Fluoroquinolone-derived Fluorescent Probes for Studies of Bacterial Penetration and Efflux

Overview

Journal Medchemcomm

Publisher Royal Society of Chemistry

Specialty Chemistry

Date 2019 Jul 16

PMID 31303987

Citations 17

Authors

M Rhia L Stone

Muriel Masi

Wanida Phetsang

Jean-Marie Pages

Matthew A Cooper

Mark A T Blaskovich

Affiliations

Soon will be listed here.

Abstract

Fluorescent probes derived from the fluoroquinolone antibiotic ciprofloxacin were synthesised using a Cu(i)-catalysed azide-alkyne cycloaddition (CuAAC) to link a ciprofloxacin azide derivative with alkyne-substituted green and blue fluorophores. The azide () and fluorophore ( and ) derivatives retained antimicrobial activity against Gram-positive and Gram-negative bacteria. The use of confocal fluorescent microscopy showed intracellular penetration, which was substantially enhanced in the presence of carbonyl cyanide 3-chlorophenylhydrazone as an efflux pump inhibitor in .

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