[18F]-labeled isoindol-1-one and isoindol-1,3-dione derivatives as potential PET imaging agents for detection of β-amyloid fibrils

In this study a novel series of isoindol-1-one and isoindol-1,3-dione derivatives for β-amyloid-specific binding agents is described. Twelve compounds were synthesized and evaluated via a competitive binding assay with [125I]TZDM against β-amyloid 1–42 (Aβ42) aggregates. Two new [18F]-labeled isoindole derivatives were synthesized and evaluated as potential β-amyloid imaging probes based on the in vivo pharmacokinetic profiles. The preliminary results suggest that these [18F]18b and [18F]18c are promising positron emission tomography (PET) imaging probes for studying accumulation of Aβ fibrils in the brains of Alzheimer’s disease (AD) patients.

Graphical abstractNovel series of isoindol-1-one and isoindol-1,3-dione derivatives for β-amyloid-specific binding agents were synthesized and evaluated by a competitive binding assay with [125I]TZDM against Aβ42 aggregates. Two new [18F]-labeled isoindole derivatives were synthesized and evaluated as potential β-amyloid imaging probes based on the in vivo pharmacokinetic profiles. In conclusion, these compounds are promising PET imaging probes for studying accumulation of Aβ fibrils in the brains of AD patients.Figure optionsDownload full-size imageDownload as PowerPoint slide