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Application and Methodology of the Non-destructive 19F Time-domain NMR Technique to Measure the Content in Fluorine-containing Drug Products
Published on: August 22, 2017
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Fluorine in medicinal chemistry.
1AstraZeneca, Alderley Park, Cheshire, United Kingdom.
Progress in Medicinal Chemistry
|March 3, 2015
Summary
Fluorine is a crucial element in medicinal chemistry, enhancing drug properties like potency and pharmacokinetics. This review explores fluorine
Area of Science:
- Medicinal Chemistry
- Organic Chemistry
- Drug Discovery
Background:
- Fluorine's incorporation into pharmaceuticals began in the late 1950s.
- The fluorine atom is a versatile tool for modifying molecular properties.
- Its use in drug design has become widespread and essential.
Purpose of the Study:
- To review the unique properties of fluorine in medicinal chemistry.
- To illustrate key strategies for optimizing drug molecules using fluorine.
- To highlight potential challenges associated with fluorine incorporation.
Main Methods:
- Survey of marketed fluorinated pharmaceuticals.
- Analysis of medicinal chemistry literature.
- Review of case studies demonstrating fluorine's impact.
Main Results:
- Fluorine substitution significantly impacts drug potency, pharmacokinetics, and physical chemistry.
- Specific examples showcase successful optimization of drug candidates through fluorination.
- Potential drawbacks and limitations of using fluorine are identified.
Conclusions:
- Fluorine is an indispensable element in modern drug discovery and development.
- Understanding fluorine's unique characteristics is key to successful medicinal chemistry.
- Careful consideration of potential pitfalls is necessary for effective drug design.
Keywords:
Conformational influences of fluorineFluorinated pharmaceuticalsFluorineFluorine in medicinal chemistryImpact of fluorine on lipophilicityImpact of fluorine on pK(a)Impact of fluorine on physical propertiesMolecular interactions of fluorine with proteinsToxic metabolites containing fluorineRelated Concept Videos
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