Structural features of piperazinyl-linked ciprofloxacin dimers required for activity against drug-resistant strains of Staphylococcus aureus

We previously demonstrated that piperazinyl-linked fluoroquinolone dimers possess potent antibacterial activity against drug-resistant strains of Staphylococcus aureus. In this study, we report the preparation and evaluation of a series of incomplete dimers toward ascertaining structural features of...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2003-07, Vol.13 (13), p.2109-2112
Hauptverfasser:	Kerns, Robert J, Rybak, Michael J, Kaatz, Glenn W, Vaka, Flamur, Cha, Raymond, Grucz, Richard G, Diwadkar, Veena U
Format:	Artikel
Sprache:	eng
Schlagworte:	Anti-Infective Agents - chemical synthesis Anti-Infective Agents - chemistry Anti-Infective Agents - pharmacology Antibacterial agents Antibiotics. Antiinfectious agents. Antiparasitic agents Biological and medical sciences Chromatography, High Pressure Liquid Chromatography, Thin Layer Ciprofloxacin - chemical synthesis Ciprofloxacin - chemistry Ciprofloxacin - pharmacology DNA, Bacterial - drug effects Drug Resistance, Bacterial Medical sciences Mutation - genetics Pharmacology. Drug treatments Pipemidic Acid - chemical synthesis Pipemidic Acid - pharmacology Piperazines - chemical synthesis Piperazines - chemistry Piperazines - pharmacology Staphylococcus aureus - drug effects Staphylococcus aureus - enzymology Staphylococcus aureus - genetics Structure-Activity Relationship Topoisomerase I Inhibitors Topoisomerase II Inhibitors
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Zusammenfassung:	We previously demonstrated that piperazinyl-linked fluoroquinolone dimers possess potent antibacterial activity against drug-resistant strains of Staphylococcus aureus. In this study, we report the preparation and evaluation of a series of incomplete dimers toward ascertaining structural features of piperazinyl-linked ciprofloxacin dimers that render these agents refractory to fluoroquinolone-resistance mechanisms in Staphylococcus aureus. Graphic
ISSN:	0960-894X 1464-3405
DOI:	10.1016/S0960-894X(03)00376-7