Department of Biological, Chemical and Pharmaceutical Sciences and Technologies (STEBICEF), University of Palermo, Via Archirafi 32, 90100 Palermo, Italy.
Mar Drugs. 2018 Aug 4;16(8):274. doi: 10.3390/md16080274.
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 IC values against 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.
新型噻唑诺托品类似物的简便合成及其作为相关革兰氏阳性和革兰氏阴性病原体生物膜形成抑制剂的活性进行了评价。所有化合物都能够以剂量依赖的方式干扰生物膜形成的第一步,对葡萄球菌菌株表现出选择性。最有效的衍生物对 ATCC 25923 的 IC 值在 0.40-2.03 μM 之间。这些新化合物表现出典型的抗毒力特征,能够抑制生物膜形成,而不影响浮游生物形式的微生物生长。