Structure-activity relationships of bacterial outer-membrane permeabilizers based on polymyxin B heptapeptides.
Bioorg Med Chem Lett
; 20(5): 1771-5, 2010 Mar 01.
Article
en En
| MEDLINE
| ID: mdl-20138759
ABSTRACT
A series of cationic cyclic heptapeptides based on polymyxin B have been synthesized for use as permeabilizers of the outer membrane of Gram-negative bacteria. Only analogs with the Dab(2)-d-Phe(3)-Leu(4)-Xxx(5) sequence (Xxx = Dab or Orn) showed a synergistic bactericidal effect when combined with conventional antibiotics, indicating that the Dab(2) residue plays a critical role in permeation of the outer membrane of Gram-negative bacteria.
Texto completo:
1
Colección:
01-internacional
Base de datos:
MEDLINE
Asunto principal:
Péptidos Cíclicos
/
Polimixina B
/
Permeabilidad de la Membrana Celular
/
Escherichia coli
/
Antibacterianos
Idioma:
En
Revista:
Bioorg Med Chem Lett
Asunto de la revista:
BIOQUIMICA
/
QUIMICA
Año:
2010
Tipo del documento:
Article
País de afiliación:
Japón