Amino acids (AAs) are among a handful of paramount classes of compounds innately involved in the origin and evolution of all known life-forms. Along with basic scientific explorations, the major goal of medicinal chemistry research in the area of tailor-made AAs is the development of more selective and potent pharmaceuticals. The growing acceptance of peptides and peptidomimetics as drugs clearly indicates that AA-based molecules become the most successful structural motif in the modern drug design. In fact, among 24 small-molecule drugs approved by FDA in 2019, 13 of them contain a residue of AA or di-amines or amino-alcohols, which are commonly considered to be derived from the parent AAs. In the present review article, we profile 13 new tailor-made AA-derived pharmaceuticals introduced to the market in 2019. Where it is possible, we will discuss the development form drug-candidates, total synthesis, with emphasis on the core-AA, therapeutic area, and the mode of biological activity.

氨基酸（AAs）是与所有已知生命形式的起源和进化固有相关的少数最重要的化合物之一。除基础科学探索外，量身定制的AA领域中药物化学研究的主要目标是开发更具选择性和效力的药物。越来越多的人们接受肽和拟肽药物作为药物，这清楚地表明，基于AA的分子成为现代药物设计中最成功的结构基序。事实上，在2019年FDA批准的24种小分子药物中，其中13种含有AA或二胺或氨基醇的残基，通常被认为是从母体AA衍生而来的。在本评论文章中，我们介绍了2019年投放市场的13种量身定制的AA衍生药品。