Norbornane-based cationic antimicrobial peptidomimetics targeting the bacterial membrane
Version 2 2024-06-06, 06:34Version 2 2024-06-06, 06:34
Version 1 2018-10-26, 15:18Version 1 2018-10-26, 15:18
journal contribution
posted on 2024-06-06, 06:34authored byShane 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.