ArticleBiometals : an international journal on the role of metal ions in biology, biochemistry, and medicine2015
Siderophore-fluoroquinolone conjugates containing potential reduction-triggered linkers for drug release: synthesis and antibacterial activity.
Article in Biometals : an international journal on the role of metal ions in biology, biochemistry, and medicine, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 22 papers.
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Who cites it
22 citing papers in PubMed.
- The Role of Bacterial Siderophores in Infection Therapy: From Anti-Infective Mechanisms to Therapeutic Advances.International journal of nanomedicine · 2025Review
- Location, Location, Location: Establishing Design Principles for New Antibacterials from Ferric Siderophore Transport Systems.Molecules (Basel, Switzerland) · 2024Review
- Exploring the Antibacterial Activity and Cellular Fates of Enterobactin-Drug Conjugates That Target Gram-Negative Bacterial Pathogens.Accounts of chemical research · 2024Article
- Benzothiazole DNA gyrase inhibitors and their conjugates with siderophore mimics: design, synthesis and evaluation.RSC advances · 2024Article
- Siderophores as tools and treatments.npj antimicrobials and resistance · 2024Review
- A Novel Natural Siderophore Antibiotic Conjugate Reveals a Chemical Approach to Macromolecule Coupling.ACS central science · 2023Article
- Siderophore conjugates to combat antibiotic-resistant bacteria.RSC medicinal chemistry · 2023Review
- Siderophore conjugation with cleavable linkers boosts the potency of RNA polymerase inhibitors against multidrug-resistantChemical science · 2023Article
- Synthesis and Characterization of DOTAM-Based Sideromycins for Bacterial Imaging and Antimicrobial Therapy.ACS infectious diseases · 2023Article
- Trojan Horse Siderophore Conjugates InduceJournal of medicinal chemistry · 2023Article
- Enzyme-Activated, Chemiluminescent Siderophore-Dioxetane Probes Enable the Selective and Highly Sensitive Detection of Bacterial Pathogens.Angewandte Chemie (International ed. in English) · 2022Article
- Tracking Uptake and Metabolism of Xenometallomycins Using a Multi-Isotope Tagging Strategy.ACS infectious diseases · 2022Article
- Design and Syntheses of New Antibiotics Inspired by Nature's Quest for Iron in an Oxidative Climate.Accounts of chemical research · 2021Review
- Enterobactin- and salmochelin-β-lactam conjugates induce cell morphologies consistent with inhibition of penicillin-binding proteins in uropathogenicChemical science · 2021Article
- Platform to Discover Protease-Activated Antibiotics and Application to Siderophore-Antibiotic Conjugates.Journal of the American Chemical Society · 2020Article
- Iron Metabolism at the Interface between Host and Pathogen: From Nutritional Immunity to Antibacterial Development.International journal of molecular sciences · 2020Review
- Recent Progress in Natural-Product-Inspired Programs Aimed To Address Antibiotic Resistance and Tolerance.Journal of medicinal chemistry · 2019Review
- Siderophore-Antibiotic Conjugate Design: New Drugs for Bad Bugs?Molecules (Basel, Switzerland) · 2019Review
- Evaluation of a reducible disulfide linker for siderophore-mediated delivery of antibiotics.Journal of biological inorganic chemistry : JBIC : a publication of the Society of Biological Inorganic Chemistry · 2018Article
- Esterase-Catalyzed Siderophore Hydrolysis Activates an Enterobactin-Ciprofloxacin Conjugate and Confers Targeted Antibacterial Activity.Journal of the American Chemical Society · 2018Article
Corrections and comments
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Authors and funding
2 authors.
Funding
Abstract
Syntheses of two Siderophore-fluoroquinolone conjugates with a potential reduction triggered linker for drug release are described. The "trimethyl lock" based linker incorporated in the conjugates was designed to be activated by taking advantage of the reductive pathway of bacterial iron metabolism. Electrochemical and LC-MS studies indicated that the linker is thermodynamically reducible by common biological reductants and the expected lactonization proceeds rapidly with concomitant release of the drug. Antibacterial activity assays revealed that conjugates with the reduction-triggered linker were more potent than their counterparts with a stable linker, which suggests that drug release occurs inside bacterial cells.
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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.