期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 22, 期 17, 页码 5700-5703出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2012.06.086
关键词
Oxindole; Neurofibirillary tangles; Tau protein; Alzheimer's disease
资金
- Funding Program for Next Generation World-Leading Researchers
- JSPS
- Grants-in-Aid for Scientific Research [23390233] Funding Source: KAKEN
This letter describes the synthesis and biological evaluation of a novel series of radioiodinated oxindole (OI) derivatives for detecting neurofibrillary tangles (NFTs) in the brains of patients with Alzheimer's disease (AD). In binding experiments in vitro, 2-oxindole (2-OI) and 3-oxindole (3-OI) derivatives showed affinity for tau aggregates. The 3-OI derivative 14 showed the highest affinity of these derivatives. In biodistribution experiments using normal mice, the OI derivatives displayed good uptake (2.4-2.5% ID/g at 2 min) and clearance from the brain with time (0.6-1.4% ID/g at 30 min). In fluorescence staining experiments using AD brain sections, 14 clearly stained NFTs. 3-OI may serve as a new molecular scaffold for developing novel NFT imaging agents. (C) 2012 Elsevier Ltd. All rights reserved.
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