Journal
BIOORGANIC & MEDICINAL CHEMISTRY
Volume 22, Issue 16, Pages 4490-4498Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2014.05.054
Keywords
Antibiotics; Linezolid; Fluorescent probes; Bacteria; Click chemistry
Funding
- NHMRC [APP631632, APP1026922, AF511105, APP1059354]
- Australian Postgraduate Award (APA) PhD scholarship
- Wellcome Trust [094977/Z/10/Z]
- ACRF
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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. (C) 2014 The Authors. Published by Elsevier Ltd. This is an open access article under the CC BY license ( http://creativecommons.org/licenses/by/3.0/).
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