Inverted analogs of the antibiotic gramicidin S with an improved biological profile
de Neeling, A.J.
van Raaij, M.J.
van der Marel, G.A.
A series of gramicidin S derivatives 4-15 are presented that have four ornithine residues as polar protonated side chains and two central hydrophobic amino acids with unaltered turn regions. These peptides were screened against human erthrocytes and our standard panel of Gram negative- and Gram positive bacteria, including four MRSA strains. Based on the antibacterial- and hemolytic data, peptides 13 and 14 have an improved biological profile compared to the clinically applied topical antibiotic gramicidin S. © 2012 Elsevier Ltd. All rights reserved.
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Bioorganic and Medicinal Chemistry, 20 (20), 6059-6062