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

被引：1
作者：
Wu, Jiajun [1 ,2 ]
Mao, Meiting [1 ,2 ]
Yang, Jie [1 ,2 ]
Li, Kexin [1 ,2 ]
Deng, Pengxin [1 ,2 ]
Zhong, Jing [1 ,2 ]
Wu, Xiaoai [3 ]
Cheng, Yan [1 ,2 ]
机构：
[1] Sichuan Univ, Sichuan Engn Lab Plant Sourced Drug, Key Lab Drug Targeting & Drug Delivery Syst, West China Sch Pharm,Educ Minist & Sichuan Prov, Chengdu 610041, Peoples R China
[2] Sichuan Univ, Sichuan Res Ctr Drug Precis Ind Technol, West China Sch Pharm, Chengdu 610041, Peoples R China
[3] Sichuan Univ, West China Hosp, Dept Nucl Med, Lab Clin Nucl Med, Chengdu 610041, Peoples R China
来源：
ORGANIC & BIOMOLECULAR CHEMISTRY | 2024年 / 22卷 / 22期
关键词：
DERIVATIVES; LIGANDS; BINDING; ISOMERIZATION; DESIGN; TAU;
D O I：
10.1039/d4ob00492b
中图分类号：
O62 [有机化学];
学科分类号：
070303 ; 081704 ;
摘要：
Nuclear imaging of aggregated alpha-synuclein pathology is an urgent clinical need for Parkinson's disease, yet promising tracers for brain alpha-synuclein aggregates are still rare. In this work, a class of compact benzothiazole derivatives was synthesized and evaluated for alpha-synuclein aggregates. Among them, azobenzothiazoles exhibited specific and selective detection of alpha-synuclein aggregates under physiological conditions. Fluoro-pegylated azobenzothiazole NN-F further demonstrated high-affinity binding to alpha-synuclein aggregates and efficient F-18-radiolabeling via nucleophilic displacement of a tosyl precursor. [F-18]NN-F was stable in plasma in vitro and showed efficient brain uptake with little defluorination in vivo.
引用
收藏
页码：4550 / 4558
页数：9
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