Norbornane-based cationic antimicrobial peptidomimetics targeting the bacterial membrane
Date
2018
Authors
Hickey, S.M.
Ashton, T.D.
Boer, G.
Bader, C.A.
Thomas, M.
Elliott, A.G.
Schmuck, C.
Yu, H.Y.
Li, J.
Nation, R.L.
Editors
Advisors
Journal Title
Journal ISSN
Volume Title
Type:
Journal article
Citation
European Journal of Medicinal Chemistry, 2018; 160:9-22
Statement of Responsibility
Shane M. Hickey, Trent D. Ashton, Gareth Boer, Christie A. Bader, Michael Thomas, Alysha G. Elliott, Carsten Schmuck, Heidi Y. Yu, Jian Li, Roger L. Nation, Matthew A. Cooper, Sally E. Plush, Douglas A. Brooks, Frederick M. Pfeffer
Conference Name
Abstract
The 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.
School/Discipline
Dissertation Note
Provenance
Description
Data source: Supplementary data, https://doi.org/10.1016/j.ejmech.2018.09.072
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Rights
2018 Elsevier Masson SAS. All rights reserved.