CHIRAL, FLUORINE-CONTAINING PHARMACEUTICALS

Fluorine is a key element in drug design due to its ability to enhance metabolic stability, binding affinity, and bioavailability. Fluorine’s properties lead to more stable drugs with longer half-lives, reducing dosing frequency and improving patient compliance. Its small size and high electronegati...

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Бібліографічні деталі
Дата:2025
Автори: Han, Jianlin, Wzorek, Alicja, Dhawan, Gagan, Zhang, Wei, Sorochinsky, Alexander, Baecker, Daniel, Ono, Taizo, Klika, Karel, Soloshonok, Vadim
Формат: Стаття
Мова:English
Опубліковано: V.I.Vernadsky Institute of General and Inorganic Chemistry 2025
Онлайн доступ:https://ucj.org.ua/index.php/journal/article/view/710
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Назва журналу:Ukrainian Chemistry Journal

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Ukrainian Chemistry Journal
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spelling oai:ojs2.1444248.nisspano.web.hosting-test.net:article-7102025-04-28T12:40:53Z CHIRAL, FLUORINE-CONTAINING PHARMACEUTICALS Han, Jianlin Wzorek, Alicja Dhawan, Gagan Zhang, Wei Sorochinsky, Alexander Baecker, Daniel Ono, Taizo Klika, Karel Soloshonok, Vadim Fluorine, chirality, drug design, pharmaceuticals, self-disproportionation of enantiomers, bioactivity. Fluorine is a key element in drug design due to its ability to enhance metabolic stability, binding affinity, and bioavailability. Fluorine’s properties lead to more stable drugs with longer half-lives, reducing dosing frequency and improving patient compliance. Its small size and high electronegativity also improve binding affinity, resulting in more effective treatments with lower doses. For example, fluorine increases a compound’s ability to cross cell memb­ranes. This article highlights advancements in chiral, fluorine-containing pharmaceuticals introduced over the past five years, focusing on their synthesis, therapeutic benefits, mechanisms of action, and the impact of fluorine on efficacy and safety. Chiral molecules, essential in drug development, exist in two enantiomeric forms with distinct biological activities. Synthesizing chiral, fluorine-containing drugs involves techniques like asymmetric synthesis to produce pure enantiomers, resulting in drugs with increased potency, selectivity, and reduced side effects. Understanding their mechanisms of action provides valuable insights into efficacy and safety. Reviewing recently FDA-approved chiral drugs offers insights into fluorine chemistry in drug development and future therapeutic innovations. Recent FDA approvals highlight the significance of chiral, fluorine-containing drugs in various therapeutic areas, enabling targeted and effective treatments. Analyzing these approvals reveals trends shaping drug development’s future. The article also addresses the need for more research into self-disproportionation of enantiomers (SDE) in chiral, fluorinated compounds and concerns about excessive fluorine levels. SDE can affect pharmaceutical product purity. Research into SDE in fluorinated compounds ensures drug quality. Additionally, fluorine’s widespread use raises environmental and health concerns, necessitating studies on long-term effects and mitigation strategies. V.I.Vernadsky Institute of General and Inorganic Chemistry 2025-03-25 Article Article Organic chemistry Органическая xимия Органічна xімія application/pdf https://ucj.org.ua/index.php/journal/article/view/710 10.33609/2708-129X.91.2.2025.55-90 Ukrainian Chemistry Journal; Vol. 91 No. 2 (2025): Ukrainian Chemistry Journal; 55-90 Украинский химический журнал; Том 91 № 2 (2025): Ukrainian Chemistry Journal; 55-90 Український хімічний журнал; Том 91 № 2 (2025): Ukrainian Chemistry Journal; 55-90 2708-129X 2708-1281 en https://ucj.org.ua/index.php/journal/article/view/710/359
institution Ukrainian Chemistry Journal
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datestamp_date 2025-04-28T12:40:53Z
collection OJS
language English
topic_facet Fluorine
chirality
drug design
pharmaceuticals
self-disproportionation of enantiomers
bioactivity.
format Article
author Han, Jianlin
Wzorek, Alicja
Dhawan, Gagan
Zhang, Wei
Sorochinsky, Alexander
Baecker, Daniel
Ono, Taizo
Klika, Karel
Soloshonok, Vadim
spellingShingle Han, Jianlin
Wzorek, Alicja
Dhawan, Gagan
Zhang, Wei
Sorochinsky, Alexander
Baecker, Daniel
Ono, Taizo
Klika, Karel
Soloshonok, Vadim
CHIRAL, FLUORINE-CONTAINING PHARMACEUTICALS
author_facet Han, Jianlin
Wzorek, Alicja
Dhawan, Gagan
Zhang, Wei
Sorochinsky, Alexander
Baecker, Daniel
Ono, Taizo
Klika, Karel
Soloshonok, Vadim
author_sort Han, Jianlin
title CHIRAL, FLUORINE-CONTAINING PHARMACEUTICALS
title_short CHIRAL, FLUORINE-CONTAINING PHARMACEUTICALS
title_full CHIRAL, FLUORINE-CONTAINING PHARMACEUTICALS
title_fullStr CHIRAL, FLUORINE-CONTAINING PHARMACEUTICALS
title_full_unstemmed CHIRAL, FLUORINE-CONTAINING PHARMACEUTICALS
title_sort chiral, fluorine-containing pharmaceuticals
description Fluorine is a key element in drug design due to its ability to enhance metabolic stability, binding affinity, and bioavailability. Fluorine’s properties lead to more stable drugs with longer half-lives, reducing dosing frequency and improving patient compliance. Its small size and high electronegativity also improve binding affinity, resulting in more effective treatments with lower doses. For example, fluorine increases a compound’s ability to cross cell memb­ranes. This article highlights advancements in chiral, fluorine-containing pharmaceuticals introduced over the past five years, focusing on their synthesis, therapeutic benefits, mechanisms of action, and the impact of fluorine on efficacy and safety. Chiral molecules, essential in drug development, exist in two enantiomeric forms with distinct biological activities. Synthesizing chiral, fluorine-containing drugs involves techniques like asymmetric synthesis to produce pure enantiomers, resulting in drugs with increased potency, selectivity, and reduced side effects. Understanding their mechanisms of action provides valuable insights into efficacy and safety. Reviewing recently FDA-approved chiral drugs offers insights into fluorine chemistry in drug development and future therapeutic innovations. Recent FDA approvals highlight the significance of chiral, fluorine-containing drugs in various therapeutic areas, enabling targeted and effective treatments. Analyzing these approvals reveals trends shaping drug development’s future. The article also addresses the need for more research into self-disproportionation of enantiomers (SDE) in chiral, fluorinated compounds and concerns about excessive fluorine levels. SDE can affect pharmaceutical product purity. Research into SDE in fluorinated compounds ensures drug quality. Additionally, fluorine’s widespread use raises environmental and health concerns, necessitating studies on long-term effects and mitigation strategies.
publisher V.I.Vernadsky Institute of General and Inorganic Chemistry
publishDate 2025
url https://ucj.org.ua/index.php/journal/article/view/710
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