Exploration of the antibiotic potentiating activity of indolglyoxylpolyamines.

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dc.contributor.author Cadelis, Melissa en
dc.contributor.author Pike, Elliot IW en
dc.contributor.author Kang, Weirong en
dc.contributor.author Wu, Zimei en
dc.contributor.author Bourguet-Kondracki, Marie-Lise en
dc.contributor.author Blanchet, Marine en
dc.contributor.author Vidal, Nicolas en
dc.contributor.author Brunel, Jean Michel en
dc.contributor.author Copp, Brent en
dc.date.accessioned 2020-02-17T22:18:32Z en
dc.date.issued 2019-12 en
dc.identifier.issn 1768-3254 en
dc.identifier.uri http://hdl.handle.net/2292/50086 en
dc.description.abstract A series of substituted di-indolglyoxylamido-spermine analogues were prepared and evaluated for intrinsic antimicrobial properties and the ability to enhance antibiotic action. As a compound class, intrinsic activity was typically observed towards Gram-positive bacteria and the fungus Cryptococcus neoformans, with notable exceptions being the 5-bromo- and 6-chloro-indole analogues which also exhibited modest activity (MIC 34-50 μM) towards the Gram-negative bacteria Escherichia coli and Klebsiella pneumoniae. Several analogues enhanced the activity of doxycycline towards the Gram-negative bacteria Pseudomonas aeruginosa, E. coli, K. pneumoniae and Acinetobacter baumannii. Of particular note was the identification of five antibiotic enhancing analogues (5-Br, 7-F, 5-Me, 7-Me, 7-OMe) which also exhibited low to no cytotoxicity and red blood cell haemolytic properties. The mechanisms of action of the 5-Br and 7-F analogues were attributed to the ability to disrupt the integrity of, and depolarize, bacterial membranes. en
dc.format.medium Print-Electronic en
dc.language eng en
dc.relation.ispartofseries European journal of medicinal chemistry en
dc.rights Items in ResearchSpace are protected by copyright, with all rights reserved, unless otherwise indicated. Previously published items are made available in accordance with the copyright policy of the publisher. en
dc.rights.uri https://researchspace.auckland.ac.nz/docs/uoa-docs/rights.htm en
dc.subject Cell Line en
dc.subject Humans en
dc.subject Gram-Negative Bacteria en
dc.subject Hemolysis en
dc.subject Cephalosporins en
dc.subject Spermine en
dc.subject Indoles en
dc.subject Anti-Bacterial Agents en
dc.subject Microbial Sensitivity Tests en
dc.subject Signal Transduction en
dc.subject Cell Membrane Permeability en
dc.subject Cell Survival en
dc.subject Hydrolysis en
dc.title Exploration of the antibiotic potentiating activity of indolglyoxylpolyamines. en
dc.type Journal Article en
dc.identifier.doi 10.1016/j.ejmech.2019.111708 en
pubs.begin-page 111708 en
pubs.volume 183 en
dc.rights.holder Copyright: The author en
pubs.publication-status Published en
dc.rights.accessrights http://purl.org/eprint/accessRights/RestrictedAccess en
pubs.subtype Journal Article en
pubs.elements-id 783794 en
pubs.org-id Medical and Health Sciences en
pubs.org-id Medical Sciences en
pubs.org-id Molecular Medicine en
pubs.org-id Pharmacy en
pubs.org-id Science en
pubs.org-id Chemistry en
pubs.org-id Science Research en
pubs.org-id Maurice Wilkins Centre (2010-2014) en
dc.identifier.eissn 1768-3254 en
pubs.record-created-at-source-date 2019-09-25 en
pubs.dimensions-id 31550659 en

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