Publikationsrepositorium - Helmholtz-Zentrum Dresden-Rossendorf
1 PublikationSynthesis and radiofluorination of novel fluoren-9-one based derivatives for the imaging of α7 nicotinic acetylcholine receptor with PET
Teodoro, R.; Scheunemann, M.; Wenzel, B.; Peters, D.; Deuther-Conrad, W.; Brust, P.
Abstract
By structure-activity relationship studies on the tilorone scaffold, the ‘one armed’ substituted dibenzothiophenes and the fluoren-9-ones were identified as the most potential α7 nAChR ligands. While the suitability of dibenzothiophene derivatives as PET tracers is recognized, the potential of fluoren-9-ones is insufficiently investigated. We herein report on a series of fluoren-9-one based derivatives targeting α7 nAChR with compounds 8a and 8c possessing the highest affinity and selectivity. Accordingly, with [18F]8a and [18F]8c we designed and initially evaluated the first fluoren-9-one derived α7 nAChR selective PET ligands. A future application of these radioligands is facilitated by the herein presented successful implementation of fully automated radiosynthesis.
Keywords: α7 nAChR; PET; Radiofluorination; Fluoren-9-one; Dibenzothiophenes
Beteiligte Forschungsanlagen
- PET-Zentrum
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Bioorganic & Medicinal Chemistry Letters 28(2018), 1471-1475
DOI: 10.1016/j.bmcl.2018.03.081
Cited 6 times in Scopus
Permalink: https://www.hzdr.de/publications/Publ-27271