Microwave-irradiated synthesis and antimicrobial activity of 2-phenyl-7-substitutedalkyl/arylaminoquinoline-4-carboxylic acid derivatives
作者:Hardik G. Bhatt、Yadvendra K. Agrawal
DOI:10.1007/s00044-009-9198-4
日期:2010.5
2-phenyl-7-substitutedquinoline-4-carboxylic acid derivatives through both conventional and microwave-irradiated methods. Intermediate 7-chloro-2-phenyl-quinoline-4-carboxylic acid was synthesized by condensation and cyclization of benzaldehyde, pyruvic acid, and m-chloroaniline in the presence of absolute ethanol and further substituted with aromatic, aliphatic, and alicyclic amines to obtain the desired
该报告集中于通过常规方法和微波辐射方法合成2-苯基-7-取代的喹啉-4-羧酸衍生物。中间体7-氯-2-苯基-喹啉-4-甲酸通过缩合和苯甲醛的环化,丙酮酸,和合成的米-氯苯胺在无水乙醇存在下,进一步用芳香族,脂肪族和脂环族胺取代,在微波辐射的影响下,以输出功率获得所需的2-苯基-7-取代的芳基/烷基氨基-喹啉-4-羧酸衍生物与常规方法相比,其收率范围为160至480 W,收率范围为90%至95%,反应时间更短。筛选所有合成的化合物对六种革兰氏阳性和四种革兰氏阴性生物的体外抗菌活性。所有合成的化合物均对广泛的微生物具有活性,对于热链球菌和铜绿假单胞菌均具有显着结果。化合物7c和7h 的最小抑菌浓度小于10μg。