Linezolid(also known as PNU-100766, U-100766) is a prototype of the oxazolidinone antimicrobials against a wide range of Gram-positive bacteria, including resistant strains of several species, such as MRSA, penicillin-resistant pneumococci, vancomycin-resistant enterococci, many different streptococci, various anaerobic bacteria, and several mycobacteria. It binds to a site on the bacterial 23S ribosomal RNA of the 50S subunit and prevents the formation of a functional 70S initiation complex, thus inhibiting bacterial mRNA translation. Linezolid is also a weak, reversible, nonselective inhibitor of monoamine oxidase.
Synthesis and Antibacterial Activity of U-100592 and U-100766, Two Oxazolidinone Antibacterial Agents for the Potential Treatment of Multidrug-Resistant Gram-Positive Bacterial Infections.
In vivo activities of U-100592 and U-100766, novel oxazolidinone antimicrobial agents, against experimental bacterial infections.
Linezolid versus vancomycin for the treatment of methicillin-resistant Staphylococcus aureus infections.
Clinical update on linezolid in the treatment of Gram-positive bacterial infections.
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