期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 18, 期 20, 页码 5701-5704出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2008.05.019
关键词
Alzheimer's disease; [F-18]-labeled; PET; imaging probe
资金
- Ministry of Science and Technology (MOST)
- Ministry of Commerce, Industry and Energy (MCIE) of Korea
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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