ArticleJournal of medicinal chemistry2019
Exploitation of Antibiotic Resistance as a Novel Drug Target: Development of a β-Lactamase-Activated Antibacterial Prodrug.
Article in Journal of medicinal chemistry, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 27 papers.
What it found
Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.
The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
27 citing papers in PubMed, 69 citations in OpenAlex.
- Perspective Approaches to "Trojan Horse" Strategy Development for Combating Bacterial Pathogens.Pharmaceuticals (Basel, Switzerland) · 2026Review
- Bacterial enzyme-responsive hydrogels for triggered delivery of antibiotics to infected wounds.Science advances · 2026Article
- Recent trends in dual-acting hybrid antibiotics and combination therapies against Gram-negative pathogens.Journal of microbiology (Seoul, Korea) · 2026Review
- Article
- Metal-Catalyzed Cross-Coupling for the Synthesis of β-Lactam Drugs and Related Chemical Probes.ChemMedChem · 2025Review
- Prodrug activation in malaria parasites mediated by an imported erythrocyte esterase, acylpeptide hydrolase (APEH).Proceedings of the National Academy of Sciences of the United States of America · 2025Article
- Strategic re-engineering of antibiotics.Nature reviews bioengineering · 2025Article
- Highly Sensitive In Vivo Imaging of Bacterial Infections with a Hydrophilicity-Switching, Self-Immobilizing, Near-Infrared Fluorogenic β-Lactamase Probe Enriched within Bacteria.Advanced science (Weinheim, Baden-Wurttemberg, Germany) · 2025Article
- Prodrug activation in malaria parasites mediated by an imported erythrocyte esterase, acylpeptide hydrolase (APEH).bioRxiv : the preprint server for biology · 2024Article
- Synthesis of ciprofloxacin-linked 1,2,3-triazole conjugates as potent antibacterial agents using click chemistry: exploring their function as DNA gyrase inhibitorsRSC advances · 2024Article
- The landscape of small-molecule prodrugs.Nature reviews. Drug discovery · 2024Review
- Staph wars: the antibiotic pipeline strikes back.Microbiology (Reading, England) · 2023Review
- Review
- Development and Evaluation of EDTA-Treated Rabbits for Bioavailability Study of Chelating Drugs Using Levofloxacin, Ciprofloxacin, Hemiacetal Ester Prodrugs, and Tetracycline.Pharmaceutics · 2023Article
- An Update Review of Approaches to Multiple Action-Based Antibacterials.Antibiotics (Basel, Switzerland) · 2023Review
- Design and Synthesis of Novel Antimicrobial Agents.Antibiotics (Basel, Switzerland) · 2023Review
- Fighting antibiotic resistance-strategies and (pre)clinical developments to find new antibacterials.EMBO reports · 2023Review
- Adenosine triphosphate-activated prodrug system for on-demand bacterial inactivation and wound disinfection.Nature communications · 2022Article
- Stimuli-Responsive Antibacterial Materials: Molecular Structures, Design Principles, and Biomedical Applications.Advanced science (Weinheim, Baden-Wurttemberg, Germany) · 2022Review
- Dimensionless parameter predicts bacterial prodrug success.Molecular systems biology · 2022Article
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
10 authors at 2 institutions in 1 country.
Funding
Abstract
Expression of β-lactamase is the single most prevalent determinant of antibiotic resistance, rendering bacteria resistant to β-lactam antibiotics. In this article, we describe the development of an antibiotic prodrug that combines ciprofloxacin with a β-lactamase-cleavable motif. The prodrug is only bactericidal after activation by β-lactamase. Bactericidal activity comparable to ciprofloxacin is demonstrated against clinically relevant E. coli isolates expressing diverse β-lactamases; bactericidal activity was not observed in strains without β-lactamase. These findings demonstrate that it is possible to exploit antibiotic resistance to selectively target β-lactamase-producing bacteria using our prodrug approach, without adversely affecting bacteria that do not produce β-lactamase. This paves the way for selective targeting of drug-resistant pathogens without disrupting or selecting for resistance within the microbiota, reducing the rate of secondary infections and subsequent antibiotic use.
Indexed as
Identifiers
What OpenQuestion holds
Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.