909904-76-3

Upstream product

• 122-04-3 4-nitro-benzoyl chloride 
• 875846-26-7 2-(4-nitrophenyl)benzothiazole-6-carbonyl chloride 
• 65644-51-1 2-(4-nitrophenyl)-1,3-benzothiazole-6-carboxylic acid 
• 909904-75-2 C₂₀H₁₁N₃O₂S₂ 

Downstream Products

• 909904-80-9 C₂₀⁽¹¹⁾CH₁₅N₃S₂ 

Relevant academic research and scientific papers

AMYLOID-IMAGING AGENTS

A molecular probe for use in the detection of amyloid in a subject includes a dibenzothiazole derivative.

Dibenzothiazoles as novel amyloid-imaging agents

Novel dibenzothiazole derivatives were synthesized and evaluated as amyloid-imaging agents. In vitro quantitative binding studies using AD brain tissue homogenates showed that the dibenzothiazole derivatives displayed high binding affinities with Ki values in the nanomolar range (6.8-36 nM). These derivatives are relatively lipophilic with partition coefficients (logP oct) in the range of 1.25-3.05. Preliminary structure-activity relationship studies indicated dibenzothiazole derivatives bearing electron-donating groups exhibited higher binding affinities than those bearing electron-withdrawing groups. A lead compound was selected for its high binding affinity and radiolabeled with [125I] through direct radioiodination using sodium [125I] iodide in the presence of Chloramine T. The radioligand (4-[2,6′]dibenzothiazolyl-2′-yl-2-[125I]-phenylamine) displayed moderate lipophilicity (logP oct, 2.70), very good brain uptake (3.71 ± 0.63% ID/g at 2 min after iv injection in mice), and rapid washout from normal brains (0.78% and 0.43% ID/g at 30 and 60 min, respectively). These studies indicated that lipophilic dibenzothiazole derivatives represent a promising pharmacophore for the development of novel amyloid-imaging agents for potential application in Alzheimer's disease and related neurodegenerative disorders.