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Total Synthesis of Septocylindrin B and C-Terminus Modified Analogues |
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| Authors: | Jo Nelissen Koen Nuyts Marta De Zotti Rob Lavigne Chris Lamberigts Wim M. De Borggraeve |
| Affiliation: | 1. Molecular Design and Synthesis, Department of Chemistry, University of Leuven, Heverlee, Belgium.; 2. Department of Chemistry, University of Padova, Padova, Italy.; 3. Laboratory of Gene Technology, Biosystems Department, University of Leuven, Heverlee, Belgium.; Bioinformatics Institute, Singapore, |
| Abstract: | The total synthesis is reported of the peptaibol Septocylindrin B which is related to the well documented channel forming peptaibol antibiotic Alamethicin. Several analogues were synthesized with a modified C-terminus, to investigate the SAR of the terminal residue Phaol. All these peptides were tested for their membrane perturbation properties by fluorescent dye leakage assay and for their antibacterial activity. |
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