Journal
BIOORGANIC & MEDICINAL CHEMISTRY
Volume 14, Issue 10, Pages 3421-3427Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2005.12.058
Keywords
quinolones; N-substituted piperazinylquinolones; in vitro antibacterial activity
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A number of N-substituted piperazinylquinolone derivatives were synthesized and evaluated for antibacterial activity against Gram-positive and Gram-negative bacteria. Preliminary results indicated that most compounds tested in this study demonstrated comparable or better activity against Staphylococcus aureus and Staphylococcus epidermidis than their parent piperazinylquinolones as reference drugs. Among these derivatives, ciprofloxacin derivative 5a, containing N-[2-[5-(methylthio)thiophen-2-yl]-2-oxoethyl] residue, showed significant improvement of potency against staphylococci, maintaining Gram-negative coverage. (c) 2006 Elsevier Ltd. All rights reserved.
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