{"database":"biostudies-literature","file_versions":[],"scores":null,"additional":{"submitter":["Pandey A"],"funding":["National Institute of General Medical Sciences","NIGMS NIH HHS"],"pagination":["14546-14556"],"full_dataset_link":["https://www.ebi.ac.uk/biostudies/studies/S-EPMC8580130"],"repository":["biostudies-literature"],"omics_type":["Unknown"],"volume":["12(43)"],"pubmed_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 <i>S. aureus</i> bacterial infections. We employed characterization using <i>in vitro</i> inhibitory assays, radiochemical, tracer-based uptake and pharmacokinetic assessment of our lead compound, culminating in <i>in vivo</i> efficacy studies in a soft tissue model of infection. Galbofloxacin exhibits a minimum inhibitory concentration of (MIC<sub>98</sub>) 93 nM in wt <i>S. aureus</i>, exceeding the potency of the parent antib"],"journal":["Chemical science"],"pubmed_title":["Galbofloxacin: a xenometal-antibiotic with potent <i>in vitro</i> and <i>in vivo</i> efficacy against <i>S. aureus</i>."],"pmcid":["PMC8580130"],"funding_grant_id":["R35GM142770","R35 GM142770"],"pubmed_authors":["Boros E","Smilowicz D","Pandey A"],"additional_accession":[]},"is_claimable":false,"name":"Galbofloxacin: a xenometal-antibiotic with potent <i>in vitro</i> and <i>in vivo</i> efficacy against <i>S. aureus</i>.","description":"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 <i>S. aureus</i> bacterial infections. We employed characterization using <i>in vitro</i> inhibitory assays, radiochemical, tracer-based uptake and pharmacokinetic assessment of our lead compound, culminating in <i>in vivo</i> efficacy studies in a soft tissue model of infection. Galbofloxacin exhibits a minimum inhibitory concentration of (MIC<sub>98</sub>) 93 nM in wt <i>S. aureus</i>, exceeding the potency of the parent antib","dates":{"release":"2021-01-01T00:00:00Z","publication":"2021 Nov","modification":"2026-05-08T16:37:24.858Z","creation":"2025-06-01T00:57:14.542Z"},"accession":"S-EPMC8580130","cross_references":{"pubmed":["34881006"],"doi":["10.1039/d1sc04283a"]}}