Binaphthyl-anchored antibacterial tripeptide derivatives with hydrophobic C-terminal amino acid variations

The facile synthesis of seven new dicationic tripeptide benzyl ester derivatives, with hydrophobic group variations in the C-terminal amino acid component, is described. Moderate to good activity was seen against Gram-positive bacteria in vitro. One cyclohexyl-substituted compound 2c was tested more...

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Detalles Bibliográficos
Autores principales: Bremner, John B, Keller, Paul A, Pyne, Stephen G, Robertson, Mark J, Sakthivel, K, Somphol, Kittiya, Baylis, Dean, Coates, Jonathan A, Deadman, John, Jeevarajah, Dharshini, Rhodes, David I
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Beilstein-Institut 2012
Materias:
Full Research Paper
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3458747/
https://www.ncbi.nlm.nih.gov/pubmed/23019457
http://dx.doi.org/10.3762/bjoc.8.142
Descripción
Sumario:The facile synthesis of seven new dicationic tripeptide benzyl ester derivatives, with hydrophobic group variations in the C-terminal amino acid component, is described. Moderate to good activity was seen against Gram-positive bacteria in vitro. One cyclohexyl-substituted compound 2c was tested more widely and showed good potency (MIC values ranging from 2–4 μg/mL) against antibiotic-resistant strains of Staphylococcus aureus and Enterococci (VRE, VSE), and against Staphylococcus epidermidis.

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