3 years ago

Oxetanyl Amino Acids for Peptidomimetics

Oxetanyl Amino Acids for Peptidomimetics
Susanne Wolfrum, Erick M. Carreira, Bernhard Wünsch, Dirk Schepmann, Guido P. Möller, Steffen Müller, Bernd T. Wolfstädter
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.

Publisher URL: http://dx.doi.org/10.1021/acs.orglett.7b00745

DOI: 10.1021/acs.orglett.7b00745

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