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Norbornane-based cationic antimicrobial peptidomimetics targeting the bacterial membrane

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dc.contributor.authorHickey, Shane M
dc.contributor.authorAshton, Trent
dc.contributor.authorBoer, Gareth
dc.contributor.authorBader, Christie
dc.contributor.authorThomas, Michael
dc.contributor.authorElliott, Alysha G
dc.contributor.authorSchmuck, Carsten
dc.contributor.authorYu, Heidi
dc.contributor.authorLi, Jian
dc.contributor.authorNation, Roger
dc.contributor.authorCooper, Matthew A.
dc.contributor.authorPlush, Sally E.
dc.date.accessioned2024-05-07T05:18:22Z
dc.date.issued2018
dc.date.updated2023-01-08T07:17:19Z
dc.description.abstractThe design, synthesis and evaluation of a small series of potent amphiphilic norbornane antibacterial agents has been performed (compound 10 MIC = 0.25 μg/mL against MRSA). Molecular modelling indicates rapid aggregation of this class of antibacterial agent prior to membrane association and insertion. Two fluorescent analogues (compound 29 with 4-amino-naphthalimide and 34 with 4-nitrobenz-2-oxa-1,3-diazole fluorophores) with good activity (MIC = 0.5 μg/mL against MRSA) were also constructed and confocal microscopy studies indicate that the primary site of interaction for this family of compounds is the bacterial membrane.en_AU
dc.description.sponsorshipF.M.P., S.M.H., & T.D.A. thank the ARC (DP140100227) and the Strategic Research Centre for Chemistry and Biotechnology (Deakin University) for financial support and a top-upscholarship for S.M.H. The authors would also like to thank the Australian Research Council for funding Deakin University's Magnetic Resonance Facility through LIEF grant LE110100141. C.A.B was funded bya Future Industry Accelerator Research and Development Voucher Scheme. J.L. & R.L.N. are supported by a research grant from the National Institute of Allergy and Infectious Diseases of the NationalInstitutes of Health (R01 AI098771). J.L. is an Australian NHMRC Senior Research Fellow, while M.A.C. is an Australian NHMRC Principal Research Fellow. The content is solely the responsibility of the authors and does not necessarily represent the official views of the National Institute of Allergy and Infectious Diseases or the National Institutes of Health. The MIC and cytotoxicity assays were performed in collaboration with CO-ADD (Community for Open Antimicrobial DrugDiscovery, co-add.org)[76] funded bytheWellcome Trust and The University of Queensland.en_AU
dc.format.mimetypeapplication/pdfen_AU
dc.identifier.issn0223-5234en_AU
dc.identifier.urihttp://hdl.handle.net/1885/317334
dc.language.isoen_AUen_AU
dc.publisherElsevieren_AU
dc.relationhttp://purl.org/au-research/grants/arc/DP140100227en_AU
dc.relationhttp://purl.org/au-research/grants/arc/LE110100141en_AU
dc.rights© 2018 Elsevier Masson SASen_AU
dc.sourceEuropean Journal of Medicinal Chemistryen_AU
dc.subjectAntimicrobialen_AU
dc.subjectAntibacterialen_AU
dc.subjectAmphiphilicen_AU
dc.subjectFluorescenceen_AU
dc.subjectNaphthalimideen_AU
dc.subjectNorbornane and microscopyen_AU
dc.titleNorbornane-based cationic antimicrobial peptidomimetics targeting the bacterial membraneen_AU
dc.typeJournal articleen_AU
local.bibliographicCitation.lastpage22en_AU
local.bibliographicCitation.startpage9en_AU
local.contributor.affiliationHickey, Shane M, University of South Australiaen_AU
local.contributor.affiliationAshton, Trent, The University of Melbourneen_AU
local.contributor.affiliationBoer, Gareth, Deakin Universityen_AU
local.contributor.affiliationBader, Christie, University of South Australiaen_AU
local.contributor.affiliationThomas, Michael, College of Science, ANUen_AU
local.contributor.affiliationElliott, Alysha G, The University of Queenslanden_AU
local.contributor.affiliationSchmuck, Carsten, University of Duisburg-Essenen_AU
local.contributor.affiliationYu, Heidi, Monash Institute of Pharmaceutical Scienceen_AU
local.contributor.affiliationLi, Jian, Monash Institute of Pharmaceutical Scienceen_AU
local.contributor.affiliationNation, Roger, Monash Institute of Pharmaceutical Scienceen_AU
local.contributor.affiliationCooper, Matthew A., University of Queenslanden_AU
local.contributor.affiliationPlush, Sally E., Cancer Research Institute, School of Pharmacy and Medical Sciences, University of South Australiaen_AU
local.contributor.authoruidThomas, Michael, u5201227en_AU
local.description.embargo2099-12-31
local.description.notesImported from ARIESen_AU
local.identifier.absfor310299 - Bioinformatics and computational biology not elsewhere classifieden_AU
local.identifier.absfor320504 - Medical biochemistry - lipidsen_AU
local.identifier.ariespublicationu3102795xPUB38en_AU
local.identifier.citationvolume160en_AU
local.identifier.doi10.1016/j.ejmech.2018.09.072en_AU
local.identifier.scopusID2-s2.0-85054429059
local.identifier.thomsonIDWOS:000450383500002
local.publisher.urlhttps://www.elsevier.com/en_AU
local.type.statusPublished Versionen_AU

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