Structure–Function Relationship between Analogues of the Antibacterial Peptide Indolicidin. I. Synthesis and Biological Activity of Analogues with Increased Amphipathicity and Elevated Net Positive Charge of the Molecule

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The antibacterial peptide indolicidin and a number of its analogues were obtained by solid phase synthesis. An optimized method of the synthesis using the Boc strategy was suggested. It was shown that the therapeutic index of indolicidin analogues increased with a decrease in the total positive charge of the molecule and its amphipathicity; i.e., the hemolytic activity of analogues within the range of concentrations examined was practically absent, while the antibacterial activity was preserved.

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