24247-22-1Relevant articles and documents
Benzo imidazo [2, 1-b] thiazole compound and application thereof (by machine translation)
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Paragraph 0069-0071, (2020/07/15)
The invention discloses a benzoimidazo [2, 1-b] thiazole compound and application thereof, and belongs to the technical field of medicines. The inhibitory activity of the synthesized benzimidazo [2, 1-b] thiazole analogues on FLTT3 is more than 90%, wherein the compounds (compounds 2 , 4, 6, 8 and 10) are IC of FLTT3-ITD kinase. 50 Lower value, in particular compound 2, IC IC50 The value is only 5.60 nm, and therefore the compound of the present invention may be used as an inhibitor FLTT3, or for preparing a drug capable of modulating or suppressing diseases associated with abnormal cell proliferation by affecting the enzymatic activity of one or more tyrosine kinases and interfering with aberrant cell proliferation, having a wide application prospect. (by machine translation)
Synthesis and evaluation of 11C-labeled imidazo[2,1-b] benzothiazoles (IBTs) as PET tracers for imaging β-amyloid plaques in Alzheimer's disease
Yousefi, Behrooz H.,Manook, André,Drzezga, Alexander,Reutern, Boris V.,Schwaiger, Markus,Wester, Hans-Jürgen,Henriksen, Gjermund
experimental part, p. 949 - 956 (2011/04/24)
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.