4.5 Article

Synthesis and antibiofilm activity of marine natural product-based 4-thiazolidinones derivatives

Journal

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 22, Issue 23, Pages 7131-7134

Publisher

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2012.09.073

Keywords

Bromopyrrole alkaloids; 4-Thiazolidinones; Antibiofilm agent

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4-Thiazolidinones derivatives of marine bromopyrrole alkaloids were synthesized as potential antibiofilm compounds. Among the synthesized compounds, some showed promising antibiofilm activity. Biological data revealed that 1,3-thiazolidin-4-one derivatives are more potent antibiofilm agents compared to 1,3-thiazinan-4-ones. Antibiofilm activity of compound 4b, 4c (MIC = 0.78 mu g/ml) was 3-fold superior than standard vancomycin (MIC = 3.125 mu g/ml) while activity of compound 4d, 4f, 4g and 4h was 2-fold (MIC = 1.56 mu g/ml) against Staphylococcus aureus biofilm. Compound 4b-4h showed equal antibiofilm activity against Staphylococcus epidermidis compared to standard Vancomycin (MIC = 3.125 mu g/ml). (C) 2012 Elsevier Ltd. All rights reserved.

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