BACKGROUND Linezolid is a bacteriostatic oxazolidinone antibiotic that has been proven to be effective for the treatment of patients with pneumonia, skin and soft tissue infections, and possibly bacteraemia, due to Gram-positive cocci. However, the drug is sometimes used for the treatment of patients with endocarditis due to Gram-positive cocci resistant to other antibiotics. METHODS We carri...

OBJECTIVES Linezolid, the first available agent in the new class of oxazolidinone antibiotics, represents a significant advance in the management options available for combating methicillin-resistant Staphylococcus aureus (MRSA) infections. In the UK it was launched for clinical use in 2001. The aim of this study was to audit the clinical use of linezolid and compliance with the guidelines of t...

Oxazolidinone antibiotics have activity against Mycobacterium tuberculosis. Linezolid, the only marketed oxazolidinone, has been used off-label in combination regimens to treat multidrug-resistant tuberculosis, but its precise contribution to the efficacy of such combinations is unclear. Another oxazolidinone, PNU-100480, has been demonstrated to have more potent activity in vitro and in a muri...

The oxazolidinones are a novel class of antimicrobial agents that target protein synthesis in a wide spectrum of gram-positive and anaerobic bacteria. The oxazolidinone PNU-100766 (linezolid) inhibits the binding of fMet-tRNA to 70S ribosomes. Mutations to oxazolidinone resistance in Halobacterium halobium, Staphylococcus aureus, and Escherichia coli map at or near domain V of the 23S rRNA, sug...

Urokinase-type plasminogen activator (uPA), a highly restricted serine protease, plays an important role in the regulation of diverse physiologic and pathologic processes. Strong clinical and experimental evidence has shown that elevated uPA expression is associated with cancer progression, metastasis, and shortened survival in patients. uPA has been considered as a promising molecular target f...

Oxazolidinone-functionalized enecarbamates undergo diastereoselective E/Z photoisomerization upon direct and triplet sensitized irradiations with chiral/achiral sensitizers, showing that the enhanced product diastereoselectivity depends on the solvent and temperature.

P754 Citation: Clinical Microbiology and Infection Volume 8, Supplement 1, 2002 AZD2563, a new oxazolidinone: bactericidal activity and synergy studies with gentamicin and vancomycin against staphylococci and streptococci R. Jones, T. Anderegg, L. Deshpande, D. Biedenbach

The geometry of the double bond in oxazolidinone-substituted ene carbamates controls the mode selectivity (ene reaction versus [2+2] cycloaddition) of singlet oxygen through stereoelectronic effects, whereas the chiral auxiliary provides high diastereoselectivity through steric shielding.

Rotaxane-structure-specific Pd-catalyzed rearrangement of propargyl or allyl urethane groups to oxazolidinone moieties proceeded efficiently. The conversion took place successively by the translation of the wheel along the axle, thus providing a novel macrocyclic catalytic system.

P1045 Citation: Clinical Microbiology and Infection Volume 8, Supplement 1, 2002 Validation of commercial dry-form panels (sensititre) for the susceptibility testing of AZD2563, a new long-acting oxazolidinone R. Jones, T. Anderegg, D. Biedenbach, P. Rhomberg