substituents. Subsequent modifications to improve physical properties were made in an attempt to achieve an acceptable pharmacokinetic profile.
Full text:
1
Collection:
01-internacional
Database:
MEDLINE
Main subject:
Antiviral Agents
/
Uracil
/
Viral Nonstructural Proteins
/
Hepacivirus
Limits:
Animals
Language:
En
Journal:
Bioorg Med Chem Lett
Journal subject:
BIOQUIMICA
/
QUIMICA
Year:
2013
Document type:
Article
Affiliation country:
United States