New pharmaceuticals approved by FDA in 2020: Small-molecule drugs derived from amino acids and related compounds

被引:30
|
作者
Liu, Aiyao [1 ]
Han, Jianlin [1 ]
Nakano, Arina [2 ]
Konno, Hiroyuki [2 ]
Moriwaki, Hiroki [3 ]
Abe, Hidenori [3 ]
Izawa, Kunisuke [3 ]
Soloshonok, Vadim A. [4 ,5 ]
机构
[1] Nanjing Forestry Univ, Coll Chem Engn, Jiangsu Co Innovat Ctr Efficient Proc & Utilizat, Nanjing 210037, Jiangsu, Peoples R China
[2] Yamagata Univ, Grad Sch Sci & Engn, Dept Biol Engn, Yonezawa, Yamagata, Japan
[3] Hamari Chem Ltd, Osaka, Japan
[4] Univ Basque Country UPV EHU, Fac Chem, Dept Organ Chem 1, Paseo Manuel Lardizabal 3, San Sebastian 20018, Spain
[5] Basque Fdn Sci, IKERBASQUE, Bilbao, Spain
基金
中国国家自然科学基金;
关键词
anticancer; asymmetric synthesis; biological activity; COVID-19; peptides; peptidomimetics; small-molecule drugs; tailor-made amino acids; DYNAMIC KINETIC RESOLUTION; CGRP-RECEPTOR ANTAGONISTS; ASYMMETRIC-SYNTHESIS; SELF-DISPROPORTIONATION; NI(II) COMPLEXES; NEUROENDOCRINE TUMORS; ADDITION-REACTIONS; R INTERCONVERSION; ENANTIOMERS SDE; SCHIFF-BASES;
D O I
10.1002/chir.23376
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Amino acids (AAs) play an important role in the modern health industry as key synthetic precursors for pharmaceuticals, biomaterials, biosensors, and drug delivery systems. Currently, over 30% of small-molecule drugs contain residues of tailor-made AAs or derived from them amino-alcohols and di-amines. In this review article, we profile 12 AA-derived new pharmaceuticals approved by the FDA in 2020. These newly introduced drugs include Tazverik (epithelioid sarcoma), Gemtesa (overactive bladder), Zeposia (multiple sclerosis), Byfavo (induction and maintenance of procedural sedation), Cu 64 dotatate, and Gallium 68 PSMA-11 (both PET imaging), Rimegepant (acute migraine), Zepzelca (lung cancer), Remdesivir (COVID-19), Amisulpride (nausea and vomiting), Setmelanotide (obesity), and Lonafarnib (progeria syndrome). For each compound, we describe the spectrum of biological activity, medicinal chemistry discovery, and synthetic preparation.
引用
收藏
页码:86 / 103
页数:18
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