作为拟肽骨架的杂环化合物：固相合成策略

Abdildinova Aizhan, Kurth Mark J, Gong Young-Dae

Innovative Drug Library Research Center, Department of Chemistry, College of Science, Dongguk University, 26, 3-ga, Pil-dong, Jung-gu, Seoul 04620, Korea.

Department of Chemistry, University of California, Davis, CA 95616, USA.

Pharmaceuticals (Basel). 2021 May 10;14(5):449. doi: 10.3390/ph14050449.

Peptidomimetics are a privileged class of pharmacophores that exhibit improved physicochemical and biological properties. Solid-phase synthesis is a powerful tool for gaining rapid access to libraries of molecules from small molecules to biopolymers and also is widely used for the synthesis of peptidomimetics. Small molecules including heterocycles serve as a core for hundreds of drugs, including peptidomimetic molecules. This review covers solid-phase synthesis strategies for peptidomimetics molecules based on heterocycles.

肽模拟物是一类具有特殊优势的药效基团，具有改善的物理化学和生物学性质。固相合成是一种强大的工具，可用于快速构建从小分子到生物聚合物的分子库，也广泛用于肽模拟物的合成。包括杂环化合物在内的小分子作为数百种药物（包括肽模拟物分子）的核心。本综述涵盖了基于杂环的肽模拟物分子的固相合成策略。