Novel inhibitors of bacterial two-component systems with gram positive antibacterial activity: pharmacophore identification based on the screening hit closantel.
Bioorg Med Chem Lett
; 8(14): 1923-8, 1998 Jul 21.
Article
en En
| MEDLINE
| ID: mdl-9873460
ABSTRACT
This SAR study has shown that the salicylanilide is the pharmacophore for inhibition of the bacterial two-component system. Hydrophobic substituents improve the potency of inhibitors in this series; however, hydrophobicity is not the sole determinant for inhibition; structural and electronic requirements also exist. Closantel (1) was found to inhibit a two-component system and to have antibacterial activity against drug resistant S. aureus and E. faecium.
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Base de datos:
MEDLINE
Asunto principal:
Salicilanilidas
/
Bacterias Grampositivas
/
Antibacterianos
Tipo de estudio:
Diagnostic_studies
/
Screening_studies
Idioma:
En
Revista:
Bioorg Med Chem Lett
Asunto de la revista:
BIOQUIMICA
/
QUIMICA
Año:
1998
Tipo del documento:
Article
País de afiliación:
Estados Unidos