High potency improvements to weak aryl uracil HCV polymerase inhibitor leads.
Bioorg Med Chem Lett
; 23(15): 4367-9, 2013 Aug 01.
Article
em 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.
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Antivirais
/
Uracila
/
Proteínas não Estruturais Virais
/
Hepacivirus
Limite:
Animals
Idioma:
En
Ano de publicação:
2013
Tipo de documento:
Article