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

Autor: John B. Bremner, Paul A. Keller, Stephen G. Pyne, Mark J. Robertson, K. Sakthivel, Kittiya Somphol, Dean Baylis, Jonathan A. Coates, John Deadman, Dharshini Jeevarajah, David I. Rhodes
Jazyk: angličtina
Rok vydání: 2012
Předmět:
Zdroj: Beilstein Journal of Organic Chemistry, Vol 8, Iss 1, Pp 1265-1270 (2012)
Druh dokumentu: article
ISSN: 1860-5397
DOI: 10.3762/bjoc.8.142
Popis: 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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