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KMID : 0043320070300020138
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Archives of Pharmacal Research
2007 Volume.30 No. 2 p.138 ~ p.145
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Synthesis and Antibacterial Activity of N-[5-(chlorobenzylthio)-1,3,4-thiadiazol-2-yl] Piperazinyl Quinolone Derivatives
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Foroumadi Alireza
Firoozpour Loghman
Emami Saeed
Mansouri Shahla
Ebrahimabadi Abdolrasoul H.
Asadipour Ali
Amini Mohsen
Saeid-Adeli Nosratollah
Shafiee Abbas
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Abstract
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A series of N-[5-(chlorobenzylthio)-1,3,4-thiadiazol-2-yl] piperazinyl quinolone derivatives (4a-l) have been synthesized by reaction of piperazinyl quinolones with 5-chloro-2-(chlorobenzylthio)-1,3,4-thiadiazoles. Their structures were confirmed by elemental analysis, IR and NMR spectra. The antibacterial activities of 4a-l against a variety of Gram-positive and Gram-negative bacteria were determined. Several compounds showed a good antibacterial activity against Gram-positive bacteria among which, compound 4e with a 2-chlorobenzylthio moiety in ciprofloxacin derivative, exhibited high activities against Staphylococcus aureus and Staphylococcus epidermidis (MIC=0.06 μg/mL). The structure-activity relationship (SAR) study revealed that the position of chlorine atom on benzyl moiety would dramatically affect the antibacterial activities of the synthesized compounds.
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KEYWORD
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Quinolones, N-substituted piperazinyl quinolones, In vitro antibacterial activity, Staphylococcus aureus, Staphylococcus epidermidis, 1, 3, 4-thiadiazole
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