Galbofloxacin: a xenometal-antibiotic with potent in vitro and in vivo efficacy against S. aureus.

ABSTRACT: Siderophore-antibiotic drug conjugates are considered potent tools to deliver and potentiate the antibacterial activity of antibiotics, but only few have seen preclinical and clinical success. Here, we introduce the gallium(iii) complex of a ciprofloxacin-functionalized linear desferrichrome, Galbofloxacin, with a cleavable serine linker as a potent therapeutic for S. aureus bacterial infections. We employed characterization using in vitro inhibitory assays, radiochemical, tracer-based uptake and pharmacokinetic assessment of our lead compound, culminating in in vivo efficacy studies in a soft tissue model of infection. Galbofloxacin exhibits a minimum inhibitory concentration of (MIC₉₈) 93 nM in wt S. aureus, exceeding the potency of the parent antib

SUBMITTER: Pandey A 

PROVIDER: S-EPMC8580130 | biostudies-literature | 2021 Nov

REPOSITORIES: biostudies-literature