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J Med Chem. 1996 Dec 6;39(25):4952-7.

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

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1
Istituto di Chimica e Tecnologia del Farmaco, Università di Perugia, Italy.

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.

PMID:
8960555
DOI:
10.1021/jm960414w
[Indexed for MEDLINE]
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