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Oxetanyl Amino Acids for Peptidomimetics

Author:
Möller, Guido P., Müller, Steffen, Wolfstädter, Bernd T., Wolfrum, Susanne, Schepmann, Dirk, Wünsch, Bernhard, Carreira, Erick M.
Source:
Organic letters 2017 v.19 no.10 pp. 2510-2513
ISSN:
1523-7052
Subject:
amino acids, bioavailability, chemical reactions, chemical structure, dipeptides, drugs, organic compounds, therapeutics
Abstract:
Peptides are important in the drug discovery process. In analogy to nonpeptidic small-molecule counterparts, they can sometimes suffer from disadvantages such as their low bioavailability and poor metabolic stability. Herein, we report the synthesis of new oxetanyl dipeptides and their incorporation into Leu-enkephalin analogues as proof-of-principle studies. The modular approach that is described enables the incorporation of a variety of oxetanyl amino acids into potential peptide therapeutics.
Agid:
5792841