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.

肽类化合物在药物发现过程中扮演着至关重要的角色。与无肽的小分子类似物相比，它们有时会遭遇诸如生物利用度低和代谢稳定性差等不利因素。本研究中，我们报道了新型氧杂环二肽的合成及其被纳入亮氨酸脑啡肽类似物中的原理性研究。所描述的模块化方法使得将多种氧杂环氨基酸融入潜在的肽类治疗药物成为可能。