Fluorine in Medicinal Chemistry: A Century of Progress and a 60-Year Retrospective of Selected Highlights

Abstract

This perspective explores the origins of both fluorine and medicinal chemistry a century ago and traces the early history of the intersection of these areas and the subsequent roles that fluorine has played in advancing medicinal innovations and diagnoses during the past 60 years. The overview highlights remarkable breakthroughs in many diverse areas of medicinal chemistry, including inter alia, anesthetics, steroidal and nonsteroidal anti-inflammatory drugs, anticancer and antiviral agents, CNS medications, antibacterials and cholesterol biosynthesis inhibitors. The increasing use of fluorine-18-labeled radiotracers in PET for diagnostic imaging of the brain, heart and in oncology is briefly presented. The signature roles of fluorine in medicinal chemistry are now firmly established. The presence of fluorine in pharmaceuticals has had a major impact on a plethora of important medical applications, such as those cited above. Fluorine will very likely continue to contribute significantly by playing multifaceted roles in enhancing future medical advances.

Spectroscopic Investigation of cis-2,4-Difluorophenol Cation by Mass-analyzed Threshold Ionization Spectroscopy

“…[1][2][3] Many fluorinated benzene derivatives, [4][5][6][7][8][9][10][11][12][13][14][15][16] are extensively studied by various spectroscopic methods. 2-Fluorophenol is regarded as one of the classic example of intramolecular hydrogen-bonding systems which have been the subject of various studies.…”

Synthesis of Novel a-Amino Acids Bearing 1,2,4-triazinone and Steroidal Moieties as Enzymetic Affect (Cellobiase Activity) Part I

“…An increased binding affinity of fluorinated drug candidates to target protein has also been reported (Filler & Saha, 2009). …”

Study of Antiadenoviralactivity of New Fluorinecontaining Heterocyclic Compounds

“…Дальнейший прогресс в этом направлении исследований связан с синтезом новых фторированных нуклеозидов, а также более глубоком понимании механизмов их действия. [6,9,11,13].…”