Linezolid is an oxazolidinone antibiotic and is effective against Gram-positive bacteria including certain strains of methicillin-resistant Staphylococcus aureus (MRSA). Linezolid was discovered in the mid-1990s and was approved for commercial use in 2000. The crystal structure was elucidated in 2008 by Yale researchers. The compound is synthetic, and many apporaches for Linezolid synthesis have been reported. It is active against Gram-positive bacteria including certain methicillin-resistant Staphylococcus aureus (MRSA).
| Mechanism of Action | Linezolid inhibits protein synthesis by binding to the 50S ribosomal subunit (23S rRNA) which prevents formation of the 70S initiation complex thus inhibiting mRNA translation. The initiation complex is composed of the 30S, 50S ribosome subunits, tRNAa nd mRNA. Since this mechanism is unique, cross-resistance between linezolid and other protein synthesis inhibitors is highly infrequent or nonexistent. It is also a nonselective monoamine oxidase (MAO) inhibitor displaying nonselective, reversible binding. |
| Spectrum | Linezolid is active against Gram-positive bacteria including certain strains of methicillin-resistant Staphylococcus aureus (MRSA). It is bacteriocidal against the majority of streptococcal strains and bacteriostatic against staphylococci and enterococci. It is also active in vitro against several mycobacteria. In vitro, it is active on select Gram-negative bacteria but does not have any activity in vivo on clinically significant species. |
| Eukaryotic Cell Culture Applications | Linezolid inhibits cytokine production from human peripheral blood monocytes in a dose-dependent manner. Linezolid was found to modify the acute phase inflammatory response. Linezolid inhibits cytokine production from human peripheral blood monocytes in a dose-dependent manner (Garcia-Roca et al, 2006). |
| Molecular Formula | C16H20FN3O4 |
| References |
Ament PW (2002) Linezolid: Its role in the treatment of Gram-positive, drug-resistant bacterial infections. Amer. Family Phys. 65(4):663-671 PMID 11871684 Garcia-Roca P, Mancilla-Ramirez J, Santos-Segura A, Fernandez-Aviles M, Calderon-Jaimes E (2006) Linezolid diminishes inflammatory cytokine production from human peripheral blood mononuclear cells. 37(1):31-35 PMID 16314183 Herrmann DJ et al (2008) Linezolid for the treatment of drug-resistant infections. Expert Rev. Anti Infect. Ther. 6(6):825-648 PMID 19053895 Shinabarger DL (1997) Mechanism of action of Oxazolidinones: Effects of Linezolid and Eperezolid on translation reactions. Antimicrob. Agents Chemother. 41(10):2132-2136 PMID 9333037 |