In vitro microbiological evaluation of 1,1'-(5,5'-(1,4-phenylene)bis(3-aryl-1H-pyrazole-5,1-(4H,5H)-diyl))diethanones, novel bisacetylated pyrazoles.

Organic and Medicinal Chemistry Letters Pub Date : 2011-09-20 DOI:10.1186/2191-2858-1-8

Vijayakumar Kanagarajan, Muthuvel Ramanathan Ezhilarasi, Mannathusamy Gopalakrishnan

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Abstract

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.

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新型双乙酰化吡唑--1,1'-(5,5'-(1,4-亚苯基)双(3-芳基-1H-吡唑-5,1-(4H,5H)-二基))二乙酮的体外微生物学评价。

采用盘扩散法和两倍序列稀释法测试了新型 1,1'-(5,5'-(1,4-亚苯基)双(3-芳基-1H-吡唑-5,1-(4H,5H)-二基)二乙酮 7-12 对受试细菌和真菌菌株的抗菌活性。化合物 7 对黄体微球菌；化合物 8 对 β-溶血性链球菌、黄体微球菌、肺炎克雷伯氏菌、石膏样小孢子菌；化合物 9 对金黄色葡萄球菌、柔性志贺氏菌、霍乱弧菌、铜绿假单胞菌、黄曲霉菌、吲哚蘑菇菌；化合物 10 对伤寒沙门氏菌、柔性志贺氏菌、石膏样小孢子菌。吉普森菌、11 对肺炎克氏菌、吉普森菌、12 对肺炎克氏菌和吉普森菌均显示出优异的抑菌区，并在 MIC 值为 6.25 μg/mL 时表现出卓越的抗菌和抗真菌活性。此外，所有测试化合物 7-12 对结核分枝杆菌 H37Rv 和耐 INH 的结核分枝杆菌都显示出良好的抗结核活性。针对结核杆菌的化合物 8 和针对耐 INH 结核杆菌的化合物 11 的 RLU 降低率分别为 89% 和 85%。

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Organic and Medicinal Chemistry Letters

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