Synthesis and characterization of novel phenylindoles as potential probes for imaging of β-amyloid plaques in the brain

H Watanabe, M Ono, M Haratake, N Kobashi…

文献索引：Watanabe, Hiroyuki; Ono, Masahiro; Haratake, Mamoru; Kobashi, Nobuya; Saji, Hideo; Nakayama, Morio Bioorganic and Medicinal Chemistry, 2010 , vol. 18, # 13 p. 4740 - 4746

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被引用次数: 19

摘要

We synthesized a novel series of phenylindole (PI) derivatives and evaluated their biological activities as probes for imaging Aβ plaques in vivo. The affinity for Aβ plaques was assessed by an in vitro-binding assay using pre-formed synthetic Aβ aggregates. 2-Phenyl-1H-indole (2-PI) derivatives showed high affinity for Aβ42 aggregates with Ki values ranging from 4 to 32nM. 2-PI derivatives clearly stained Aβ plaques in an animal model of AD. In ...