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 |