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Norbornane-based cationic antimicrobial peptidomimetics targeting the bacterial membrane

Version 2 2024-06-06, 06:34
Version 1 2018-10-26, 15:18
journal contribution
posted on 2024-06-06, 06:34 authored by Shane M Hickey, Trent D Ashton, Gareth BoerGareth 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, Fred PfefferFred Pfeffer
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.

History

Journal

European journal of medicinal chemistry

Volume

160

Pagination

9-22

Location

Amsterdam, The Netherlands

ISSN

0223-5234

eISSN

1768-3254

Language

eng

Publication classification

C1 Refereed article in a scholarly journal

Copyright notice

2018, Elsevier Masson SAS

Publisher

Elsevier