Oxetanyl Amino Acids for Peptidomimetics

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...

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Veröffentlicht in:Organic letters 2017-05, Vol.19 (10), p.2510-2513
Hauptverfasser: Möller, Guido P, Müller, Steffen, Wolfstädter, Bernd T, Wolfrum, Susanne, Schepmann, Dirk, Wünsch, Bernhard, Carreira, Erick M
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container_end_page 2513
container_issue 10
container_start_page 2510
container_title Organic letters
container_volume 19
creator Möller, Guido P
Müller, Steffen
Wolfstädter, Bernd T
Wolfrum, Susanne
Schepmann, Dirk
Wünsch, Bernhard
Carreira, Erick M
description 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.
doi_str_mv 10.1021/acs.orglett.7b00745
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title Oxetanyl Amino Acids for Peptidomimetics
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