An azido-oxazolidinone antibiotic for live bacterial cell imaging and generation of antibiotic variants.
Bioorg Med Chem
; 22(16): 4490-8, 2014 Aug 15.
Article
em En
| MEDLINE
| ID: mdl-25023540
ABSTRACT
An azide-functionalised analogue of the oxazolidinone antibiotic linezolid was synthesised and shown to retain antimicrobial activity. Using facile 'click' chemistry, this versatile intermediate can be further functionalised to explore antimicrobial structure-activity relationships or conjugated to fluorophores to generate fluorescent probes. Such probes can report bacteria and their location in a sample in real time. Modelling of the structures bound to the cognate 50S ribosome target demonstrates binding to the same site as linezolid is possible. The fluorescent probes were successfully used to image Gram-positive bacteria using confocal microscopy.
Palavras-chave
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Azidas
/
Oxazolidinonas
/
Corantes Fluorescentes
/
Bactérias Gram-Positivas
/
Antibacterianos
Idioma:
En
Revista:
Bioorg Med Chem
Assunto da revista:
BIOQUIMICA
/
QUIMICA
Ano de publicação:
2014
Tipo de documento:
Article
País de afiliação:
Austrália