In vitro and in vivo evaluation of fluorinated indanone derivatives as potential positron emission tomography agents for the imaging of monoamine oxidase B in the brain.
Copper-mediated radiofluorination
Fluorine-18
Indanone derivatives
MAO-B
PET tracers
Journal
Bioorganic & medicinal chemistry letters
ISSN: 1464-3405
Titre abrégé: Bioorg Med Chem Lett
Pays: England
ID NLM: 9107377
Informations de publication
Date de publication:
15 09 2021
15 09 2021
Historique:
received:
07
05
2021
revised:
30
06
2021
accepted:
05
07
2021
pubmed:
14
7
2021
medline:
5
1
2022
entrez:
13
7
2021
Statut:
ppublish
Résumé
Monoamine oxidases (MAOs) play a key role in the metabolism of major monoamine neurotransmitters. In particular, the upregulation of MAO-B in Parkinson's disease, Alzheimer's disease and cancer augmented the development of selective MAO-B inhibitors for diagnostic and therapeutic purposes, such as the anti-parkinsonian MAO-B irreversible binder l-deprenyl (Selegiline®). Herein we report on the synthesis of novel fluorinated indanone derivatives for PET imaging of MAO-B in the brain. Out of our series, the derivatives 6, 8, 9 and 13 are amongst the most affine and selective ligands for MAO-B reported so far. For the derivative 6-((3-fluorobenzyl)oxy)-2,3-dihydro-1H-inden-1-one (6) exhibiting an outstanding affinity (K
Identifiants
pubmed: 34256118
pii: S0960-894X(21)00481-9
doi: 10.1016/j.bmcl.2021.128254
pii:
doi:
Substances chimiques
Indans
0
Monoamine Oxidase Inhibitors
0
indacrinone
B926Y9U4QN
Monoamine Oxidase
EC 1.4.3.4
Types de publication
Journal Article
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM
Pagination
128254Informations de copyright
Copyright © 2021 Elsevier Ltd. All rights reserved.