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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…

文献索引: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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被引用次数: 30

摘要

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 ...