Piperazinyl-linked fluoroquinolone dimers possessing potent antibacterial activity against drug-resistant strains of Staphylococcus aureus

The synthesis of symmetric and asymmetric piperazinyl-linked dimers of the fluoroquinolone class of antibiotics is described. Specific dimers are shown to possess potent antibacterial activity against drug-resistant strains of Staphylococcus aureus, including strains possessing resistance due to the...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2003-05, Vol.13 (10), p.1745-1749
Hauptverfasser:	Kerns, Robert J., Rybak, Michael J., Kaatz, Glenn W., Vaka, Flamur, Cha, Raymond, Grucz, Richard G., Diwadkar, Veena U., Ward, Tracey D.
Format:	Artikel
Sprache:	eng
Schlagworte:	Anti-Bacterial Agents - chemical synthesis Anti-Bacterial Agents - pharmacology Antibacterial agents Antibiotics. Antiinfectious agents. Antiparasitic agents Bacterial Proteins Biological and medical sciences Cross-Linking Reagents - chemistry Dimerization DNA Topoisomerase IV - genetics Drug Resistance, Bacterial Fluoroquinolones - chemical synthesis Fluoroquinolones - pharmacology Medical sciences Microbial Sensitivity Tests Multidrug Resistance-Associated Proteins Pharmacology. Drug treatments Piperazines - chemistry Staphylococcus aureus - drug effects Structure-Activity Relationship
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Zusammenfassung:	The synthesis of symmetric and asymmetric piperazinyl-linked dimers of the fluoroquinolone class of antibiotics is described. Specific dimers are shown to possess potent antibacterial activity against drug-resistant strains of Staphylococcus aureus, including strains possessing resistance due to the NorA multidrug efflux pump and a mutation in the quinolone resistance-determining region of topoisomerase IV. Graphic
ISSN:	0960-894X 1464-3405
DOI:	10.1016/S0960-894X(03)00208-7