Use este identificador para citar ou linkar para este item: https://locus.ufv.br//handle/123456789/23607
Tipo: Artigo
Título: Synthesis and evaluation of cadiolide analogues as inhibitors of bacterial biofilm formation
Autor(es): Mairink, Simone Z.
Barbosa, Luiz C. A.
Boukouvalas, John
Pedroso, Silvia H. S. P.
Magalhães, Paula P.
Farias, Luiz M.
Santos, Simone G.
Abstract: Bacterial biofilm infections pose a major clinical challenge due to the ability of biofilms to resist high levels of conventional antibiotics. In the present study, we describe the synthesis and biofilm inhibiting properties of nine new butenolides related to the cadiolide family of marine antibiotics. Eight new cadiolide analogues were synthesized using oxazole−ynone Diels−Alder cycloaddition/cycloreversion as the key step. Their effects on bacterial growth and biofilm formation were investigated against a range of Gram-positive and Gram-negative bacteria, namely Staphylococcus aureus, Enterococcus faecalis, Acinetobacter baumannii, Escherichia coli, Klebsiella pneumoniae and Pseudomonas aeruginosa. The cadiolide analogues strongly inhibited biofilm formation of the two Gram-positive bacteria (S. aureus and E. faecalis) at concentrations as low as 0.3 μg mL−1 and 0.5 μg mL−1, respectively. The identification of synthetic cadiolides with potent biofilm-inhibiting capabilities opens a new avenue for therapeutic interventions and highlights the potential of this class of compounds for antimicrobial drug development.
Palavras-chave: Cadiolides
Biofilm inhibition
Escherichia coli
Klebsiella pneumoniae
Enterococcus faecalis
Staphylococcus aureus
Editor: Medicinal Chemistry Research
Tipo de Acesso: Springer Science+Business Media, LLC, part of Springer Nature 2018
URI: https://doi.org/10.1007/s00044-018-2246-1
http://www.locus.ufv.br/handle/123456789/23607
Data do documento: Dez-2018
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