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[F-18]-labeled isoindol-1-one and isoindol-1,3-dione derivatives as potential PET imaging agents for detection of beta-amyloid fibrils
- Authors
- Lee, Ji Hoon; Byeon, Seong Rim; Kim, YoungSoo; Lim, Soo Jeong; Oh, Seung Jun; Moon, Dae Hyuk; Yoo, Kyung Ho; Chung, Bong Young; Kim, Dong Jin
- Issue Date
- 15-10월-2008
- Publisher
- PERGAMON-ELSEVIER SCIENCE LTD
- Keywords
- Alzheimer' s disease; [F-18]-labeled; PET; imaging probe
- Citation
- BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, v.18, no.20, pp.5701 - 5704
- Indexed
- SCIE
SCOPUS
- Journal Title
- BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
- Volume
- 18
- Number
- 20
- Start Page
- 5701
- End Page
- 5704
- ISSN
- 0960-894X
- Abstract
- In this study a novel series of isoindol-1-one and isoindol-1,3-dione derivatives for beta-amyloid-specific binding agents is described. Twelve compounds were synthesized and evaluated via a competitive binding assay with [I-125]TZDM against beta-amyloid 1-42 (A beta 42) aggregates. Two new [F-18]-labeled isoindole derivatives were synthesized and evaluated as potential beta-amyloid imaging probes based on the in vivo pharmacokinetic profiles. The preliminary results suggest that these [F-18]18b and [F-18]18c are promising positron emission tomography (PET) imaging probes for studying accumulation of A beta fibrils in the brains of Alzheimer's disease (AD) patients. (C) 2008 Elsevier Ltd. All rights reserved.
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