Rational design and synthesis of potent aminoglycoside antibiotics against resistant bacterial strains.
Bioorg Med Chem
; 19(1): 30-40, 2011 Jan 01.
Article
em En
| MEDLINE
| ID: mdl-21177112
ABSTRACT
Based on the structural information of biomacromolecule-aminoglycoside complexes, a series of kanamycin B analogues were rationally designed and synthesized. A convenient approach to the construction of kanamycin derivatives, in which the C4'-position on ring I of neamine moiety was modified, was developed. Most synthetic analogues exhibited good to excellent antibiotic activity against some typical drug-resistant bacteria. The disclosed results suggested that the C4'-position of aminoglycosides such as kanamycin may be an ideal site for modification to gain new modifying enzyme-resistant aminoglycoside antibiotics.
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Desenho de Fármacos
/
Aminoglicosídeos
/
Antibacterianos
Idioma:
En
Ano de publicação:
2011
Tipo de documento:
Article
País de afiliação:
China