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Issue 1, 2019
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Antibacterial properties and clinical potential of pleuromutilins

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Covering: up to 2018

Pleuromutilins are a clinically validated class of antibiotics derived from the fungal diterpene (+)-pleuromutilin (1). Pleuromutilins inhibit bacterial protein synthesis by binding to the peptidyl transferase center (PTC) of the ribosome. In this review we summarize the biosynthesis and recent total syntheses of (+)-pleuromutilin (1). We review the mode of interaction of pleuromutilins with the bacterial ribosome, which involves binding of the C14 extension and the tricyclic core to the P and A sites of the PTC, respectively. We provide an overview of existing clinical agents, and discuss the three primary modes of bacterial resistance (mutations in ribosomal protein L3, Cfr methylation, and efflux). Finally we collect structure–activity relationships from publicly available reports, and close with some forward looking statements regarding future development.

Graphical abstract: Antibacterial properties and clinical potential of pleuromutilins

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Publication details

The article was received on 01 May 2018 and first published on 06 Jul 2018

Article type: Review Article
DOI: 10.1039/C8NP00042E
Citation: Nat. Prod. Rep., 2019,36, 220-247

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    Antibacterial properties and clinical potential of pleuromutilins

    O. Goethe, A. Heuer, X. Ma, Z. Wang and S. B. Herzon, Nat. Prod. Rep., 2019, 36, 220
    DOI: 10.1039/C8NP00042E

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