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A Platform of Anti-biofilm Assays Suited to the Exploration of Natural Compound Libraries
Published on: December 27, 2016
'Inverted' analogs of the antibiotic gramicidin S with an improved biological profile
Varsha V Kapoerchan1, Annemiek D Knijnenburg, Peter Keizer
1Bioorganic Synthesis, Leiden Institute of Chemistry, Leiden University, PO Box 9502, 2300 RA Leiden, The Netherlands.
Abstract:
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.
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