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  • Title: Design, synthesis and biological evaluation of oxazolidinone-quinolone hybrids.
    Author: Hubschwerlen C, Specklin JL, Sigwalt C, Schroeder S, Locher HH.
    Journal: Bioorg Med Chem; 2003 May 15; 11(10):2313-9. PubMed ID: 12713843.
    Abstract:
    Oxazolidinone-quinolone hybrids that combine the pharmacophores of a quinolone and an oxazolidinone were synthesised and shown to be active against a variety of resistant and susceptible Gram-positive and fastidious Gram-negative organisms. The best compounds in this series overcome all types of resistance in relevant clinical Gram-positive pathogens. The nature of the spacer greatly influences the antibacterial activity. The dual mode of action could be demonstrated for compounds having a piperazinyl spacer. Antibacterial activity was higher at acidic pH.
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