PREPARATION AND ANTIMICROBIAL ASSESSMENT OF 2-THIOETHER-LINKED QUINOLONYL-CARBAPENEMS

This reports the synthesis and in vitro antimicrobial properties of a series of 2-thioether-linked quinolonyl-carbapenems. Although the titl e compounds exhibited broad spectrum activity, the MICs were generally higher than those observed for selected benchmark carbapenems, quinol onyl-penems, and quinolones. Enzyme assays suggested that the title co mpounds are potent inhibitors of penicillin binding proteins and ineff icient inhibitors of bacterial DNA-gyrase. Uptake studies indicated th at the new compounds are not substrates for the norA encoded quinolone efflux pump.