期刊
ANTIBIOTICS-BASEL
卷 10, 期 9, 页码 -出版社
MDPI
DOI: 10.3390/antibiotics10091034
关键词
heteroaromatic stilbene derivatives; antimicrobial activity; Staphylococcus aureus; Enterococcus faecalis; Escherichia coli; Pseudomonas aeruginosa; Acinetobacter baumannii; Klebsiella pneumoniae
资金
- Ministry of Research (MIUR) Italy [PRIN2017SFBFER]
The research team focused on synthesizing novel antibiotics - synthetic heteroaromatic stilbene derivatives, which have a broad spectrum of antibacterial activity. Experimental validation showed excellent bacteriostatic activity, paving the way for the development of new antibiotics.
The widespread use of antibiotics has led to a gradual increase in drug-resistant bacterial infections, which severely weakens the clinical efficacy of antibacterial therapies. In recent decades, stilbenes aroused great interest because of their high bioavailability, as well as their manifold biological activity. Our research efforts are focused on synthetic heteroaromatic stilbene derivatives as they represent a potentially new type of antibiotic with a wide antibacterial spectrum. Herein, a preliminary molecular modeling study and a versatile synthetic scheme allowed us to define eight heteroaromatic stilbene derivatives with potential antimicrobial activity. In order to evaluate our compound's activity spectrum and antibacterial ability, minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) tests have been performed on Gram-positive and Gram-negative ATCC strains. Compounds PB4, PB5, PB7, and PB8 showed the best values in terms of MIC and were also evaluated for MBC, which was found to be greater than MIC, confirming a bacteriostatic activity. For all compounds, we evaluated toxicity on colon-rectal adenocarcinoma cells tumor cells (CaCo2), once it was established that the whole selected set was more active than 5-Fluorouracil in reducing CaCo-2 cells viability. To the best of our knowledge, the biological assays have shown for these derivatives an excellent bacteriostatic activity, compared to similar molecular structures previously reported, thus paving the way for a new class of antibiotic compounds.
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