Comparison of in vitro activities of fluoroquinolone-like 2,4- and 1,3-diones

Lisa M. Oppegard, Kathryn R. Streck, Jonathan D. Rosen, Heidi A. Schwanz, Karl Drlica, Robert J. Kerns, Hiroshi Hiasa

Research output: Contribution to journalArticlepeer-review

22 Scopus citations

Abstract

Bacterial resistance presents a difficult issue for fluoroquinolone treatment of bacterial infections. In previous work, we reported that 8-methoxy-quinazoline-2,4-diones are active against quinolone-resistant mutants of Escherichia coli. Here, we demonstrate the activity of a representative 8-methoxy-quinazoline-2,4-dione against quinolone-resistant gyrases. Furthermore, 8-methoxy-quinazoline-2,4-dione and other diones are shown to inhibit Staphylococcus aureus gyrase and topoisomerase IV with similar degrees of efficacy, suggesting that the diones might act as dual-targeting agents against S. aureus.

Original languageEnglish (US)
Pages (from-to)3011-3014
Number of pages4
JournalAntimicrobial agents and chemotherapy
Volume54
Issue number7
DOIs
StatePublished - Jul 2010

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