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

Ji Hoon Lee, Seong Rim Byeon, YoungSoo Kim, Soo Jeong Lim, Seung Jun Oh, Dae Hyuk Moon, Kyung Ho Yoo, Bong Young Chung, Dong Jin Kim

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Abstract

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.

Original languageEnglish
Pages (from-to)5701-5704
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Volume18
Issue number20
DOIs
Publication statusPublished - 2008 Oct 15

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All Science Journal Classification (ASJC) codes

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

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