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Synthesis and biological evaluation of some thiazolidinones as antimicrobial agents.

机译:一些噻唑烷酮作为抗微生物剂的合成与生物学评价。

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摘要

A novel series of thiazolidinone derivatives namely 4-(4-dimethylamino-6-{4-[5-(4-ethylpiperazin-1-ylmethyl)-4-oxo-2-phenylthiazolidin-3-yl]-phenylamino}-[1,3,5]triazin-2-yloxy)-1-methyl-1H-quinolin-2-one have been synthesized from the key intermediate 4-[4-(4-aminophenylamino)-6-dimethylamino-[1,3,5]triazin-2-yloxy]-1-methyl-1H-quinolin-2-one (7). Condensation reaction of compound 7 with different aldehyde derivatives were performed to obtain Schiff base derivatives, which after cyclization gave thiazolidinones and finally they were reacted with N-ethylpiperazine to get target compounds. The newly synthesized compounds were evaluated for their antimicrobial activity against eight bacterial strains (Staphylococcus aureus, Bacillus cereus, Escherichia coli, Pseudomonas aeruginosa, Klebsiella pneumoniae, Salmonella typhi, Proteus vulgaris, Shigella flexneri) and four fungal strains (Aspergillus niger, Candida albicans, Aspergillus fumigatus, Aspergillus clavatus).
机译:一系列新型噻唑烷酮衍生物,即4-(4-二甲基氨基-6- {4- [5-(4-乙基哌嗪-1-基甲基)-4-氧代-2-苯基噻唑烷-3-基] -phenylamino} - [1 3,5]三嗪-2-基氧基)-1-甲基-1H-喹啉-2-酮已从关键中间体4- [4-(4-氨基苯基氨基)-6-二甲基氨基 - [1,3, 5]三嗪-2-基氧基] -1-甲基-1H-喹啉-2-一(7)。 进行用不同醛衍生物进行化合物7的缩合反应以获得席夫碱衍生物,环化在环唑烷烃后,最后将它们与N-乙基哌嗪反应以得到靶化合物。 评估新合成的化合物,对八种细菌菌株进行抗微生物活性(金黄色葡萄球菌,芽孢杆菌,大肠杆菌,假霉素,铜绿素,肺炎群岛,沙门氏菌,Proteus vulgaris,Shigella Flexeri)和四个真菌菌株(Aspergillus Niger,Candida albicans, 曲霉菌fumigatus,aspergillus clavatus)。

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