Norbornane-based cationic antimicrobial peptidomimetics targeting the bacterial membrane
- Author(s)
- Hickey, SM; Ashton, TD; Boer, G; Bader, CA; Thomas, M; Elliott, AG; Schmuck, C; Yu, HY; Li, J; Nation, RL; Cooper, MA; Plush, SE; Brooks, DA; Pfeffer, FM;
- Journal Title
- European Journal of Medicinal Chemistry
- Publication Type
- Journal Article
- Abstract
- The design, synthesis and evaluation of a small series of potent amphiphilic norbornane antibacterial agents has been performed (compound 10 MIC=0.25mug/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=0.5mug/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.
- Publisher
- Elsevier
- Research Division(s)
- Chemical Biology
- PubMed ID
- 30316060
- Publisher's Version
- https://doi.org/10.1016/j.ejmech.2018.09.072
- Terms of Use/Rights Notice
- Refer to copyright notice on published article.
Creation Date: 2018-10-23 08:48:41
Last Modified: 2018-10-23 08:52:00