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.
Bibliographical noteFunding Information:
We are grateful to the Ministry of Science and Technology (MOST) and Ministry of Commerce, Industry and Energy (MCIE) of Korea for financial support.
All Science Journal Classification (ASJC) codes
- Molecular Medicine
- Molecular Biology
- Pharmaceutical Science
- Drug Discovery
- Clinical Biochemistry
- Organic Chemistry