TAILIEUCHUNG - Kanagarajan et al. Organic and Medicinal Chemistry Letters 2011, 1:8
Kanagarajan et al. Organic and Medicinal Chemistry Letters 2011, 1:8 ORIGINAL Open Access 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 Kanagarajan1,2, Muthuvel Ramanathan Ezhilarasi2 and Mannathusamy Gopalakrishnan2* 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 b-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 | Kanagarajan et al. Organic and Medicinal Chemistry Letters 2011 1 8 http content 1 1 8 o Organic and Medicinal Chemistry Letters a SpringerOpen Journal ORIGINAL Open Access In vitro microbiological evaluation of 1 1 - 5 5 - 1 4-phenylene bis 3-aryl-1 H-pyrazole-5 1- 4H 5H -diyl diethanones novel bisacetylated pyrazoles Vijayakumar Kanagarajan1 2 Muthuvel Ramanathan Ezhilarasi 2 and Mannathusamy Gopalakrishnan2 Abstract Novel 1 1 - 5 5 - 1 4-phenylene b s 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 b-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 ag 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. Keywords bisacetylated pyrazoles in situ acetylation antibacterial activity antifungal activity antitubercular activity 1. Introduction Mycobacterium tuberculosis MTB is a pathogenic bacterial species in the genus Mycobacterium and is the causative agent of most cases of tuberculosis. Tuberculosis is a common and often deadly infectious disease in humans 1 2 . Tuberculosis is the most common opportunistic disease in persons infected with human immunodeficiency virus 3 . The genome of MTB is rich in
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