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The Oxazolidinones

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Antibacterials

Part of the book series: Topics in Medicinal Chemistry ((TMC,volume 26))

Abstract

The oxazolidinones, exemplified by linezolid and now tedizolid phosphate, are established as successful clinical agents for the treatment of a variety of serious infections caused by Gram-positive pathogens. Out of more than one dozen oxazolidinone drug candidates tested in clinical trials over the last 20+ years, only these two agents have exhibited the optimal balance of potency, pharmacokinetic behavior, and safety to become marketed antibacterial agents. The reason for this situation is discussed in the context of a new wave of emerging candidate drugs. An assessment of these nascent oxazolidinones is provided. Progress in the areas of structure-activity relationships (SAR), mechanism of action (MOA), safety characteristics, and resistance development is discussed. Finally, we speculate on the future of the oxazolidinones as a class of antibacterial agents with continuing therapeutic utility.

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  1. Department of Chemistry and Biochemistry, Calvin College, 1726 Knollcrest Circle SE, Grand Rapids, MI, 49546, USA

    Michael R. Barbachyn

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  1. Department of Chemistry & Biochemistry, University of Notre Dame, Notre Dame, Indiana, USA

    Jed F. Fisher

  2. Department of Chemistry & Biochemistry, University of Notre Dame, Notre Dame, Indiana, USA

    Shahriar Mobashery

  3. Department of Chemistry & Biochemistry, University of Notre Dame, Notre Dame, Indiana, USA

    Marvin J. Miller

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Barbachyn, M.R. (2017). The Oxazolidinones. In: Fisher, J., Mobashery, S., Miller, M. (eds) Antibacterials. Topics in Medicinal Chemistry, vol 26. Springer, Cham. https://doi.org/10.1007/7355_2017_15

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