Format

Send to

Choose Destination
Bioorg Med Chem Lett. 2018 May 15;28(9):1471-1475. doi: 10.1016/j.bmcl.2018.03.081. Epub 2018 Mar 29.

Synthesis and radiofluorination of novel fluoren-9-one based derivatives for the imaging of α7 nicotinic acetylcholine receptor with PET.

Author information

1
Helmholtz-Zentrum Dresden-Rossendorf, Institute of Radiopharmaceutical Cancer Research, Permoserstraße 15, Leipzig 04318, Germany. Electronic address: r.teodoro@hzdr.de.
2
Helmholtz-Zentrum Dresden-Rossendorf, Institute of Radiopharmaceutical Cancer Research, Permoserstraße 15, Leipzig 04318, Germany.
3
DanPET AB, Rosenstigen 7, Malmö SE-21619, Sweden.

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:

Dibenzothiophenes; Fluoren-9-one; PET; Radiofluorination; α7 nAChR

PMID:
29628323
DOI:
10.1016/j.bmcl.2018.03.081
[Indexed for MEDLINE]

Supplemental Content

Full text links

Icon for Elsevier Science
Loading ...
Support Center