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  • Title: Preparation and antimicrobial assessment of 2-thioether-linked quinolonyl-carbapenems.
    Author: Hershberger PM, Switzer AG, Yelm KE, Coleman MC, Devries CA, Rourke FJ, Davis BW, Kraft WG, Twinem TL, Koenigs PM, Paule SM, Siehnel RJ, Zoutendam PH, Imbus R, Demuth TP.
    Journal: J Antibiot (Tokyo); 1998 Sep; 51(9):857-71. PubMed ID: 9820237.
    Abstract:
    This reports the synthesis and in vitro antimicrobial properties of a series of 2-thioether-linked quinolonyl-carbapenems. Although the title compounds exhibited broad spectrum activity, the MICs were generally higher than those observed for selected benchmark carbapenems, quinolonyl-penems, and quinolones. Enzyme assays suggested that the title compounds are potent inhibitors of penicillin binding proteins and inefficient inhibitors of bacterial DNA-gyrase. Uptake studies indicated that the new compounds are not substrates for the norA encoded quinolone efflux pump.
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