Laboratorium für Organische Chemie, ETH Zürich , Vladimir-Prelog-Weg 3, 8093 Zürich, Switzerland.
Competence Center for Systems Physiology and Metabolic Diseases, Schorenstrasse 16, 8603 Schwerzenbach, Switzerland.
Org Lett. 2017 May 19;19(10):2510-2513. doi: 10.1021/acs.orglett.7b00745. Epub 2017 May 1.
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.
肽在药物发现过程中很重要。与非肽类小分子类似物相比，它们有时会受到一些缺点的影响，如生物利用度低和代谢稳定性差。在本文中，我们报告了新的氧杂环丁烷二肽的合成及其作为原理验证研究被纳入亮氨酸脑啡肽类似物。所描述的模块化方法能够将各种氧杂环丁烷氨基酸纳入潜在的肽治疗药物中。
