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Mar. Drugs 2018, 16(8), 274; https://doi.org/10.3390/md16080274

New Thiazole Nortopsentin Analogues Inhibit Bacterial Biofilm Formation

Department of Biological, Chemical and Pharmaceutical Sciences and Technologies (STEBICEF), University of Palermo, Via Archirafi 32, 90100 Palermo, Italy
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Received: 21 June 2018 / Revised: 23 July 2018 / Accepted: 24 July 2018 / Published: 4 August 2018
(This article belongs to the Special Issue New Strategies to Counteract Antibiotic Resistance Mechanisms)
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Abstract

New thiazole nortopsentin analogues were conveniently synthesized and evaluated for their activity as inhibitors of biofilm formation of relevant Gram-positive and Gram-negative pathogens. All compounds were able to interfere with the first step of biofilm formation in a dose-dependent manner, showing a selectivity against the staphylococcal strains. The most active derivatives elicited IC50 values against Staphylococcus aureus ATCC 25923, ranging from 0.40–2.03 µM. The new compounds showed a typical anti-virulence profile, being able to inhibit the biofilm formation without affecting the microbial growth in the planktonic form. View Full-Text
Keywords: marine alkaloids; nortopsentin analogues; thiazole derivatives; anti-virulence agents; antibiofilm agents marine alkaloids; nortopsentin analogues; thiazole derivatives; anti-virulence agents; antibiofilm agents
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).
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Carbone, A.; Parrino, B.; Cusimano, M.G.; Spanò, V.; Montalbano, A.; Barraja, P.; Schillaci, D.; Cirrincione, G.; Diana, P.; Cascioferro, S. New Thiazole Nortopsentin Analogues Inhibit Bacterial Biofilm Formation. Mar. Drugs 2018, 16, 274.

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