Title:Oxazolidinone-containing Hybrids with Antibacterial Activity against Methicillin-resistant Staphylococcus aureus (MRSA): A Mini-review
Volume: 21
Issue: 27
Author(s): Dan Jiang, Bi Liu and Tao Gao*
Affiliation:
- Hubei Key Laboratory of Radiation Chemistry and Functional Materials, School of Nuclear Technology and Chemistry & Biology, Hubei University of Science and Technology, Xian Ning 437100,China
Keywords:
Antibacterial, Hybrid compounds, Methicillin-resistant Staphylococcus aureus, Oxazolidinone, Structure-activity
relationships, Gram-positive bacteria.
Abstract: The increasing danger of methicillin-resistant Staphylococcus aureus (MRSA) and the
limited therapeutic options for invasive MRSA infections make an urgent demand for the development
of novel anti-MRSA agents. Oxazolidinone derivatives could inhibit protein synthesis by acting
on the ribosomal 50S subunit of the bacteria and prevent the formation 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 that are resistant to oxazolidinones
have already emerged. Hybridization of oxazolidinone 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 oxazolidinonecontaining
hybrids with anti-MRSA activity developed in the last decade to set up the direction for
the design and development of oxazolidinone-containing hybrids with high efficiency and low toxicity.