ArticleAntimicrobial agents and chemotherapy2011
Contrasting effects of acidic pH on the extracellular and intracellular activities of the anti-gram-positive fluoroquinolones moxifloxacin and delafloxacin against Staphylococcus aureus.
Article in Antimicrobial agents and chemotherapy, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 80 papers.
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Who cites it
80 citing papers in PubMed.
- Analysis of Pooled Phase III Efficacy Data for Delafloxacin in Acute Bacterial Skin and Skin Structure Infections.Clinical infectious diseases : an official publication of the Infectious Diseases Society of America · 2019Trial
- Efficacy and safety of delafloxacin compared with vancomycin plus aztreonam for acute bacterial skin and skin structure infections: a Phase 3, double-blind, randomized study.The Journal of antimicrobial chemotherapy · 2017Trial
- Delafloxacin Resistance and MIC-Distribution in Ciprofloxacin-Resistant Enterobacterales: A Retrospective Evaluation of Minimum Inhibitory Concentrations.Antibiotics (Basel, Switzerland) · 2026Article
- Evaluation of in vitro activity of delafloxacin against Staphylococcus aureus MSSA and MRSA isolated from a Brazilian tertiary hospital.Brazilian journal of microbiology : [publication of the Brazilian Society for Microbiology] · 2026Article
- Genome-wide network of antibiotic susceptibility in Pseudomonas aeruginosa.The Journal of antimicrobial chemotherapy · 2026Article
- Current Recommendations, Antibiotic Resistance, and Emerging Treatments for Gram-Positive Ocular Infections in the United States.Antibiotics (Basel, Switzerland) · 2026Review
- Evaluating the efficacy of delafloxacin and combination therapy against Staphylococcus aureus Biofilms: insights into activity in acidic environments.Scientific reports · 2026Article
- Delafloxacin: what does a new fluoroquinolone offer?Revista espanola de quimioterapia : publicacion oficial de la Sociedad Espanola de Quimioterapia · 2026Review
- Article
- Delafloxacin-Loaded Poly(d,l-lactide-ACS omega · 2024Article
- Article
- Impact of Growth Conditions on High-Throughput Identification of Repurposing Drugs forAntibiotics (Basel, Switzerland) · 2024Article
- Article
- Measurement of Accumulation of Antibiotics to Staphylococcus aureus in Phagosomes of Live Macrophages.Angewandte Chemie (International ed. in English) · 2024Article
- New Antimicrobials for Gram-Positive Sustained Infections: A Comprehensive Guide for Clinicians.Pharmaceuticals (Basel, Switzerland) · 2023Review
- Updated Review on Clinically-Relevant Properties of Delafloxacin.Antibiotics (Basel, Switzerland) · 2023Review
- Activity of Delafloxacin and Comparator Fluoroquinolones against Multidrug-ResistantAntibiotics (Basel, Switzerland) · 2023Article
- Novel ciprofloxacin and norfloxacin-tetrazole hybrids as potential antibacterial and antiviral agents: TargetingJournal of molecular structure · 2023Article
- Structural modeling of hERG channel-drug interactions using Rosetta.Frontiers in pharmacology · 2023Article
- Interaction between moxifloxacin and Mcl-1 and MITF proteins: the effect on growth inhibition and apoptosis in MDA-MB-231 human triple-negative breast cancer cells.Pharmacological reports : PR · 2022Article
20 more citing papers are in PubMed but not listed here.
Corrections and comments
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Authors and funding
3 authors.
Funding
No grant is acknowledged in the PubMed record.
Abstract
In contrast to currently marketed fluoroquinolones, which are zwitterionic, delafloxacin is an investigational fluoroquinolone with an anionic character that is highly active against Gram-positive bacteria. We have examined the effect of acidic pH on its accumulation in Staphylococcus aureus and in human THP-1 cells, in parallel with its activity against extracellular and intracellular S. aureus. Moxifloxacin was used as a comparator. Delafloxacin showed MICs 3 to 5 log(2) dilutions lower than those of moxifloxacin for a collection of 35 strains with relevant resistance mechanisms and also proved to be 10-fold more potent against intracellular S. aureus ATCC 25923. In medium at pH 5.5, this difference was further enhanced, with the MIC decreasing by 5 log(2) dilutions. In infected cells incubated in acidic medium, the relative potency was 10-fold higher than that at neutral pH and the maximal relative efficacy reached a bactericidal effect at 24 h. These results can be explained by a 10-fold increase in delafloxacin accumulation in both bacteria and cells at acidic pH, making delafloxacin one of the most efficient drugs tested in this model. Opposite effects were seen for moxifloxacin with respect to both activity and accumulation. As reported for zwitterionic fluoroquinolones, delafloxacin was found associated with the soluble fraction in homogenates of eukaryotic cells. Taken together, these properties may confer to delafloxacin an advantage for the eradication of S. aureus in acidic environments, including intracellular infections.
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