(18)F]-labeled isoindol-1-one and isoindol-1,3-dione derivatives as potential PET imaging agents for detection of beta-amyloid fibrils |
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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 |
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Affiliation: | Center for Chemoinformatics Research, Korea Institute of Science and Technology, PO Box 131, Cheongryang, Seoul 130-650, South Korea. |
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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 [(125)I]TZDM against beta-amyloid 1-42 (Abeta42) aggregates. Two new [(18)F]-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 [(18)F]18b and [(18)F]18c are promising positron emission tomography (PET) imaging probes for studying accumulation of Abeta fibrils in the brains of Alzheimer's disease (AD) patients. |
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