1396341-18-6Relevant articles and documents
Synthesis and biological evaluation of novel oxindole derivatives for imaging neurofibrillary tangles in Alzheimer's disease
Watanabe, Hiroyuki,Ono, Masahiro,Kimura, Hiroyuki,Matsumura, Kenji,Yoshimura, Masashi,Okamoto, Yoko,Ihara, Masafumi,Takahashi, Ryosuke,Saji, Hideo
supporting information; experimental part, p. 5700 - 5703 (2012/10/07)
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.