Antimicrobial and Cytotoxicity Activities of 2-(aryl)-3-(benzo[d][1,3] dioxol-5-yl)thiazolidin-4-ones

Author(s): Silvana P. Souza, Hellen G. Masteloto, Daniel S. da Silva, Juliana H. Azambuja, Elizandra Braganhol, Juliana S. Ribeiro, Rafael G. Lund, Wilson Cunico*

Journal Name: Letters in Drug Design & Discovery

Volume 14 , Issue 9 , 2017

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Graphical Abstract:


Background: This study evaluated the biological properties of twelve 1,3-thiazolidin-4- ones by assessing antifungal and antibacterial activities.

Methods: All compounds were tested against three fungi and two bacteria. The lowest concentration that produced a ≥50% inhibition of the growth of yeast in comparison with positive control was identified as MIC50. Compound 1b showed the best antifungal result against Candida albicans with MIC50 100 μg/ml (52.38% of growth inhibition). In the antifungal Rhodotorula assay, two compounds showed good antifungal activity with MIC50 100 μg/ml (1f: 82.91% and 1i: 61.91%). For C. parapsilosis compound 1i has MIC50 200 μg/ml.

Results and Conclusion: No antibacterial activity was found for Staphylococcus aureus and Escherichia coli at the highest concentration tested (400 μg/ml). The cytotoxicity study for three compounds was carried out against primary astrocyte cells and no toxic effect was found at 400 μM. This study discovered at least two potential compounds that will guide further chemical modification to search for better results.

Keywords: 4-thiazolidinones, 1, 3-benzodioxol, candida albicans, candida parapsilosis, rhodotorula mucilaginosa, astrocytes.

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Article Details

Year: 2017
Page: [1042 - 1047]
Pages: 6
DOI: 10.2174/1570180814666170106143418
Price: $65

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