ArticleAntimicrobial agents and chemotherapy2010
Structure-activity relationships of diverse oxazolidinones for linezolid-resistant Staphylococcus aureus strains possessing the cfr methyltransferase gene or ribosomal mutations.
Article in Antimicrobial agents and chemotherapy, 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 58 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.
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
58 citing papers in PubMed, 145 citations in OpenAlex.
- Platelet profile in patients with acute bacterial skin and skin structure infections receiving tedizolid or linezolid: findings from the Phase 3 ESTABLISH clinical trials.Antimicrobial agents and chemotherapy · 2014Trial
- Efficacy, safety, tolerability and population pharmacokinetics of tedizolid, a novel antibiotic, in Latino patients with acute bacterial skin and skin structure infections.The Brazilian journal of infectious diseases : an official publication of the Brazilian Society of Infectious DiseasesTrial
- Designing the Next Generation of Antibiotics: Structure, SAR, and Strategy in Medicinal Chemistry (2000-2025).Medicinal research reviews · 2026Review
- Current Recommendations, Antibiotic Resistance, and Emerging Treatments for Gram-Positive Ocular Infections in the United States.Antibiotics (Basel, Switzerland) · 2026Review
- Subinhibitory Concentrations of Rifampicin Synergize with Linezolid to Delay Resistance Evolution in Clinical Methicillin-Resistant Staphylococcus Aureus.Microorganisms · 2026Article
- Performance of EUCAST disc diffusion and supplementary methods to detect reduced susceptibility to linezolid in enterococci- the NordicAST LRE-study.The Journal of antimicrobial chemotherapy · 2026Article
- Huisgen Cycloaddition of Azidoazulenes: Synthesis, Structural and Optical Properties of 2- and 6-(1,2,3-Triazol-1-yl)azulenes.Molecules (Basel, Switzerland) · 2026Article
- Hybrid Antibiotics Targeting the Bacterial Ribosome.ACS central science · 2025Article
- Identification of genetic mutations conferring tedizolid resistance in MRSA mutants.European journal of clinical microbiology & infectious diseases : official publication of the European Society of Clinical Microbiology · 2025Article
- Fluorescent Antibiotics: Bridging Diagnostic and Therapy in the Fight against Bacterial Infections.Small science · 2025Review
- Antechodynamics and Antechokinetics: Dynamics and Kinetics of Antibiotic Resistance Biomolecules.Biomolecules · 2025Review
- Comparative In Vitro Drug Susceptibility Study of Five Oxazolidinones AgainstPathogens (Basel, Switzerland) · 2025Article
- Diversity in Adaptive Evolution of Methicillin-ResistantInfection and drug resistance · 2025Article
- Oxazolidinone antibiotics impairAntimicrobial agents and chemotherapy · 2024Article
- New Oxazolidinones for Tuberculosis: Are Novel Treatments on the Horizon?Pharmaceutics · 2024Review
- In vitro activity of tedizolid against 43 species of Nocardia species.Scientific reports · 2024Article
- Staph wars: the antibiotic pipeline strikes back.Microbiology (Reading, England) · 2023Review
- Co-Existence of Oxazolidinone Resistance GenesAntibiotics (Basel, Switzerland) · 2023Article
- Ribosome-targeting antibiotics and resistanceRSC medicinal chemistry · 2023Review
- Comparative Assessment of Docking Programs for Docking and Virtual Screening of Ribosomal Oxazolidinone Antibacterial Agents.Antibiotics (Basel, Switzerland) · 2023Article
Corrections and comments
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Authors and funding
10 authors at 3 institutions in 3 countries.
Funding
Abstract
Staphylococcal resistance to linezolid (LZD) is mediated through ribosomal mutations (23S rRNA or ribosomal proteins L3 and L4) or through methylation of 23S rRNA by the horizontally transferred Cfr methyltransferase. To investigate the structural basis for oxazolidinone activity against LZD-resistant (LZD(r)) strains, we compared structurally diverse, clinically relevant oxazolidinones, including LZD, radezolid (RX-1741), TR-700 (torezolid), and a set of TR-700 analogs (including novel CD-rings and various A-ring C-5 substituents), against a panel of laboratory-derived and clinical LZD(r) Staphylococcus aureus strains possessing a variety of resistance mechanisms. Potency against all strains was correlated with optimization of C- and D-rings, which interact with more highly conserved regions of the peptidyl transferase center binding site. Activity against cfr strains was retained with either hydroxymethyl or 1,2,3-triazole C-5 groups but was reduced by 2- to 8-fold in compounds with acetamide substituents. LZD, which possesses a C-5 acetamide group and lacks a D-ring substituent, demonstrated the lowest potency against all strains tested, particularly against cfr strains. These data reveal key features contributing to oxazolidinone activity and highlight structural tradeoffs between potency against susceptible strains and potency against strains with various resistance mechanisms.
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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.