The Potential and Uniqueness of Fluorine in the Field of Medicinal Chemistry

Stavroula Koulocheri, A.

Department of Biological Chemistry, Medical School, National and Kapodistrian University of Athens, NKUA, Greece

Dr. Stavroula Koulocheri, A., Department of Biological Chemistry, Medical School, National and Kapodistrian University of Athens, NKUA, Greece.

Keywords: Fluorinated Drugs; Pharmaceutical; Fluoro-Substituent; Acid/Base Profile; Metabolic Stability; Binding Affinity

Abstract

The highly electronegative and unique fluorine incorporated to organic compounds can play an essential role in medicinal chemistry. The rational introduction of fluorine has the potential to modulate pKa, potency, membrane permeability and influence conformation, protein binding and pharmacokinetic properties. There are many applications of fluorine substitution in drug discovery and are progressively increasing in parallel with the development of new synthetic strategies and methodologies.
In this review the exploration of the interesting characteristics of the C-F bond in organofluorine compounds is described and some examples of marketed fluorinated medicines are shown. The many advantages of fluorine in candidate drugs constitute a great challenge for further optimisation and future development of drugs with high potency and efficacy.

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