Oxazolidinone-containing Hybrids with Antibacterial Activity against Methicillin-resistant Staphylococcus aureus (MRSA): A Mini-review

(E-pub Ahead of Print)

Author(s): Dan Jiang, Bi Liu, Tao Gao*

Journal Name: Current Topics in Medicinal Chemistry

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The increasing danger by methicillin-resistant Staphylococcus aureus (MRSA) and the limited therapeutic op-tions towards invasive MRSA infections make an urgent demand for the development of novel anti-MRSA agents. Oxazol-idinone derivatives could inhibit protein synthesis by acting on the ribosomal 50S subunit of the bacteria and prevent for-mation of a functional 70S initiation complex, so oxazolidinones are a novel class of antimicrobial agents with potential activity against a wide range of clinically significant multidrug-resistant Gram-positive pathogens. However, oxazolidinones such as linezolid are associated with significant adverse events, and myelosuppression represents the main unfavorable side effects. Moreover, MRSA isolates which are resistant to oxazolidinones have already emerged. Hybridization of oxazoli-dinone with other antibacterial pharmacophores has the potential to interact with multiple targets or to counterbalance the known side effects associated with each pharmacophore. Thus, oxazolidinone-containing hybrids are useful scaffolds for the development of novel anti-MRSA agents. This review covers the recent advances of oxazolidinone-containing hybrids with anti-MRSA activity developed in last decade to set up

Keywords: Oxazolidinone, Hybrid compounds, Antibacterial, Methicillin-resistant Staphylococcus aureus, Structure-activity re-lationships, Toxicity

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Article Details

Published on: 12 November, 2020
(E-pub Ahead of Print)
DOI: 10.2174/1568026620999201113104935
Price: $95

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