Fluorinated Diaryl Sulfides

Nashwa      Jarkas

doi:10.2174/1568026611313080006

Abstract

Diaryl sulfides also known as diphenyl sulfides, phenylthiobenzylamines, and biphenylthiols are a class of compounds with phenylthiophenyl scaffold that have been validated as biomarkers to label the brain serotonin transporter (SERT), in vivo. The development of those synthetic and non-natural compounds started more than a decade ago when the observation that 5-chloro-((2-((dimethylamino)methyl)phenyl)thio)benzene-methanol hydrochloride also called 403U76 inhibited the serotonin and norepinephrine uptake into rat brain synaptosomes, led to the preparation of few derivatives based on 403U76 chemical structure. The new class of compounds, called the diaryl sulfide family, was investigated as biomarkers for the brain SERT. The promising data demonstrated by the carbon-11 labeled diaryl sulfides led to the translation of few of them into humans and the further evaluation of the phenylthiophenyl core structure by developing some fluorinated derivatives. This review will mainly focus on the fluorinated diaryl sulfides as fluorine-containing tracers validated to image the human brain SERT using positron emission tomography.

Keywords: Biphenylthiols, Diaryl Sulfides, Diphenyl Sulfides, Fluorine-18, Phenylthiobenzylamines, Serotonin Transporter.

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