ArticleBioorganic & medicinal chemistry letters2012
Studies on the antimicrobial properties of N-acylated ciprofloxacins.
Article in Bioorganic & medicinal chemistry letters, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 19 papers.
What it found
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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.
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Who cites it
19 citing papers in PubMed.
- The Difluoroboranyl-Fluoroquinolone Derivative "7a" Inhibits Bacterial DNA Gyrase and Exhibits Potent Activity Against Ciprofloxacin-ResistantMolecules (Basel, Switzerland) · 2026Article
- Emulsified Homo (Ciprofloxacin) Polymer Nanoparticles for Antibacterial Applications.International journal of molecular sciences · 2025Article
- A green marriage: the union of theophylline's catalytic activity and healing potential.RSC advances · 2025Review
- Advancements in Synthetic Strategies and Biological Effects of Ciprofloxacin Derivatives: A Review.International journal of molecular sciences · 2024Review
- Synthesis and biological evaluation of pyridylpiperazine hybrid derivatives as urease inhibitors.Frontiers in chemistry · 2024Article
- Protease inhibition, in vitro antibacterial and IFD/MM-GBSA studies of ciprofloxacin-based acetanilides.PloS one · 2023Article
- Ultrasonic-Assisted Synthesis of Benzofuran Appended Oxadiazole Molecules as Tyrosinase Inhibitors: Mechanistic Approach through Enzyme Inhibition, Molecular Docking, Chemoinformatics, ADMET and Drug-Likeness Studies.International journal of molecular sciences · 2022Article
- Article
- Ultrasound-Assisted Synthesis and In Silico Modeling of Methanesulfonyl-Piperazine-Based Dithiocarbamates as Potential Anticancer, Thrombolytic, and Hemolytic Structural Motifs.Molecules (Basel, Switzerland) · 2022Article
- Enzyme-Responsive Nanoparticles and Coatings Made from Alginate/Peptide Ciprofloxacin Conjugates as Drug Release System.Antibiotics (Basel, Switzerland) · 2021Article
- An immunoinformatics approach for the design of a multi-epitope vaccine targeting super antigen TSST-1 of Staphylococcus aureus.Journal, genetic engineering & biotechnology · 2021Article
- Synthesis, Hemolytic Studies, andACS omega · 2021Article
- Resistance pattern ofIranian journal of microbiology · 2020Article
- Characterizing the Antimicrobial Activity ofAntimicrobial agents and chemotherapy · 2017Article
- An Update on Clinical Burden, Diagnostic Tools, and Therapeutic Options ofInfectious diseases · 2017Review
- Anionic fluoroquinolones as antibacterials against biofilm-producing Pseudomonas aeruginosa.Bioorganic & medicinal chemistry letters · 2016Article
- Syntheses and Antibacterial Activity of N-Acylated Ciprofloxacin Derivatives Based on the Trimethyl Lock.ACS medicinal chemistry letters · 2015Article
- Pharmacological characterization of 7-(4-(Piperazin-1-yl)) ciprofloxacin derivatives: antibacterial activity, cellular accumulation, susceptibility to efflux transporters, and intracellular activity.Pharmaceutical research · 2014Article
- Draft Genome Sequence of Strain CBD-635, a Methicillin-Resistant Staphylococcus aureus USA100 Isolate.Genome announcements · 2013Article
Corrections and comments
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Authors and funding
11 authors.
Funding
Abstract
Fluoroquinolone antibiotics have been a mainstay in the treatment of bacterial diseases. The most notable representative, ciprofloxacin, possesses potent antimicrobial activity; however, a rise in resistance to this agent necessitates development of novel derivatives to prolong the clinical lifespan of these antibiotics. Herein we have synthesized and analyzed the antimicrobial properties of a library of N-acylated ciprofloxacin analogues. We find that these compounds are broadly effective against Gram-positive and Gram-negative bacteria, with many proving more effective than the parental drug, and several possessing MICs ≤1.0 μg/ml against methicillin-resistant Staphylococcus aureus and Bartonella species. An analysis of spontaneous mutation frequencies reveals very low potential for resistance in MRSA compared to existing fluoroquinolones. Mode of action profiling reveals that modification of the piperazinyl nitrogen by acylation does not alter the effect of these molecules towards their bacterial target. We also present evidence that these N-acylated compounds are highly effective at killing intracellular bacteria, suggesting the suitability of these antibiotics for therapeutic treatment.
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Registered trials
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