期刊
MOLECULES
卷 26, 期 1, 页码 -出版社
MDPI
DOI: 10.3390/molecules26010081
关键词
antibiofilm agents; antibiotic resistance; thiazole derivatives; marine alkaloids analogues; nortopsentin
资金
- European Union 2014-2020 PON Ricerca e Innovazione grant from the Italian Ministry of Education, University and Research [ARS01_00432]
Anti-virulence strategy, particularly targeting biofilm formation, is considered a promising approach to combat antibiotic resistance. A new series of 18 thiazole derivatives showed high selectivity against Gram-positive bacterial strains and promisingly inhibited biofilm formation without affecting microbial growth. These compounds represent potential lead candidates for the development of new anti-virulence agents.
Anti-virulence strategy is currently considered a promising approach to overcome the global threat of the antibiotic resistance. Among different bacterial virulence factors, the biofilm formation is recognized as one of the most relevant. Considering the high and growing percentage of multi-drug resistant infections that are biofilm-mediated, new therapeutic agents capable of counteracting the formation of biofilms are urgently required. In this scenario, a new series of 18 thiazole derivatives was efficiently synthesized and evaluated for its ability to inhibit biofilm formation against the Gram-positive bacterial reference strains Staphylococcus aureus ATCC 25923 and S. aureus ATCC 6538 and the Gram-negative strain Pseudomonas aeruginosa ATCC 15442. Most of the new compounds showed a marked selectivity against the Gram-positive strains. Remarkably, five compounds exhibited BIC50 values against S. aureus ATCC 25923 ranging from 1.0 to 9.1 mu M. The new compounds, affecting the biofilm formation without any interference on microbial growth, can be considered promising lead compounds for the development of a new class of anti-virulence agents.
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