Oseltamivir analogues bearing N-substituted guanidines as potent neuraminidase inhibitors.
J Med Chem
; 57(7): 3154-60, 2014 Apr 10.
Article
em En
| MEDLINE
| ID: mdl-24649802
ABSTRACT
A series of oseltamivir analogues bearing an N-substituted guanidine unit were prepared and evaluated as inhibitors of neuraminidases from four strains of influenza. The two most potent analogues identified contain relatively small N-guanidine substituents (N-methyl and N-hydroxyl) and display enhanced inhibition with IC50 values in the low nanomolar range against neuraminidases from wild-type and oseltamivir-resistant strains. Potential advantages of including the N-hydroxyguanidine moiety in neuraminidase inhibitors are also discussed.
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Antivirais
/
Vírus da Influenza A
/
Oseltamivir
/
Guanidinas
/
Neuraminidase
Limite:
Humans
Idioma:
En
Revista:
J Med Chem
Ano de publicação:
2014
Tipo de documento:
Article