Development of an 18 F-labeled azobenzothiazole tracer for α-synuclein aggregates in the brain

Nuclear imaging of aggregated α-synuclein pathology is an urgent clinical need for Parkinson's disease, yet promising tracers for brain α-synuclein aggregates are still rare. In this work, a class of compact benzothiazole derivatives was synthesized and evaluated for α-synuclein aggregates. Amo...

Ausführliche Beschreibung

Gespeichert in:
Bibliographische Detailangaben
Veröffentlicht in:Organic & biomolecular chemistry 2024-06, Vol.22 (22), p.4550-4558
Hauptverfasser: Wu, Jiajun, Mao, Meiting, Yang, Jie, Li, Kexin, Deng, Pengxin, Zhong, Jing, Wu, Xiaoai, Cheng, Yan
Format: Artikel
Sprache:eng
Schlagworte:
Online-Zugang:Volltext
Tags: Tag hinzufügen
Keine Tags, Fügen Sie den ersten Tag hinzu!
Beschreibung
Zusammenfassung:Nuclear imaging of aggregated α-synuclein pathology is an urgent clinical need for Parkinson's disease, yet promising tracers for brain α-synuclein aggregates are still rare. In this work, a class of compact benzothiazole derivatives was synthesized and evaluated for α-synuclein aggregates. Among them, azobenzothiazoles exhibited specific and selective detection of α-synuclein aggregates under physiological conditions. Fluoro-pegylated azobenzothiazole NN-F further demonstrated high-affinity binding to α-synuclein aggregates and efficient F-radiolabeling nucleophilic displacement of a tosyl precursor. [ F]NN-F was stable in plasma and showed efficient brain uptake with little defluorination .
ISSN:1477-0520
1477-0539
DOI:10.1039/d4ob00492b