Fluoroquinolone-derived fluorescent probes for studies of bacterial penetration and efflux.

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 (2) and fluorophore (3 and 4) 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 Escherichia coli.

SUBMITTER: Stone MRL 

PROVIDER: S-EPMC6596217 | biostudies-literature | 2019 Jun

REPOSITORIES: biostudies-literature