Preprint Article Version 1 Preserved in Portico This version is not peer-reviewed

Heteroaryl-Ethylenes as New Lead Compounds in the Fight against High Priority Bacterial Strains

Version 1 : Received: 30 July 2021 / Approved: 3 August 2021 / Online: 3 August 2021 (13:32:14 CEST)

A peer-reviewed article of this Preprint also exists.

Bongiorno, D.; Musso, N.; Bonacci, P.G.; Bivona, D.A.; Massimino, M.; Stracquadanio, S.; Bonaccorso, C.; Fortuna, C.G.; Stefani, S. Heteroaryl-Ethylenes as New Lead Compounds in the Fight against High Priority Bacterial Strains. Antibiotics 2021, 10, 1034. Bongiorno, D.; Musso, N.; Bonacci, P.G.; Bivona, D.A.; Massimino, M.; Stracquadanio, S.; Bonaccorso, C.; Fortuna, C.G.; Stefani, S. Heteroaryl-Ethylenes as New Lead Compounds in the Fight against High Priority Bacterial Strains. Antibiotics 2021, 10, 1034.

Journal reference: Antibiotics 2021, 10, 1034
DOI: 10.3390/antibiotics10091034

Abstract

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 for their manifold biological activity. Our research efforts are focused on synthetic heteroaromatic stilbene deriva-tives 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 Con-centration (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 however was found to be greater than MIC, confirming a bacteriostatic activity. For all compounds, we evaluated toxici-ty on colon-rectal adenocarcinoma cells tumor cells (CaCo2), once established that the whole se-lected 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.

Keywords

heteroaromatic stilbene derivatives; antimicrobial activity; Staphylococcus aureus; Enterococcus faecalis; Escherichia coli; Pseudomonas aeruginosa; Acinetobacter baumannii; Klebsiella pneumoniae.

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