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An azido-oxazolidinone antibiotic for live bacterial cell imaging and generation of antibiotic variants.

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.

journal_name

Bioorg Med Chem

journal_title

Bioorganic & medicinal chemistry

authors

Phetsang W,Blaskovich MA,Butler MS,Huang JX,Zuegg J,Mamidyala SK,Ramu S,Kavanagh AM,Cooper MA

doi

10.1016/j.bmc.2014.05.054

subject

Has Abstract

pub_date

2014-08-15 00:00:00

pages

4490-8

issue

16

eissn

0968-0896

issn

1464-3391

pii

S0968-0896(14)00413-1

journal_volume

22

pub_type

杂志文章

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