Synthesis and evaluation of cationic norbornanes as peptidomimetic antibacterial agents
Data(s) |
14/06/2015
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Resumo |
A series of structurally amphiphilic biscationic norbornanes have been synthesised as rigidified, low molecular weight peptidomimetics of cationic antimicrobial peptides. A variety of charged hydrophilic functionalities were attached to the norbornane scaffold including aminium, guanidinium, imidazolium and pyridinium moieties. Additionally, a range of hydrophobic groups of differing sizes were incorporated through an acetal linkage. The compounds were evaluated for antibacterial activity against both Gram-negative and Gram-positive bacteria. Activity was observed across the series; the most potent of which exhibited an MIC's ≤ 1 μg mL(-1) against Streptococcus pneumoniae, Enterococcus faecalis and several strains of Staphylococcus aureus, including multi-resistant methicillin resistant (mMRSA), glycopeptide-intermediate (GISA) and vancomycin-intermediate (VISA) S. aureus. |
Identificador | |
Idioma(s) |
eng |
Publicador |
Royal Society of Chemistry |
Relação |
http://dro.deakin.edu.au/eserv/DU:30075594/hickey-synthesisandevaluation-2015.pdf http://www.dx.doi.org/10.1039/c5ob00621j http://www.ncbi.nlm.nih.gov/pubmed/25958967 |
Direitos |
2015, Royal Society of Chemistry |
Palavras-Chave | #Anti-Bacterial Agents #Cations #Dose-Response Relationship, Drug #Gram-Negative Bacteria #Gram-Positive Bacteria #Microbial Sensitivity Tests #Norbornanes #Peptidomimetics #Structure-Activity Relationship |
Tipo |
Journal Article |