Synthesis of fluorine substituted pyrazolopyrimidines as potential leads for the development of PET-imaging agents for the GABA A receptors

A Hoepping, M Diekers, W Deuther-Conrad…

Index: Hoepping, Alexander; Diekers, Michael; Deuther-Conrad, Winnie; Scheunemann, Matthias; Fischer, Steffen; Hiller, Achim; Wegner, Florian; Steinbach, Joerg; Brust, Peter Bioorganic and Medicinal Chemistry, 2008 , vol. 16, # 3 p. 1184 - 1194

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Citation Number: 30

Abstract

Neuroimaging of GABAA receptors offers the potential for a better diagnosis of diseases related to a dysfunction of the GABAergic neurotransmission. A series of potent fluorinated analogues of the pyrazolopyrimidine Indiplon has been synthesized and evaluated in vitro as potential agents for imaging the GABAA receptor by means of positron emission tomography (PET). The most promising compound N-(3-fluoropropyl)-N-[3-[3-(thiophene-2 ...

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