An adamantyl amino acid containing gramicidin S analogue with broad spectrum antibacterial activity and reduced hemolytic activity
de Neeling, A.J.
van Raaij, M.J.
van der Marel, G.A.
TNO Defensie en Veiligheid
The cyclic cationic antimicrobial peptide gramicidin S (GS) is an effective topical antibacterial agent that is toxic for human red blood cells (hemolysis). Herein, we present a series of amphiphilic derivatives of GS with either two or four positive charges and characteristics ranging between very polar and very hydrophobic. Screening of this series of peptide derivatives identified a compound that combines effective antibacterial activity with virtually no toxicity within the same concentration range. This peptide acts against both Gram-negative and Gram-positive bacteria, including several MRSA strains, and represents an interesting lead for the development of a broadly applicable antibiotic. © 2010 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.
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Methicillin-resistant Staphylococcus aureus (MRSA)
Chemistry - A European Journal, 16 (40), 12174-12181