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Microwave-assisted green synthesis, antimicrobial activity, and drug-likeness of novel isoindolinone derivatives

机译:微波辅助绿色合成,抗微生物活性和新型异吲哚啉酮衍生物的药物相似性

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摘要

An efficient and green microwave method has been developed for the synthesis of novel isoindolinone derivatives with good yields. The framework of these derivatives was constructed from beta-ketocarboxylic acids, various primary amines, and 2-carboxybenzaldehyde via cetrimonium bromide salt-promoted multicomponent cascade of decarboxylation/lactamization reaction. This methodology features a simple, environmentally friendly approach, employing water as a green solvent and using a one-pot, three-component reaction. The synthesized compounds were evaluated for their antimicrobial activity in vitro against six microorganisms, namely Escherichia coli,Serratia,Staphylococcus aureus, Bacillus subtilis,Aspergillus niger, andFusarium oxysporum. The results revealed that these derivatives have a significant antimicrobial activity. In addition, the drug-likeness of these derivatives has been evaluated.
机译:已经开发了一种有效和绿色的微波方法,用于合成具有良好产量的新型异吲哚醌衍生物。 这些衍生物的骨架由β-酮羧酸,各种伯胺和2-羧苄醛构成通过香料溴化物盐促进的脱羧/内酰胺化反应的多组分级联。 该方法具有简单,环保的方法,采用水作为绿色溶剂,并使用单罐三组分反应。 在体外评价合成的化合物对六种微生物,即大肠杆菌,沙拉氏菌,金黄色葡萄球菌,枯草芽孢杆菌,Aspergillus尼日尔,Andfusarium oxysporum。 结果表明,这些衍生物具有显着的抗微生物活性。 此外,已经评估了这些衍生物的药物象征。

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