Antimicrobial activities of some amino derivatives of 5, 7-dibromo-2-methyl-8-benzoyloxyquinoline.

Bollettino chimico farmaceutico Pub Date : 2004-11-01
N J Nwodo, G B Okide, C O Esimone
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Abstract

In an attempt to design and synthesize more potent quinoline-based chemotherapeutic agents structural modifications of 5, 7-Dibromo-2-methyl-8-benzoyloxyqinoline was carried out. The replacement of the bromine atoms with the requisite alkylamino compound gave four amino-derivatives viz: bis(dipropylamino)-dipyrrolidino-, dipiperidino- and dipiperazino derivatives. The antimicrobial activities of these compounds were investigated against selected Gram-positive bacteria (Staphylococcus aureus and Bacillus subtilis), Gram-negative bacteria (Escherichin coli, Pseudomonas aeruginosa and Klebsiella spp) and yeast (Candida albicans). All the compounds showed broad or significant antimicrobial activity, which varied from two to ninety times that of the parent compound. The dipyrrolidino derivative was the most effective against Gram-positive bacteria and yeast while the dipiperidino derivative was the most effective against Gram-negative bacteria. No correlation has been established between the minimum inhibitory, (MIC) concentrations of the derivatives and the structural modifications.

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5,7 -二溴-2-甲基-8-苯甲酰氧喹啉部分氨基衍生物的抗菌活性。
为了设计和合成更有效的喹啉类化疗药物,对5,7 -二溴-2-甲基-8-苯甲酰氧喹啉进行了结构修饰。溴原子被必需的烷基胺化合物取代,得到了四种氨基衍生物,即双(二丙胺)-二吡咯里迪诺-、二吡咯里迪诺-和二哌嗪基衍生物。研究了这些化合物对选定的革兰氏阳性菌(金黄色葡萄球菌和枯草芽孢杆菌)、革兰氏阴性菌(大肠杆菌、铜绿假单胞菌和克雷伯氏菌)和酵母菌(白色念珠菌)的抑菌活性。所有化合物都显示出广泛或显著的抗菌活性,其活性从母体化合物的2倍到90倍不等。双吡咯利迪诺衍生物对革兰氏阳性菌和酵母菌的抑菌效果最好,而双吡咯利迪诺衍生物对革兰氏阴性菌的抑菌效果最好。衍生物的最小抑制浓度(MIC)与结构修饰之间没有相关性。
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