Synthesis and evaluation of novel furanones as biofilm inhibitors in opportunistic human pathogens.
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Date
2022-08-27
Authors
Gómez, Andromeda-Celeste
Lyons, Thérèse
Mamat, Uwe
Yero, Daniel
Bravo, Marc
Daura, Xavier
Elshafee, Osama
Brunke, Sascha
Gahan, Cormac G. M.
O'Driscoll, Michelle
Journal Title
Journal ISSN
Volume Title
Publisher
Elsevier
Published Version
Abstract
Diseases caused by biofilm-forming pathogens are becoming increasingly prevalent and represent a major threat to human health. This trend has prompted a search for novel inhibitors of microbial biofilms which could, for example, be used to potentiate existing antibiotics. Naturally-occurring, halogenated furanones isolated from marine algae have proven to be effective biofilm inhibitors in several bacterial species. In this work, we report the synthesis of a library of novel furanones and their subsequent evaluation as biofilm inhibitors in several opportunistic human pathogens including S. enterica, S. aureus, E. coli, S. maltophilia, P. aeruginosa and C. albicans. A number of the most potent compounds were subjected to further analysis by confocal laser-scanning microscopy for their effects on P. aeruginosa and C. albicans biofilms individually, in addition to mixed polymicrobial biofilms. Lastly, we investigated the impact of a promising candidate on survival rates in vivo using a Galleria mellonella model.
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Keywords
Furanones , Biofilms , Quorum sensing , Salmonella enterica , Staphylococcus aureus , Pseudomonas aeruginosa , Escherichia coli , Stenotrophomonas maltophilia , Candida albicans
Citation
Gómez, A.-C., Lyons, T., Mamat, U., Yero, D., Bravo, M., Daura, X., Elshafee, O., Brunke, S., Gahan, C.G.M., O’Driscoll, M., Gibert, I. and O’Sullivan, T.P. (2022) ‘Synthesis and evaluation of novel furanones as biofilm inhibitors in opportunistic human pathogens’, European Journal of Medicinal Chemistry, 242, 114678 (16 pp). doi: 10.1016/j.ejmech.2022.114678