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Updated: Jun 13, 2026

High Throughput, Real-time, Dual-readout Testing of Intracellular Antimicrobial Activity and Eukaryotic Cell Cytotoxicity
Published on: November 16, 2016
Antibacterial oxazolidinones: emerging structure-toxicity relationships
1Department of Pharmaceutical Chemistry and the Small Molecule Discovery Center, University of California, San Francisco, 1700 4th Street, San Francisco, CA 94158, USA. adam.renslo@ucsf.edu
Abstract:
The oxazolidinones are an important class of synthetic bacterial protein synthesis inhibitors with activity against Gram-positive and some fastidious Gram-negative bacteria. Key toxicological issues with the class include reversible inhibition of monoamine oxidase enzymes and reversible myelosuppression that can occur in patients treated for longer than the recommended course of therapy. Recent studies have uncovered the likely molecular mechanism underlying oxazolidinone-related myelosuppression and other toxicities, and these will be discussed here. Also reviewed are recent reports of structural modifications that can attenuate one or more of the undesired effects of oxazolidinones, while retaining the desired antibacterial effect.
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