Push-pull benzothiazole derivatives as probes for detecting beta-amyloid plaques in Alzheimer's brains
- Bioorg Med Chem. 2009 Oct 1;17(19):7002-7. doi: 10.1016/j.bmc.2009.08.032.
- 1. Graduate School of Pharmaceutical Sciences, Kyoto University, 46-29 Yoshida Shimoadachi-cho, Sakyo-ku, Kyoto 606-8501, Japan. [email protected]
We synthesized push-pull benzothiazole derivatives and evaluated their potential as beta-amyloid imaging probes. In binding experiments in vitro, the benzothiazoles showed excellent affinity for synthetic Abeta(1-42) aggregates. beta-Amyloid plaques in the mouse and human brain were clearly visualized with the benzothiazoles, reflecting the results in vitro. These compounds may be a useful scaffold for the development of novel PET/SPECT and fluorescent tracers for detecting beta-amyloid in Alzheimer's brains.
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