New Thiazole Nortopsentin Analogues Inhibit Bacterial Biofilm Formation

新型噻唑诺托普森汀类似物可抑制细菌生物膜形成

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作者:Anna Carbone, Barbara Parrino, Maria Grazia Cusimano, Virginia Spanò, Alessandra Montalbano, Paola Barraja, Domenico Schillaci, Girolamo Cirrincione, Patrizia Diana, Stella Cascioferro

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.

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