Binaphthyl-anchored antibacterial tripeptide derivatives with hydrophobic C-terminal amino acid variations
oleh: 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
| Format: | Article |
|---|---|
| Diterbitkan: | Beilstein-Institut 2012-08-01 |
Deskripsi
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.