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