Synthesis and antibacterial activity of N-[5-chlorobenzylthio-1,3,4-thiadiazol-2-yl] piperazinyl quinolone derivatives

被引：0
作者：
Alireza Foroumadi
Loghman Firoozpour
Saeed Emami
Shahla Mansouri
Abdolrasoul H. Ebrahimabadi
Ali Asadipour
Mohsen Amini
Nosratollah Saeid-Adeli
Abbas Shafiee
机构：
[1] Tehran University of Medical Sciences,Pharmaceutical Sciences Research Center
[2] Kerman University of Medical Sciences,Department of Medicinal Chemistry, Faculty of Pharmacy
[3] Mazandaran University of Medical Sciences,Department of Medicinal Chemistry, Faculty of Pharmacy
[4] Kerman University of Medical Sciences,Department of Microbiology, Faculty of Medicine
来源：
Archives of Pharmacal Research | 2007年 / 30卷
关键词：
Quinolones; -substituted piperazinyl quinolones; antibacterial activity; 1,3,4-thiadiazole;
D O I：
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摘要：
A series ofN-[5-(chlorobenzylthio)-1,3,4-thiadiazol-2-yl] piperazinyl quinolone derivatives (4a-1) have been synthesized by reaction of piperazinyl quinolones with 5-chloro-2-(chloroben-zylthio)-1,3,4-thiadiazoles. Their structures were confirmed by elemental analysis, IR and NMR spectra. The antibacterial activities of4a-1 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 againstStaphylococcus aureus andStaphylococcus 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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