Synthesis and antibacterial activity of new N-[2-(thiophen-3-yl)ethyl] piperazinyl quinolones.
As a part of continuing search for potential antibacterial agents in the quinolones field, we have synthesized novel quinolone agents bearing N-[2-(thiophen-3-yl)ethyl] piperazinyl moiety in the 7-position of the quinolone ring. In vitro antibacterial evaluation of the target compounds showed that N-[2-(thiophen-3-yl)ethyl] group attached to piperazine ring served as promising C-7 substituent for piperazinyl quinolone antibacterials. Among these derivatives, ciprofloxacin analogues, containing N-[2-(thiophen-3-yl)-2-hydroxyiminoethyl] or N-[2-(thiophen-3-yl)-2-methoxyiminoethyl] residue provided a high inhibition against all the tested Gram-positive organisms including methicillin-resistant Staphylococcus aureus comparable or superior with respect to the reference drugs norfloxacin and ciprofloxacin.
Letafat
Bahram
B
Department of Chemistry, Islamic Azad University, Central Tehran-Branch, Tehran, Iran.
Emami
Saeed
S
Mohammadhosseini
Negar
N
Faramarzi
Mohammad Ali
MA
Samadi
Nasrin
N
Shafiee
Abbas
A
Foroumadi
Alireza
A
D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D009682:Magnetic Resonance Spectroscopy; D008826:Microbial Sensitivity Tests; D015363:Quinolones / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D013055:Spectrophotometry, Infrared
D000900:Anti-Bacterial Agents; D015363:Quinolones