S.P.P. School of Pharmacy and Technology Management, NMIMS University, Vile Parle, Mumbai 400056, India.
Bioorg Med Chem Lett. 2012 Dec 1;22(23):7131-4. doi: 10.1016/j.bmcl.2012.09.073. Epub 2012 Oct 3.
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 μg/ml) was 3-fold superior than standard vancomycin (MIC=3.125 μg/ml) while activity of compound 4d, 4f, 4g and 4h was 2-fold (MIC=1.56 μg/ml) against Staphylococcus aureus biofilm. Compound 4b-4h showed equal antibiofilm activity against Staphylococcus epidermidis compared to standard Vancomycin (MIC=3.125 μg/ml).
海洋溴代吡咯生物碱的 4-噻唑烷酮衍生物被合成为有潜力的抗生物膜化合物。在所合成的化合物中，一些表现出有前景的抗生物膜活性。生物数据表明，与 1,3-噻唑烷-4-酮衍生物相比，1,3-噻唑烷-4-酮衍生物是更有效的抗生物膜剂。化合物 4b、4c（MIC=0.78μg/ml）的抗生物膜活性比标准万古霉素（MIC=3.125μg/ml）高 3 倍，而化合物 4d、4f、4g 和 4h 的活性则高 2 倍（MIC=1.56μg/ml），对抗金黄色葡萄球菌生物膜。化合物 4b-4h 对表皮葡萄球菌的抗生物膜活性与标准万古霉素（MIC=3.125μg/ml）相当。
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