Synthesis and In‐vitro Antibacterial Activity of N‐Piperazinyl Quinolone Derivatives with a 2‐Thienyl Group

摘要: Background and the purpose of study: Fluoroquinolones are an important group antimicrobial agents that used widely in treatment various infectious diseases. The present study was to synthesize new N-piperazinyl quinolone derivatives with 5-chloro-2-theinyl having possible activity. Methods: Reaction ciprofloxacin (1), norfloxacin (2) enoxacin (3) α-bromoketone 10 or α-bromooxime 11a-c DMF, presence NaHCO3 at room temperature, afforded corresponding ketones 4a-c oxime 5-7(a-c), respectively. Results major conclusion: synthesized compounds were tested against a series Grampositive Gram-negative bacteria. results MIC tests both Gram-positive bacteria revealed (compounds 4a, 5a, 6a 7a) more active than analogues. Compound containing N-[2-(5-chlorothiophen-2-yl)-2-hydroxyiminoethyl] residue provided high vitro antibacterial activity bacteria, 0.06, 0.125, 0.5 0.125 µg/mL S. aureus, epidermidis, E. feacalis B. subtilis, Its found be 4 8 times better reference drug (ciprofloxacin) all