American Chemical Society
ol7b00745_si_003.cif (1.07 MB)

Oxetanyl Amino Acids for Peptidomimetics

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posted on 2017-05-01, 17:50 authored by Guido P. Möller, Steffen Müller, Bernd T. Wolfstädter, Susanne Wolfrum, Dirk Schepmann, Bernhard Wünsch, Erick M. Carreira
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.