Synthesis and antibacterial activity of new fluoroquinolones containing a substituted N-(phenethyl)piperazine moiety.
N-(Phenethyl)piperazinyl quinolone derivatives that bear a methoxyimino-substituent have been synthesized and evaluated for antimicrobial activity against Gram-positive and Gram-negative microorganisms. In addition, to define structure-activity relationships, ciprofloxacin derivatives containing 2-oxo-2-phenylethyl or 2-hydroxyimino-2-phenylethyl moieties at N-4 position of piperazine ring were prepared and tested. Ciprofloxacin derivatives, containing a N-(chloro-substituted phenethyl) residue, showed in vitro Gram-positive and Gram-negative activity generally comparable or superior to that of reference quinolones.
Foroumadi
Alireza
A
Faculty of Pharmacy and Pharmaceutical Sciences Research Center, Tehran University of Medical Sciences, Tehran 14174, Iran. aforoumadi@yahoo.com
Ghodsi
Shahram
S
Emami
Saeed
S
Najjari
Somayyeh
S
Samadi
Nasrin
N
Faramarzi
Mohammad Ali
MA
Beikmohammadi
Leila
L
Shirazi
Farshad H
FH
Shafiee
Abbas
A
D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D024841:Fluoroquinolones / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D006090:Gram-Negative Bacteria / Q000187:drug effects*; D006094:Gram-Positive Bacteria / Q000187:drug effects*; D066298:In Vitro Techniques; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D010879:Piperazines / Q000737:chemistry*; D013237:Stereoisomerism; D013329:Structure-Activity Relationship
D000900:Anti-Bacterial Agents; D024841:Fluoroquinolones; D010879:Piperazines