Abstract Eight new 7-substituted quinolin-8-ol derivatives were synthesized in moderate to good yields through quinolin-8-ol, and secondary amines as the starting reagents. The structures of the prepared compounds have been characterized by elemental analysis and 1H/13C NMR. The antimicrobial activity of this new series of heterocyclic compounds has been achieved "in vitro" against some bacterial strains by means of the disk method, and most of the tested compounds have shown comparable or greater antibacterial activity than nitroxoline (standard antibiotic). It was very motivating to observe that POM (Petra/Osiris/Molinspiration) bioinformatic analyses of compound 5 exhibited better antibacterial activity (MIC = 10 μg/mL against B. subtilis bacteria), and higher drug score (DS = 0.57) compared with Nitroxoline (DS = 0.47; MIC = 20 μg/mL). Molecular docking investigations were also conducted to investigate the binding affinities as well as interactions of some compounds with the target proteins.

中文翻译：

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一些新的 7-取代喹啉-8-醇衍生物的合成和抗菌活性评价：POM 分析、对接和抗菌药效团位点的鉴定

摘要 以喹啉-8-醇和仲胺为起始试剂，以中等至良好的收率合成了8种新型7-取代喹啉-8-醇衍生物。所制备化合物的结构已通过元素分析和1H/13C NMR表征。这一系列新杂环化合物的抗菌活性已通过圆盘法在“体外”对一些细菌菌株实现，并且大多数测试的化合物显示出与硝基喹啉（标准抗生素）相当或更高的抗菌活性。观察到化合物 5 的 POM（Petra/Osiris/Molinspiration）生物信息学分析表现出更好的抗菌活性（MIC = 10 μg/mL 对枯草芽孢杆菌细菌）和更高的药物评分（DS = 0.57）与硝基氧嘧啶相比，这是非常令人鼓舞的(DS = 0.47; MIC = 20 微克/毫升）。还进行了分子对接研究以研究结合亲和力以及某些化合物与靶蛋白的相互作用。