2,6-Bis-arylmethyloxy-5-hydroxychromones with antiviral activity against both hepatitis C virus (HCV) and SARS-associated coronavirus (SCV).
Eur J Med Chem
; 46(11): 5698-704, 2011 Nov.
Article
em En
| MEDLINE
| ID: mdl-21925774
ABSTRACT
In this study, as a bioisosteric alternative scaffold of the antiviral aryl diketoacids (ADKs), we used 5-hydroxychromone on which two arylmethyloxy substituents were installed. The 5-hydroxychromones (5b-5g) thus prepared showed anti-HCV activity and, depending on the aromatic substituents on the 2-arylmethyloxy moiety, some of the derivatives (5b-5f) were also active against SCV. In addition, unlike the ADKs which showed selective inhibition against the helicase activity of the SCV NTPase/helicase, the 5-hydroxychromones (5b-5f) were active against both NTPase and helicase activities of the target enzyme. Among those, 3-iodobenzyloxy-substituted derivative 5e showed the most potent activity against HCV (EC(50) = 4 µM) as well as SCV (IC(50) = 4 µM for ATPase activity, 11 µM for helicase activity) and this might be used as a platform structure for future development of the multi-target or broad-spectrum antivirals.
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Antivirais
/
Cromonas
/
Hepacivirus
/
Coronavírus Relacionado à Síndrome Respiratória Aguda Grave
Tipo de estudo:
Risk_factors_studies
Limite:
Humans
Idioma:
En
Revista:
Eur J Med Chem
Ano de publicação:
2011
Tipo de documento:
Article