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  • Title: Novel oxazolidinone-quinolone hybrid antimicrobials.
    Author: Gordeev MF, Hackbarth C, Barbachyn MR, Banitt LS, Gage JR, Luehr GW, Gomez M, Trias J, Morin SE, Zurenko GE, Parker CN, Evans JM, White RJ, Patel DV.
    Journal: Bioorg Med Chem Lett; 2003 Dec 01; 13(23):4213-6. PubMed ID: 14623004.
    Abstract:
    Antimicrobial compounds incorporating oxazolidinone and quinolone pharmacophore substructures have been synthesized and evaluated. Representative analogues 2, 5, and 6 display an improved potency versus linezolid against gram-positive and fastidious gram-negative pathogens. The compounds are also active against linezolid- and ciprofloxacin-resistant Staphylococcus aureus and Enterococcus faecium strains. The MOA for these new antimicrobials is consistent with a combination of protein synthesis and gyrase A/topoisomerase IV inhibition, with a structure-dependent degree of the contribution from each inhibitory mechanism.
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