Saeed Arayne M, Sultana Najma, Haroon Urooj, Ahmed Mesaik M, Asif Muhammad
Department of Chemistry, University of Karachi, Karachi, 75272, Pakistan.
Arch Pharm Res. 2009 Jul;32(7):967-74. doi: 10.1007/s12272-009-1700-5. Epub 2009 Jul 31.
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.
本研究通过芳香胺对药物3 - 羧酸部分进行亲核取代反应来合成各种依诺沙星类似物。游离羧基用于形成酰胺，并评估官能团交换对母体不同生物活性的影响。这些衍生物的结构通过各种光谱技术和质谱得以确定。对这些衍生物作为抗菌剂针对一系列革兰氏阳性和革兰氏阴性细菌进行了评估，结果显示其中一些对革兰氏阴性测试菌株展现出显著改善的抗菌谱。此外，与依诺沙星不同，还发现这些衍生物能够调节吞噬细胞的氧化爆发反应，表现出中度至显著的抑制活性。
