Norbornane-based cationic antimicrobial peptidomimetics targeting the bacterial membrane.
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ABSTRACT:
SUBMITTER: Hickey SM
PROVIDER: S-EPMC6309908 | biostudies-literature | 2018 Dec
REPOSITORIES: biostudies-literature
Publications
Norbornane-based cationic antimicrobial peptidomimetics targeting the bacterial membrane.
Hickey Shane M SM Ashton Trent D TD Boer Gareth G Bader Christie A CA Thomas Michael M Elliott Alysha G AG Schmuck Carsten C Yu Heidi Y HY Li Jian J Nation Roger L RL Cooper Matthew A MA Plush Sally E SE Brooks Douglas A DA Pfeffer Frederick M FM
European journal of medicinal chemistry 20181003
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 ...[more]
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