ArticleAntimicrobial agents and chemotherapy2011
The MUT056399 inhibitor of FabI is a new antistaphylococcal compound.
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 47 papers.
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Who cites it
47 citing papers in PubMed, 73 citations in OpenAlex.
- Fatty Acid Biosynthesis Inhibitors─Fabimycin and Triclosan─Trigger Distinct Resistance Mutations in FabI and Potently Kill Gram-Negative Pathogens.ACS infectious diseases · 2026Article
- Bacterial Acyl Carrier Proteins Are a Cytoplasmic Target for Different Cationic Antimicrobial and Antibiofilm Peptides.International journal of molecular sciences · 2026Article
- Fatty acid biosynthesis inhibitors fabimycin and triclosan trigger distinct resistance mutations in FabI and potently kill Gram-negative pathogens.bioRxiv : the preprint server for biology · 2026Article
- Antimicrobial potential of compounds from the MMV pandemic response box and COVID box against carbapenem-resistant Acinetobacter baumannii.Brazilian journal of microbiology : [publication of the Brazilian Society for Microbiology] · 2025Article
- Structure-Activity Relationships and Design of Focused Libraries Tailored for Staphylococcus Aureus Inhibition.Molecular informatics · 2025Article
- Fighting Antimicrobial Resistance: Innovative Drugs in Antibacterial Research.Angewandte Chemie (International ed. in English) · 2025Review
- Lipid-Centric Approaches in Combating Infectious Diseases: Antibacterials, Antifungals and Antivirals with Lipid-Associated Mechanisms of Action.Antibiotics (Basel, Switzerland) · 2023Review
- X-ray screening identifies active site and allosteric inhibitors of SARS-CoV-2 main protease.Science (New York, N.Y.) · 2021Article
- A Long Residence Time Enoyl-Reductase Inhibitor Explores an Extended Binding Region with Isoenzyme-Dependent Tautomer Adaptation and Differential Substrate-Binding Loop Closure.ACS infectious diseases · 2021Article
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- Synthesis of an acyl-acyl carrier protein synthetase inhibitor to study fatty acid recycling.Scientific reports · 2020Article
- Novel Targets for Antimicrobials.Turkish journal of pharmaceutical sciences · 2020Review
- Nonactive-Site Mutations inACS omega · 2020Article
- Critical analysis of antibacterial agents in clinical development.Nature reviews. Microbiology · 2020Review
- Ligand- and Structure-Based Approaches of Escherichia coli FabI Inhibition by Triclosan Derivatives: From Chemical Similarity to Protein Dynamics Influence.ChemMedChem · 2019Article
- Staphylococcus aureus Utilizes Host-Derived Lipoprotein Particles as Sources of Fatty Acids.Journal of bacteriology · 2018Article
- Bacterial fatty acid metabolism in modern antibiotic discovery.Biochimica et biophysica acta. Molecular and cell biology of lipids · 2017Review
- Exogenous fatty acid metabolism in bacteria.Biochimie · 2017Review
- Clinical Relevance of Type II Fatty Acid Synthesis Bypass in Staphylococcus aureus.Antimicrobial agents and chemotherapy · 2017Article
Corrections and comments
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Authors and funding
11 authors at 2 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
MUT056399 is a highly potent new inhibitor of the FabI enzyme of both Staphylococcus aureus and Escherichia coli. In vitro, MUT056399 was very active against S. aureus strains, including methicillin-susceptible S. aureus (MSSA), methicillin-resistant S. aureus (MRSA), linezolid-resistant, and multidrug-resistant strains, with MIC(90)s between 0.03 and 0.12 μg/ml. MUT056399 was also active against coagulase-negative staphylococci, with MIC(90)s between 0.12 and 4 μg/ml. The antibacterial spectrum is consistent with specific FabI inhibition with no activity against bacteria using FabK but activity against FabI-containing Gram-negative bacilli. In vitro, resistant clones of S. aureus were obtained at a low frequency. All of the resistant clones analyzed were found to contain mutations in the fabI gene. In vivo, MUT056399, administered subcutaneously, protected mice from a lethal systemic infection induced by MSSA, MRSA, and vancomycin-intermediate S. aureus strains (50% effective doses ranging from 19.3 mg/kg/day to 49.6 mg/kg/day). In the nonneutropenic murine thigh infection model, the same treatment with MUT056399 reduced the bacterial multiplication of MSSA and MRSA in the thighs of immunocompetent mice. These properties support MUT056399 as a very promising candidate for a novel drug to treat severe staphylococcal infections.
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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.