2. Academic Validation
  3. Tailor-made amino acids in the design of small-molecule blockbuster drugs

Tailor-made amino acids in the design of small-molecule blockbuster drugs

  • Eur J Med Chem. 2021 Aug 5:220:113448. doi: 10.1016/j.ejmech.2021.113448.
Jianlin Han 1,  Hiroyuki Konno 2,  Tatsunori Sato 3,  Vadim A Soloshonok 4,  Kunisuke Izawa 5
Affiliations

Affiliations

  • 1 Jiangsu Co-Innovation Center of Efficient Processing and Utilization of Forest Resources, College of Chemical Engineering, Nanjing Forestry University, Nanjing, 210037, Jiangsu, China.
  • 2 Department of Biological Engineering, Graduate School of Science and Engineering, Yamagata University, Yonezawa, Yamagata, 992-8510, Japan.
  • 3 Hamari Chemicals Ltd., 1-19-40, Nankokita, Suminoe-ku, Osaka, 559-0034, Japan.
  • 4 Department of Organic Chemistry I, Faculty of Chemistry, University of the Basque Country UPV/EHU, Paseo Manuel Lardizábal 3, 20018, San Sebastián, Spain; IKERBASQUE, Basque Foundation for Science, María Díaz de Haro 3, Plaza Bizkaia, 48013, Bilbao, Spain. Electronic address: [email protected].
  • 5 Hamari Chemicals Ltd., 1-19-40, Nankokita, Suminoe-ku, Osaka, 559-0034, Japan. Electronic address: [email protected].
PMID: 33906050 DOI: 10.1016/j.ejmech.2021.113448
Abstract

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.

Keywords

Amino-alcohols; Asymmetric synthesis; Blockbuster drugs; Diamines; Drug design and development; Modern pharmaceuticals; Small-molecule drugs; Tailor-made amino acids.

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