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.
MeSH terms
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Bacterial Proteins / drug effects
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Carbapenems / chemical synthesis
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Carbapenems / chemistry*
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Carbapenems / pharmacology*
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Carrier Proteins / drug effects
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Cell Division
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Gram-Negative Bacteria / drug effects*
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Gram-Negative Bacteria / enzymology
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Gram-Positive Bacteria / drug effects*
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Gram-Positive Bacteria / enzymology
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Hexosyltransferases / drug effects
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Microbial Sensitivity Tests
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Multidrug Resistance-Associated Proteins
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Multienzyme Complexes / drug effects
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Muramoylpentapeptide Carboxypeptidase / drug effects
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Penicillin-Binding Proteins
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Peptidyl Transferases / drug effects
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Quinolones / chemistry*
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Structure-Activity Relationship
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Topoisomerase II Inhibitors
Substances
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Bacterial Proteins
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Carbapenems
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Carrier Proteins
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Multidrug Resistance-Associated Proteins
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Multienzyme Complexes
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PGE-5428060
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Penicillin-Binding Proteins
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Quinolones
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Topoisomerase II Inhibitors
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NorA protein, Staphylococcus
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Peptidyl Transferases
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Hexosyltransferases
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Muramoylpentapeptide Carboxypeptidase