Journal ArticleDOI
Applications of fluorine-containing amino acids for drug design.
Haibo Mei,Jianlin Han,Karel D. Klika,Kunisuke Izawa,Tatsunori Sato,Nicholas A. Meanwell,Vadim A. Soloshonok,Vadim A. Soloshonok +7 more
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TLDR
The goal of this Review article is to highlight the current state-of-the-art in this area by profiling 42 selected compounds that combine fluorine and amino acid structural elements, including examples of drug-candidates that although withdrawn from development had a significant impact on the progress of medicinal chemistry and/or provided a deeper understanding of the nature and mechanism of biological action.About:
This article is published in European Journal of Medicinal Chemistry.The article was published on 2020-01-15. It has received 122 citations till now.read more
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Journal ArticleDOI
Next generation organofluorine containing blockbuster drugs
Jianlin Han,Attila Márió Remete,Luca S. Dobson,Loránd Kiss,Kunisuke Izawa,Hiroki Moriwaki,Vadim A. Soloshonok,Vadim A. Soloshonok,David O'Hagan +8 more
TL;DR: This Review highlights a selection of the most successful organo-fluorine drugs, that have achieved blockbuster status, namely, sitagliptin (diabetes), sofosbuvir (hepatitis C), emtricitabine (HIV), glecaprevir/pibrentasvir ( hepatitisC), elvitegravir (Hiv), dolutegravirs (H HIV), bictegravIR (H IV),
Journal ArticleDOI
Fluorine-containing drugs approved by the FDA in 2019
Haibo Mei,Attila Márió Remete,Yupiao Zou,Hiroki Moriwaki,Santos Fustero,Loránd Kiss,Vadim A. Soloshonok,Vadim A. Soloshonok,Jianlin Han +8 more
TL;DR: Eleven new fluorine-containing FDA-approved drugs have been profiled and details of their discovery and preparation are discussed, including four examples of aromatic fluorine, three aromatic CF3 group, three aliphatic CF3 and one compound with aromaticCF3O group.
Journal ArticleDOI
Chemical Aspects of Human and Environmental Overload with Fluorine
Jianlin Han,Loránd Kiss,Haibo Mei,Attila Márió Remete,Maja Ponikvar-Svet,Daniel M. Sedgwick,Raquel Román,Santos Fustero,Hiroki Moriwaki,Vadim A. Soloshonok,Vadim A. Soloshonok +10 more
TL;DR: A comprehensive and critical review of the effects of fluoride ions and organofluorine compounds (mainly pharmaceuticals and agrochemicals) on human health and the environment is presented in this article.
Journal ArticleDOI
Visible-Light Photoredox-Catalyzed Remote Difunctionalizing Carboxylation of Unactivated Alkenes with CO 2
Lei Song,Dong-Min Fu,Liang Chen,Yuan-Xu Jiang,Jian-Heng Ye,Lei Zhu,Yu Lan,Yu Lan,Qiang Fu,Da-Gang Yu +9 more
TL;DR: This visible-light photoredox catalysis strategy provides a facile method to synthesize a series of carboxylic acids, such as non-natural α-amino acids, bearing valuable fluorine- or phosphorus-containing functional groups, and shows mild reaction conditions, broad substrate scope, and good functional group tolerance.
Journal ArticleDOI
Tailor-Made Amino Acids and Fluorinated Motifs as Prominent Traits in Modern Pharmaceuticals.
Haibo Mei,Jianlin Han,Sarah White,Daniel J. Graham,Kunisuke Izawa,Tatsunori Sato,Santos Fustero,Nicholas A. Meanwell,Vadim A. Soloshonok,Vadim A. Soloshonok +9 more
TL;DR: This review profiles 39 selected compounds featuring both of these traits in the same molecule, the total synthesis, source of the corresponding amino acids and fluorinated residues, and the medicinal chemistry aspects and biological properties of the molecules.
References
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Applications of Fluorine in Medicinal Chemistry
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