1240348-54-2

Upstream product

• 21675-02-5 4-acetylaminophenacyl bromide 
• 99-81-0 4-Nitrophenacyl bromide 
• 1747-60-0 6-methoxybenzothiazol-2-ylamine 
• 1240348-29-1 2-(p-acetamidophenyl)-7-methoxyimidazo[2,1-b]benzothiazole 
• 1206722-58-8 2-(p-methylaminophenyl)-7-methoxyimidazo[2,1-b]benzothiazole 
• 1206722-59-9 4-(7-methoxyimidazo[2,1-b]benzothiazol-2-yl)benzenamine 
• 24247-22-1 7-methoxy-2-(4-nitrophenyl)benzo[d]imidazo[2,1-b]thiazole 

Downstream Products

• 1240348-23-5 2-(p-methylaminophenyl)-7-(2-fluoroethoxy)imidazo[2,1-b]benzothiazole 
• 1240348-38-2 2-(p-methylaminophenyl)-7-(2-tosyloxyethoxy)imidazo[2,1-b]benzothiazole 
• 1240348-39-3 [18F]2-(p-methylaminophenyl)-7-(2-fluoroethoxy)imidazo[2,1-b]benzothiazole 

Relevant academic research and scientific papers

Synthesis and evaluation of 11C-labeled imidazo[2,1-b] benzothiazoles (IBTs) as PET tracers for imaging β-amyloid plaques in Alzheimer's disease

We report a novel series of 11C-labeled imidazo[2,1-b] benzothiazoles (IBTs) as tracers for imaging of cerebral β-amyloid (Aβ) deposits in patients with Alzheimer's disease (AD) by means of positron emission tomography (PET). From a series of 11 compounds, candidates were identified to have a high binding affinity for Aβ. Selected compounds were prepared as O- or N-[11C]methyl derivatives and shown to have a high initial brain uptake in wild-type mice (range 1.9-9.2% I.D./g at 5 min). 2-(p-[11C]Methylaminophenyl)-7-methoxyimidazo[2,1-b] benzothiazole ([11C]5) was identified as a lead based on the combined favorable properties of high initial brain uptake, rapid clearance from normal brain, and high in vitro affinity for Aβ1-40 (Ki = 3.5 nM) and Aβ1-42 (5.8 nM), which were superior to the Pittsburgh compound B (1a). In an APP/PS1 mouse model of AD (Tg), we demonstrate a specific uptake of [11C]5 in Aβ-containing telencephalic brain regions by means of small-animal PET that was confirmed by regional brain biodistribution, ex vivo autoradiography, and immunohistochemistry. Analysis of brain sections of Tg mice receiving a single bolus injection of [11C]5 and [ 3H]1a together revealed that the tracers bind to Aβ plaques in the brain of Tg mice in a comparable pattern. Taken together, these data suggest that IBTs represent useful PET imaging agents for high-sensitivity detection of Aβ plaques.

A novel 18F-labeled imidazo[2,1- b ]benzothiazole (IBT) for high-contrast PET imaging of β-amyloid plaques

18F-labeled imidazo[2,1-b]benzothiazole ([18F]8) was synthesized and evaluated as a tracer for cerebral β-amyloid deposits (Aβ) by means of positron emission tomography (PET). [18F]8 exhibits a high affinity to Aβ and suit