Jiangsu Co-Innovation Center of Efficient Processing and Utilization of Forest Resources, College of Chemical Engineering, Nanjing Forestry University, Nanjing, 210037, Jiangsu, China.
Department of Biological Engineering, Graduate School of Science and Engineering, Yamagata University, Yonezawa, Yamagata, 992-8510, Japan.
Eur J Med Chem. 2021 Aug 5;220:113448. doi: 10.1016/j.ejmech.2021.113448. Epub 2021 Apr 16.
The role of amino acids (AAs) in modern health industry is well-appreciated. Residues of individual AAs, or their chemical modifications, such as diamines and amino alcohols, are frequently found in the structures of modern pharmaceuticals. The goal of this review article, is to emphasize that, currently, tailor-made AAs serve as key structural features in many most successful pharmaceuticals, so-called blockbuster drugs. In the present article, we profile 14 small-molecule drugs, underscoring the breadth of structural variety of AAs applications in numerous therapeutic areas. For each compound, we provide spectrum of biological activity, medicinal chemistry discovery, and synthetic approaches.
氨基酸（AAs）在现代健康产业中的作用备受关注。在现代药物的结构中，经常可以发现单个氨基酸的残基或其化学修饰物，如二胺和氨基醇。本文的目的是强调，目前，定制氨基酸是许多最成功的药物（所谓的重磅炸弹药物）的关键结构特征。在本文中，我们介绍了 14 种小分子药物，强调了在许多治疗领域中应用氨基酸结构多样性的广泛程度。对于每种化合物，我们提供了生物活性、药物化学发现和合成方法的范围。
