Synthesis and Antibacterial Activity of Quinolone‐Based Compounds Containing a Coumarin Moiety

Abstract

A new series of quinolone-based compounds containing a coumarin moiety have been synthesized and studied for their antibacterial activity against a panel of gram-positive and gram-negative bacteria, including methicillin-resistant Staphylococcus aureus (MRSA). The results of the antibacterial evaluation of N-[2-(coumarin-3-yl)ethyl]piperazinyl quinolone derivatives in comparison with parent quinolones (norfloxacin, ciprofloxacin, and enoxacin) indicated that N-[2-(coumarin-3-yl)-2-oxoethyl]ciprofloxacin derivative (compound 8b) showed comparable or more potent antibacterial activity with respect to the reference drugs against the test strains. Generally, in both gram-positive and gram-negative bacteria, better results are obtained with cyclopropyl at the N-1 position of the quinolone ring and 2-oxo- on the ethyl spacer of coumarin and piperazine rings.