Design, synthesis, antibacterial activity and physicochemical parameters of novel N-4-piperazinyl derivatives of norfloxacin

被引：71

作者：

Abuo-Rahma, Gamal El-Din A. A. ^{[1
]}

Sarhan, Hatem. A. ^{[2
]}

Gad, Gamal F. M. ^{[3
]}

机构：

[1] Menia Univ, Fac Pharm, Dept Med Chem, Al Minya 61519, Egypt

[2] Menia Univ, Fac Pharm, Dept Pharmaceut, Al Minya 61519, Egypt

[3] Menia Univ, Fac Pharm, Dept Microbiol, Al Minya 61519, Egypt

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2009年 / 17卷 / 11期

关键词：

Norfloxacin; Antibacterial; Mannich bases; Physicochemical properties; PARTITION-COEFFICIENTS; MANNICH-BASES; DNA GYRASE; FLUOROQUINOLONE DERIVATIVES; STAPHYLOCOCCUS-AUREUS; HOMOLOGOUS SERIES; ESCHERICHIA-COLI; ACCUMULATION; ANTIMICROBIALS; CIPROFLOXACIN;

D O I：

10.1016/j.bmc.2009.04.027

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

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. (C) 2009 Elsevier Ltd. All rights reserved.

引用

页码：3879 / 3886

页数：8

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