Linezolid (formerly U-100766) and eperezolid (formerly U-100592) are novel oxazolidinone antimicrobial agents that are active against multi-drug-resistant staphylococci, streptococci, enterococci, corynebacteria, and mycobacteria. Preliminary studies also demonstrated that the compounds inhibited some test strains of anaerobic bacteria. Therefore, we extended the in vitro evaluation of these agents to include a total of 54 different anaerobic species. Minimal inhibitory concentration (MIC) values were determined using a standard agar dilution method for 143 anaerobic bacterial isolates. Eperezolid and linezolid demonstrated potent activity against the anaerobic Gram-positive organisms with most MIC values in the range of 0.25-4 microg/mL. Viridans streptococci demonstrated MICs of 1-2 microg/mL; Peptostreptococcus species and Propionibacterium species were inhibited by =0.25-1 microg/mL. Clostridial species were generally susceptible to the oxazolidinones (MICs of =0.25-8 microg/mL); however, seven strains of Clostridium difficile with linezolid MICs of 16 microg/mL or greater were detected. Against the anaerobic Gram-negative organisms, linezolid was more potent than eperezolid, especially for Bacteroides species. Linezolid inhibited most bacteroides in the range of 2-8 microg/mL, while eperezolid was generally two- to eight-fold less active. Linezolid and eperezolid both demonstrated potent activity against Fusobacterium species,Mobiluncus species,Prevotella intermedia, and Porphyromonas asaccharolytica (MICs of =0.25-0.5 microg/mL). Overall, the oxazolidinones demonstrated a significant level of activity against a number of clinically-important anaerobic bacterial species. Linezolid may potentially provide a broader spectrum of anaerobic coverage than eperezolid due to its greater activity against Bacteroides species.
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http://dx.doi.org/10.1006/anae.1997.0115 | DOI Listing |
Infect Drug Resist
January 2025
Department of Infectious Disease, Changzheng Hospital, Navy Medical University, Shanghai, People's Republic of China.
The Hepatorenal Syndrome-Acute Kidney Injury (HRS-AKI) patients infected with methicillin-resistant (MRSA) urgently require safe and effective treatment options due to their compromised hepatic and renal functions, as well as thrombocytopenia resulting from hypersplenism. In our case, an HRS-AKI patient who underwent continuous renal replacement therapy for fluid overload developed fever with chills. His blood tests indicated elevated C-reactive protein and neutrophils, low platelet count, and bilateral lung infiltrates.
View Article and Find Full Text PDFACS Med Chem Lett
January 2025
Department of Pharmaceutical Chemistry, R. C. Patel Institute of Pharmaceutical Education and Research, Shirpur, Maharashtra 425405, India.
Linezolid, a widely used oxazolidinone antibiotic, exhibits potent activity against resistant bacterial infections but is associated with serotonergic toxicity, primarily due to its inhibition of monoamine oxidase (MAO). MAOs, consisting of MAO-A and MAO-B isoforms, play crucial roles in neurotransmitter metabolism, with implications for neurodegenerative disorders like Parkinson's and Alzheimer's diseases. This study aims to optimize Linezolid's structure to transform it into a selective MAO-B inhibitor.
View Article and Find Full Text PDFEur J Med Chem
January 2025
Lung Cancer Center, Laboratory of Lung Cancer, and Laboratory of Human Diseases and Immunotherapies, West China Hospital, Sichuan University, Chengdu, 610041, China; Institute of Immunology and Inflammation, Frontiers Science Center for Disease-related Molecular Network, West China Hospital, Sichuan University, Chengdu, 610041, China. Electronic address:
The increasing threat of antibiotic resistance has necessitated the development of new antibacterial agents. 33 novel antibacterial agents have been approved by the U.S.
View Article and Find Full Text PDFTransl Clin Pharmacol
December 2024
Department of Clinical Pharmacology and Therapeutics, Seoul National University Bundang Hospital, Seoul National University College of Medicine, Seongnam 13620, Korea.
Unlabelled: Delpazolid is an oxazolidinone-class antibiotic under development for treating diseases caused by antimicrobial-resistant gram-positive bacteria. This study compared the pharmacokinetics (PK) and safety of two formulations of delpazolid 400 mg with distinct excipient compositions: Batch No. 3183817R (test drug) and Batch No.
View Article and Find Full Text PDFInt J Mol Sci
December 2024
Faculty of Soil Science, M.V. Lomonosov Moscow State University, Leninskie Gory, 1, 119991 Moscow, Russia.
The black garden ant () is a widely distributed species across Europe, North America, and North Africa, playing a pivotal role in ecological processes within its diverse habitats. However, the microbiome associated with remains poorly investigated. In the present study, we isolated a novel species, , from the soil of the anthill.
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