Synthesis and antibacterial activity of some novel N-substituted piperazinyl-quinolones.
A series of N-substituted-piperazinyl-quinolones were synthesized and evaluated for in vitro antibacterial activity. Compounds with a 2-(2,4-dichlorophenyl)-2-oxoethyl group attached to the piperazine ring (5a-c) had similar antibacterial activity to the reference drugs, ciprofloxacin, norfloxacin and enoxacin against both Gram-positive and Gram-negative bacteria. The oximes 6a-c and 6g-i were almost less active than corresponding ketones against the tested microorganisms, however the 2,4-difluorophenyl analogues (6g-i) were more active than 2,4-dichlorophenyl derivatives (6a-c). If the hydrogen of oxime is replaced with a benzyl group (6d-f & 6j-l), in-vitro antibacterial activity was decreased against both Gram-positive and Gram-negative bacteria. Generally ciprofloxacin derivatives were more active than norfloxacin and enoxacin derivatives.
Foroumadi
A
A
Department of Medicinal Chemistry, Faculty of Pharmacy, Kerman University of Medical Sciences, Kerman, Iran.
Davood
A
A
Mirzaei
M
M
Emami
S
S
Moshafi
M H
MH
D042462:4-Quinolones; D000890:Anti-Infective Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D001419:Bacteria / Q000187:drug effects; D007202:Indicators and Reagents; D008826:Microbial Sensitivity Tests; D010879:Piperazines / Q000138:chemical synthesis* / Q000494:pharmacology*; D012015:Reference Standards; D013055:Spectrophotometry, Infrared
D042462:4-Quinolones; D000890:Anti-Infective Agents; D007202:Indicators and Reagents; D010879:Piperazines