Synthesis and in vitro antibacterial evaluation of N-[5-(5-nitro-2-thienyl)-1,3,4-thiadiazole-2-yl] piperazinyl quinolones.
A series of N-[5-(5-nitro-2-thienyl)-1,3,4-thiadiazole-2-yl]piperazinyl quinolones (7a-c) were synthesized and evaluated for in vitro antibacterial activity against some Gram-positive and Gram-negative bacteria. The antibacterial data revealed that compounds 7a-c had strong and better activity against tested Gram-positive organisms than the reference quinolones such as ciprofloxacin, norfloxacin and enoxacin. However, all three compounds were nearly inactive against Gram-negative bacteria. Compound 7a (ciprofloxacin analogue) was the most active compound against Gram-positive bacteria (MIC=0.008-0.015 mug mL(-1)).
Foroumadi
Alireza
A
Department of Medicinal Chemistry, Faculty of Pharmacy, Kerman University of Medical Sciences, Haft Bagh Street, Kerman, Iran. aforoumadi@yahoo.com
Mansouri
Shahla
S
Kiani
Zahra
Z
Rahmani
Afsaneh
A
D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D001419:Bacteria / Q000187:drug effects; D002939:Ciprofloxacin / Q000494:pharmacology; D015365:Enoxacin / Q000494:pharmacology; D008826:Microbial Sensitivity Tests; D009643:Norfloxacin / Q000494:pharmacology; D000077489:Piperazine; D010879:Piperazines / Q000737:chemistry*; D015363:Quinolones / Q000138:chemical synthesis / Q000494:pharmacology*
D000900:Anti-Bacterial Agents; D010879:Piperazines; D015363:Quinolones; D000077489:Piperazine; D015365:Enoxacin; D002939:Ciprofloxacin; D009643:Norfloxacin