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Genetic polymorphisms in drug targets have emerged as critical determinants of interindividual variability in drug response and toxicity. Pharmacogenomic investigations increasingly focus on identifying these variations to personalize and optimize therapeutic interventions. A drug target may be a receptor, enzyme, or signaling protein involved in pharmacologic responses or disease-related pathways. While early pharmacogenetic studies focused primarily on drug metabolism, current research...
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Group 17 elements, known as halogens, are nonmetals. At room temperature, fluorine and chlorine are gases, bromine is a liquid, and iodine a solid. Astatine is a highly unstable radioactive element, so currently, most of its properties are unknown due to its short half-life. Tennessine is a synthetic element also predicted to be in this group. 
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Polyfluorinated groups in medicinal chemistry.

Marcella Bassetto1, Salvatore Ferla, Fabrizio Pertusati

  • 1School of Pharmacy & Pharmaceutical Sciences, Cardiff University, Redwood Building, King Edwards VII Avenue, Cardiff, United Kingdom.

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Polyfluorinated groups offer benefits in drug discovery, enhancing activity and reducing toxicity. Further research into these moieties is crucial for developing new pharmaceuticals.

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Area of Science:

  • Medicinal Chemistry
  • Drug Discovery
  • Organic Fluorine Chemistry

Background:

  • Fluorine incorporation is a validated strategy in medicinal chemistry.
  • Polyfluoroalkyl groups, beyond trifluoromethyl, remain underexplored in drug design.
  • Hesitancy exists for novel functional groups until efficacy and safety are confirmed.

Purpose of the Study:

  • To demonstrate the advantages of polyfluorinated groups in pharmaceutical compounds.
  • To highlight structure-activity relationship (SAR) studies supporting polyfluorinated moieties.
  • To advocate for the increased exploration of higher polyfluoroalkyl/aryl groups.

Main Methods:

  • Structure-Activity Relationship (SAR) analysis.
  • Evaluation of polyfluorinated moieties in drug candidates.
  • Comparative studies of fluorinated vs. non-fluorinated compounds.

Main Results:

  • Polyfluorinated groups significantly enhance the properties of active pharmaceutical ingredients.
  • SAR studies identified specific polyfluorinated moieties as key structural features.
  • The potential of higher polyfluoroalkyl/aryl groups is demonstrated.

Conclusions:

  • Polyfluorinated groups are valuable tools in medicinal chemistry.
  • Further investigation into higher polyfluoroalkyl/aryl moieties is warranted.
  • These groups are expected to gain prominence in future drug discovery.