Synthesis and evaluation of aromatic BDSF bioisosteres on biofilm formation and colistin sensitivity in pathogenic bacteria

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dc.contributor.authorGómez, Andromeda-Celeste
dc.contributor.authorHorgan, Conor
dc.contributor.authorYero, Daniel
dc.contributor.authorBravo, Marc
dc.contributor.authorDaura, Xavier
dc.contributor.authorO'Driscoll, Michelle
dc.contributor.authorGibert, Isidre
dc.contributor.authorO'Sullivan, Timothy P.
dc.contributor.funderIrish Research Council
dc.contributor.funderMinisterio de Ciencia e Innovación
dc.contributor.funderAgència de Gestió d'Ajuts Universitaris i de Recerca
dc.date.accessioned2023-10-16T16:21:46Z
dc.date.available2023-10-16T15:10:18Zen
dc.date.available2023-10-16T16:21:46Z
dc.date.issued2023-09-23
dc.date.updated2023-10-16T14:10:19Zen
dc.description.abstractThe diffusible signal factor family (DSF) of molecules play an important role in regulating intercellular communication, or quorum sensing, in several disease-causing bacteria. These messenger molecules, which are comprised of cis-unsaturated fatty acids, are involved in the regulation of biofilm formation, antibiotic tolerance, virulence and the control of bacterial resistance. We have previously demonstrated how olefinic N-acyl sulfonamide bioisosteric analogues of diffusible signal factor can reduce biofilm formation or enhance antibiotic sensitivity in a number of bacterial strains. This work describes the design and synthesis of a second generation of aromatic N-acyl sulfonamide bioisosteres. The impact of these compounds on biofilm production in Acinetobacter baumannii, Escherichia coli, Burkholderia multivorans, Burkholderia cepacia, Burkholderia cenocepacia, Pseudomonas aeruginosa and Stenotrophomonas maltophilia is evaluated, in addition to their effects on antibiotic tolerance. The ability of these molecules to increase survival rates on co-administration with colistin is also investigated using the Galleria infection model.en
dc.description.sponsorshipIrish Research Council (Government of Ireland Postgraduate Research Scholarship (GOIPG/2017/1111), (GOIPG/2021/227)); Ministerio de Ciencia e Innovación (Spanish MICINN (PID2019-111364RB-I00); Agència de Gestió d'Ajuts Universitaris i de Recerca (Catalan AGAUR (2021 SGR00092))
dc.description.statusPeer revieweden
dc.description.versionPublished Version
dc.format.mimetypeapplication/pdfen
dc.identifier.articleid115819
dc.identifier.citationGómez, A.-C., Horgan, C., Yero, D., Bravo, M., Daura, X., O’Driscoll, M., Gibert, I. and O’Sullivan, T.P. (2023) ‘Synthesis and evaluation of aromatic BDSF bioisosteres on biofilm formation and colistin sensitivity in pathogenic bacteria’, European Journal of Medicinal Chemistry, 261, 115819 (16 pp). https://doi.org/10.1016/j.ejmech.2023.115819.
dc.identifier.doi10.1016/j.ejmech.2023.115819en
dc.identifier.eissn1768-3254
dc.identifier.endpage16
dc.identifier.issn0223-5234
dc.identifier.journaltitleEuropean Journal of Medicinal Chemistry
dc.identifier.startpage1
dc.identifier.urihttps://hdl.handle.net/10468/15122
dc.identifier.volume261
dc.language.isoenen
dc.publisherElsevier
dc.relation.urihttps://doi.org/10.1016/j.ejmech.2023.115819
dc.rights© 2023 The Authors. Published by Elsevier Masson SAS. This is an open access article under the CC BY license (http://creativecommons.org/licenses/by/4.0/).
dc.rights.urihttp://creativecommons.org/licenses/by/4.0/
dc.subjectDiffusible signal factor
dc.subjectQuorum sensing
dc.subjectBiofilms
dc.subjectResistance
dc.subjectAcinetobacter baumannii
dc.subjectEscherichia coli
dc.subjectBurkholderia multivorans
dc.subjectBurkholderia cepacia
dc.subjectBurkholderia cenocepacia
dc.subjectPseudomonas aeruginosa and Stenotrophomonas maltophilia
dc.titleSynthesis and evaluation of aromatic BDSF bioisosteres on biofilm formation and colistin sensitivity in pathogenic bacteriaen
dc.typeArticle (peer-reviewed)
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