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 assays, were evaluated. Finally, conductivity measurements have been performed to elucidate ion channel forming properties.
Grotenbreg
Gijsbert M
GM
Leiden Institute of Chemistry, Gorlaeus Laboratories, P. O. Box 9502, 2300, RA Leiden, The Netherlands.
Witte
Martin D
MD
van Hoof
Peter A V
PA
Spalburg
Emile
E
Reiss
Philipp
P
Noort
Daan
D
de Neeling
Albert J
AJ
Koert
Ulrich
U
van der Marel
Gijsbert A
GA
Overkleeft
Herman S
HS
Overhand
Mark
M
D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D001419:Bacteria / Q000187:drug effects*; D019281:Dimerization; D006096:Gramicidin / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D006461:Hemolysis; D007473:Ion Channels / Q000737:chemistry; D008826:Microbial Sensitivity Tests; D008968:Molecular Conformation; D012680:Sensitivity and Specificity; D013329:Structure-Activity Relationship
D000900:Anti-Bacterial Agents; D007473:Ion Channels; D006096:Gramicidin