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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

Vijayakumar Kanagarajan12, Muthuvel Ramanathan Ezhilarasi2 and Mannathusamy Gopalakrishnan2*

Author Affiliations

1 Energetics Research Institute, Nanyang Technological University, 50, Nanyang Avenue, Singapore-639 798, Republic of Singapore

2 Synthetic Organic Chemistry Laboratory, Department of Chemistry, Annamalai University, Annamalainagar 608 002, Tamil Nadu, India

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Organic and Medicinal Chemistry Letters 2011, 1:8  doi:10.1186/2191-2858-1-8

Published: 20 September 2011


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.

bisacetylated pyrazoles; in situ acetylation; antibacterial activity; antifungal activity; antitubercular activity

Graphical abstract