Department of Chemistry, Sardar Patel University, Vallabh Vidyanagar, 388120 Gujarat, India.
Saudi Pharm J. 2011 Apr;19(2):75-83. doi: 10.1016/j.jsps.2011.01.005. Epub 2011 Feb 3.
A new series of 12 derivatives of 4-pyrazolyl-N-arylquinoline-2,5-dione (4a-l) were synthesized by one pot base catalyzed cyclocondensation reaction of 1-aryl-5-chloro-3-methyl-1H-pyrazole-4-carbaldehyde (1a-c), Meldrum's acid (2) and 3-arylamino-5,5-disubstitutedcyclohex-2-enone (3a-d). All the compounds were characterized by elemental analysis, FT-IR, (1)H NMR and (13)C NMR spectral data and were screened, against six bacterial pathogens, namely Bacillus subtilis, Clostridium tetani, Streptococcus pneumoniae, Salmonella typhi, Vibrio cholerae, Escherichia coli and antifungal activity, against two fungal pathogens Aspergillus fumigatus and Candida albicans, using broth microdilution MIC (minimum inhibitory concentration) method. Some of the compounds were found to be equipotent or more potent than commercial drugs, against most of the employed strains, as evident from the screening data.
通过一锅碱催化缩合反应，将 1-芳基-5-氯-3-甲基-1H-吡唑-4-甲醛（1a-c）、Meldrum's 酸（2）和 3-芳基氨基-5,5-二取代环己-2-烯酮（3a-d）合成了一系列 12 种新的 4-吡唑基-N-芳基喹啉-2,5-二酮（4a-l）衍生物。所有化合物均通过元素分析、FT-IR、（1）H NMR 和（13）C NMR 光谱数据进行了表征，并通过微量肉汤稀释法（最小抑菌浓度，MIC）对其进行了抗六种细菌病原体（枯草芽孢杆菌、破伤风梭菌、肺炎链球菌、伤寒沙门氏菌、霍乱弧菌和大肠杆菌）和两种真菌病原体（烟曲霉和白色念珠菌）的活性筛选。从筛选数据可以看出，一些化合物在大多数试验菌株中与商业药物相当或更有效。
