Highly functionalized cyclic beta-amino acid moieties as promising scaffolds in peptide research and drug design

Kiss, Loránd and Mándity, István M. and Fülöp, Ferenc (2017) Highly functionalized cyclic beta-amino acid moieties as promising scaffolds in peptide research and drug design. AMINO ACIDS, 49 (9). pp. 1441-1455. ISSN 0939-4451 (print); 1438-2199 (online)

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Abstract

Peptide-based drug research has received high attention in the field of medicinal chemistry over the past decade. For drug design, to improve proteolytic stability, it is desirable to include unnatural building blocks, such as conformationally restricted beta-amino acid moieties, into the peptide sequence. Accordingly, the synthesis and incorporation of such conformationally rigid systems into novel type of peptides has gained large interest. Our research group has designed highly efficient methods for the construction of potential antimicrobial peptides. Moreover, a number of synthetic approaches have been developed for the synthesis of various pharmacologically interesting cyclic beta-amino acid derivatives as monomers with multiple stereogenic centers.

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