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Firoozpour, Loghman,Emami, Saeed,Mansouri, Shahla,Ebrahimabadi, Abdolrasoul H.,Asadipour, Ali,Amini, Mohsen,Saeid-Adeli, Nosratollah,Shafiee, Abbas,Foroumadi, Alireza 대한약학회 2007 Archives of Pharmacal Research Vol.30 No.2
A series of N-[5-(chlorobenzylthio)-1,3,4-thiadiazol-2-yl] piperazinyl quinolones derivatives (4a-I) 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-I 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 ${\mu}$g/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.
Alireza Foroumadi,Loghman Firoozpour,Saeed Emami,Shahla Mansouri,Abdolrasoul H. Ebrahimabadi,Ali Asadipour,Mohsen Amini,Nosratollah Saeid-Adeli,Abbas Shafiee 대한약학회 2007 Archives of Pharmacal Research Vol.30 No.2
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.