Kanagarajan Vijayakumar, Ezhilarasi Muthuvel Ramanathan, Gopalakrishnan Mannathusamy
Synthetic Organic Chemistry Laboratory, Department of Chemistry, Annamalai University, Annamalainagar 608 002, Tamil Nadu, India.
Org Med Chem Lett. 2011 Sep 20;1(1):8. doi: 10.1186/2191-2858-1-8.
Novel 1,1'-(5,5'-(1,4-phenylene)bis(3-aryl-1H-pyrazole-5,1-(4H,5H)-diyl))diethanones 7-12 were tested for their antimicrobial activity by disc diffusion and twofold serial dilution method against the tested bacterial and fungal strains. Compounds 7 against Micrococcus luteus, 8 against β-Heamolytic streptococcus, M. luteus, Klebsiella pneumonia, Microsporum gypseum, 9 against Staphylococcus aureus, Shigella flexneri, Vibreo cholerae, Pseudomonas aeruginosa, Aspergillus flavus, Mucor indicus, 10 against Salmonella typhii, S. flexneri, M. gypseum, 11 against K. pneumonia, M. gypseum, 12 against K. pneumonia, and M. gypseum show superior zone of inhibitions and exhibited excellent antibacterial and antifungal activities at a MIC value of 6.25 μg/mL. Moreover, all the tested compounds 7-12 revealed promising antitubercular activity against Mycobacterium tuberculosis H37Rv and INH-resistant M. tuberculosis. Compounds 8 against M. tuberculosis and 11 against INH-resistant M. tuberculosis exhibited the percentage of reduction in RLU at 89 and 85%, respectively.
通过纸片扩散法和两倍系列稀释法，对新型1,1'-(5,5'-(1,4-亚苯基)双(3-芳基-1H-吡唑-5,1-(4H,5H)-二亚基))二乙酮7-12针对受试细菌和真菌菌株的抗菌活性进行了测试。化合物7对藤黄微球菌、8对β-溶血性链球菌、藤黄微球菌、肺炎克雷伯菌、石膏样小孢子菌、9对金黄色葡萄球菌、弗氏志贺菌、霍乱弧菌、铜绿假单胞菌、黄曲霉、印度毛霉、10对伤寒沙门菌、弗氏志贺菌、石膏样小孢子菌、11对肺炎克雷伯菌、石膏样小孢子菌、12对肺炎克雷伯菌和石膏样小孢子菌显示出较好的抑菌圈，并且在6.25μg/mL的最低抑菌浓度值时表现出优异的抗菌和抗真菌活性。此外，所有受试化合物7-12对结核分枝杆菌H37Rv和耐异烟肼结核分枝杆菌均显示出有前景的抗结核活性。化合物8对结核分枝杆菌和11对耐异烟肼结核分枝杆菌的相对发光单位减少百分比分别为89%和85%。
