Design, synthesis, antibacterial activity and physicochemical parameters of novel N-4-piperazinyl derivatives of norfloxacin.
We report herein the synthesis of some N-Mannich bases in addition to different N-4 substituents of norfloxacin. The antibacterial activities of the newly synthesized compounds were evaluated and correlated with their physicochemical properties. Results revealed that some of the tested compounds exhibited better inhibitory activities than the reference antibiotic norfloxacin against Pseudomonas aeruginosa, Escherichia coli, Klebsiella pneumonia and Staphylococcus aureus strains. Correlation results showed that there is no single physicochemical parameter that can determine the effect of N-4 piperazinyl group on the activity of these fluoroquinolones, where lipophilicity, molecular mass and electronic factors may influence the activity.
Department of Medicinal Chemistry, Faculty of Pharmacy, Minia University, 61519-Minia, Egypt. gamalaburahma@yahoo.com
Gamal el-Din A A
Gel-D
Abuo-Rahma
Hatem A
HA
Sarhan
Gamal F M
GF
Gad
D000900:Anti-Bacterial Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D055598:Chemical Phenomena; D015195:Drug Design; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D009643:Norfloxacin / Q000737:chemistry*; D010879:Piperazines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D011549:Pseudomonas / Q000187:drug effects*
D000900:Anti-Bacterial Agents; D010879:Piperazines; D009643:Norfloxacin