Department of Chemistry, Sardar Patel University, Vallabh Vidyanagar, Gujarat, India.
Arch Pharm (Weinheim). 2011 Feb;344(2):91-101. doi: 10.1002/ardp.201000010. Epub 2010 Dec 22.
A new series of 32 derivatives of 4-pyrazolyl-N-(hetero)arylquinoline 5a-p and 6a-p were synthesized by a one-pot base-catalyzed cyclocondensation reaction of 1-phenyl-3-(hetero)aryl-pyrazole-4-carbaldehyde 1a-h, malononitrile 2, and 3-(hetero)aryl-5,5-disubstitutedcyclohex-2-enone 3a-b or 4a-b, respectively. All the synthesized compounds were characterized by elemental analysis, FT-IR, (1) H-NMR, and (13) C-NMR spectral data. All the synthesized compounds 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 method. Some of the compounds were found to be more or equipotent against most of the employed strains than commercially available drugs as evident from the screening data.
通过一锅碱催化缩合反应，由 1-苯基-3-（杂）芳基吡唑-4-甲醛 1a-h、丙二腈 2 和 3-（杂）芳基-5,5-二取代环己-2-烯酮 3a-b 或 4a-b 分别合成了一系列 32 种 4-吡唑基-N-（杂环）芳基喹啉 5a-p 和 6a-p 的衍生物。所有合成的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。所有合成的化合物均采用肉汤微量稀释 MIC 法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、大肠杆菌）和抗两种真菌病原体（烟曲霉和白色念珠菌）的筛选。从筛选数据可以看出，一些化合物对大多数所使用的菌株的活性比市售药物更有效或相当。
