Potent 6-desfluoro-8-methylquinolones as new lead compounds in antibacterial chemotherapy

Journal of Medicinal Chemistry
V CecchettiT Xin

Abstract

In a furtherance of our SAR study on the C-6 position of quinolone antibacterials, a series of 6-desfluoro-8-methylquinolones were synthesized and evaluated for their in vitro antimicrobial activity. As a result of this study, compounds with strong activity against Gram-positive bacteria, including ciprofloxacin-resistant and methicillin-resistant Staphylococcus aureus, were identified. The best Gram-positive antibacterial activity was exhibited by piperidinyl derivative 6c, which was 17 times more potent than ciprofloxacin and displayed extremely high activity against Streptococcus pneumoniae with an MIC value of <0.016 microg/mL. Thus, we have shown that substituent combinations in the quinolone ring, excluding the C-6 fluorine atom, might produce powerful antibacterial agents.

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Citations

Nov 30, 2013·Spectrochimica Acta. Part A, Molecular and Biomolecular Spectroscopy·Y Sheena MaryPavel Pazdera
Jul 15, 2004·Toxicology in Vitro : an International Journal Published in Association with BIBRA·G ViolaV Cecchetti
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Jun 7, 2014·Journal of Medicinal Chemistry·Manuela DonalisioOriana Tabarrini

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