Preparation and antimicrobial assessment of 2-thioether-linked quinolonyl-carbapenems.

Autor: Hershberger PM; Procter & Gamble Pharmaceuticals, Health Care Research Center, Mason, OH 45040-8006, USA., 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 Jr
Jazyk: angličtina
Zdroj: The Journal of antibiotics [J Antibiot (Tokyo)] 1998 Sep; Vol. 51 (9), pp. 857-71.
DOI: 10.7164/antibiotics.51.857
Abstrakt: 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.
Databáze: MEDLINE