Synthesis and biological evaluation of novel turn-modified gramicidin S analogues.
The synthesis of novel gramicidin S analogues having additional functionalities in the turn region by employing a biomimetic approach is described. The preservation of beta-sheet character in all analogues was established by NMR and the biological activity was evaluated.
Grotenbreg
Gijsbert M
GM
Leiden Institute of Chemistry, Gorlaeus Laboratories, PO Box 9502, 2300 RA Leiden, The Netherlands.
Spalburg
Emile
E
de Neeling
Albert J
AJ
van der Marel
Gijsbert A
GA
Overkleeft
Herman S
HS
van Boom
Jacques H
JH
Overhand
Mark
M
D006090:Gram-Negative Bacteria / Q000187:drug effects; D006094:Gram-Positive Bacteria / Q000187:drug effects; D006096:Gramicidin / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology*; D008826:Microbial Sensitivity Tests; D018716:Molecular Mimicry; D019906:Nuclear Magnetic Resonance, Biomolecular; D017433:Protein Structure, Secondary
D006096:Gramicidin