Synthesis and biological evaluations of enoxacin carboxamide derivatives

被引：13

作者：

Arayne, M. Saeed ^{[1
]}

Sultana, Najma ^{[2
]}

Haroon, Urooj ^{[1
]}

Mesaik, M. Ahmed ^{[3
]}

Asif, Muhammad ^{[3
]}

机构：

[1] Univ Karachi, Dept Chem, Karachi 75272, Pakistan

[2] Univ Karachi, Dept Pharmaceut Chem, Fac Pharm, Karachi 75272, Pakistan

[3] Univ Karachi, Panjwani Ctr Mol Med & Drug Res, Int Ctr Biol & Chem Sci, Karachi 75272, Pakistan

来源：

ARCHIVES OF PHARMACAL RESEARCH | 2009年 / 32卷 / 07期

关键词：

Enoxacin; Nucleophilic substitution; Derivatives; Antibacterial activity; Oxidative burst response; ANTIBACTERIAL ACTIVITY; QUINOLONE ANTIBACTERIALS; PIPERAZINYL QUINOLONES; ANTIMICROBIAL ACTIVITY; CLINICAL EFFICACY; INVITRO ACTIVITY; IN-VITRO; PHARMACOKINETICS; CIPROFLOXACIN; AGENTS;

D O I：

10.1007/s12272-009-1700-5

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The present work deals with the synthesis of various enoxacin analogues via nucleophilic substitution of 3-carboxylic acid moiety of the drug by aromatic amines. The free carboxylic group was utilized in the formation of amides and the effect of functional group exchange on different biological activities of the parent was evaluated. The structure of these derivatives was established by various spectroscopic techniques and mass spectrometry. The derivatives were evaluated as antibacterial agents against a series of Gram-positive and Gram-negative bacteria whereby some of them displayed considerably improved antimicrobial profile against Gram-negative test strains. Additionally unlike enoxacin, the derivatives were also found to modulate oxidative burst response of phagocytes exhibiting moderate to significant inhibitory activity.

引用

页码：967 / 974

页数：8

共 36 条

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