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 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.