Synthesis and biological evaluation of gramicidin S dimers

The design and synthesis of analogues of the cyclic beta-sheet gramicidin S (GS), having additional functionalities in their turn regions, is reported. The monomeric GS analogues were transformed into dimers and their activities towards biological membranes, through antimicriobial and hemolytic assa...

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Veröffentlicht in:	Organic & biomolecular chemistry 2005-01, Vol.3 (2), p.233-238
Hauptverfasser:	Grotenbreg, Gijsbert M, Witte, Martin D, van Hoof, Peter A V, Spalburg, Emile, Reiss, Philipp, Noort, Daan, de Neeling, Albert J, Koert, Ulrich, van der Marel, Gijsbert A, Overkleeft, Herman S, Overhand, Mark
Format:	Artikel
Sprache:	eng
Schlagworte:	Anti-Bacterial Agents - chemical synthesis Anti-Bacterial Agents - chemistry Anti-Bacterial Agents - pharmacology Bacteria - drug effects Dimerization Gramicidin - chemical synthesis Gramicidin - chemistry Gramicidin - pharmacology Hemolysis Ion Channels - chemistry Microbial Sensitivity Tests Molecular Conformation Sensitivity and Specificity Structure-Activity Relationship
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Beschreibung
Zusammenfassung:	The design and synthesis of analogues of the cyclic beta-sheet gramicidin S (GS), having additional functionalities in their turn regions, is reported. The monomeric GS analogues were transformed into dimers and their activities towards biological membranes, through antimicriobial and hemolytic assays, were evaluated. Finally, conductivity measurements have been performed to elucidate ion channel forming properties.
ISSN:	1477-0520 1477-0539
DOI:	10.1039/b414618b