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A facile synthesis and antibacterial activity of novel pyrrolo[3,4-b]quinolin-2(3H)-yl)benzamides

机译:新型吡咯并[3,4-b]喹啉-2(3H)-基)苯甲酰胺的合成及抗菌活性

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A new series of pyrrolo[3,4-b]quinolin-2(3H)-yl)benzamides were designed based on molecular hybridization approach and synthesized by reaction of benzohydrazide derivatives with 9-phenylfuro[3,4-b]quinoline-1,3-diones in the presence of an Et3N catalyst. Simple reaction, excellent yield, simple separation process and eco-friendly approach by minimizing the chemical waste renders this protocol particularly attractive. The series 9a–g was evaluated for in vitro antibacterial activity against (+ve bacteria) Staphylococcus aureus ATCC 25923 and Enterococcus faecalis ATCC 29212, (?ve bacterium) Escherichia coli ATCC 25922. In vitro minimum inhibitory concentration (MIC) evaluations showed that the compound 9a was effective against E. coli (MIC: 0.25?mg/mL) S. aureus (MIC: 0.25?mg/mL) and E. faecalis (MIC: 0.5?mg/mL).
机译:基于分子杂交方法设计了一系列新的吡咯并[3,4-b]喹啉-2(3H)-基)苯甲酰胺,并通过苯甲酰肼衍生物与9-苯基呋喃[3,4-b]喹啉-1反应合成在Et3N催化剂存在下的-3-二酮。简单的反应,优异的收率,简单的分离工艺和通过最小化化学废物的环保方法使该方案特别有吸引力。评估了9a–g系列对(+ ve细菌)金黄色葡萄球菌ATCC 25923和粪肠球菌ATCC 29212((ve细菌)大肠杆菌ATCC 25922)的体外抗菌活性。体外最低抑菌浓度(MIC)评价显示化合物9a对大肠杆菌(MIC:0.25?mg / mL),金黄色葡萄球菌(MIC:0.25?mg / mL)和粪肠球菌(MIC:0.5?mg / mL)有效。

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