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Margarita S. Stiazhkina, Ulyana A. Budanova, Yuri L. Sebyakin

Alkyl-indole derivatives of unnatural tetrapeptides: synthesis and evaluation of biological activity


Abstract. Peptidomimetics are small molecules that are able to mimic the functional and structural features of peptides. The application of rational design during the development process allows their use as effective antibacterial agents with improved pharmacokinetic properties. In this work, we have constructed a series of cationic amphiphiles based on the alkyl-indole derivative of L-serine, differing in amino acid composition in the polar block and have potential antimicrobial activity. A universal preparation scheme has been developed, which makes it possible to obtain target compounds in quantities necessary for further study of biological properties. Based on the analysis of antimicrobial activity, it was found that structures with a higher lipophilicity value and a smaller polar block volume demonstrate the best results.
Key words: peptidomimetics, lipotetrapeptides, cationic amphiphiles, minimum inhibitory concentration, antibacterial activity
Moscow University Chemistry Bulletin.
2023, Vol. 64, No. 2, P. 187

Copyright (C) Chemistry Dept., Moscow State University, 2002
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