Synthesis and antibacterial activity of quinolone-based compounds containing a coumarin moiety.
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.
Emami
Saeed
S
Department of Medicinal Chemistry, Mazandaran University of Medical Sciences, Sari, Iran. sd_emami@yahoo.com
Foroumadi
Alireza
A
Faramarzi
Mohammad A
MA
Samadi
Nasrin
N
D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D015169:Colony Count, Microbial; D003374:Coumarins / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D006090:Gram-Negative Bacteria / Q000187:drug effects; D006094:Gram-Positive Bacteria / Q000187:drug effects; D016106:Methicillin Resistance; D008826:Microbial Sensitivity Tests; D015363:Quinolones / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D013055:Spectrophotometry, Infrared; D013203:Staphylococcal Infections / Q000188:drug therapy; D013329:Structure-Activity Relationship
D000900:Anti-Bacterial Agents; D003374:Coumarins; D015363:Quinolones