24247-22-1

Upstream product

• 38956-24-0 2-(2-imino-6-methoxy-benzothiazol-3-yl)-1-(4-nitro-phenyl)-ethanone 
• 1747-60-0 6-methoxybenzothiazol-2-ylamine 
• 99-81-0 4-Nitrophenacyl bromide 

Downstream Products

• 1240348-54-2 2-(p-methylaminophenyl)-7-hydroxyimidazo[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 
• 1132827-30-5 4-(7-hydroxyimidazo[2,1-b]benzothiazol-2-yl)benzenamine 

Relevant academic research and scientific papers

Benzo imidazo [2, 1-b] thiazole compound and application thereof (by machine translation)

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 biological evaluation of diaryl urea derivatives as FLT3 inhibitors

As a class III receptor tyrosine kinase (RTK), FMS-like tyrosine kinase 3 (FLT3) is always overexpressed in many cases of acute leukemia. This paper studies the structure-based synthesis and biological evaluation of diaryl urea derivatives as FLT3 inhibitors. Encouragingly, compounds 15b, 16b, 24a, and 24c showed excellent biological activities in a low nanomolar range. In particular, compound 16b demonstrated significant inhibitory potency against FLT3-ITD (IC50 = 5.60 nM) and better antiproliferative activity than quizartinib against MV4-11 cell line (IC50 = 0.176 nM). It is indicated that compound 16b for the treatment of acute myeloid leukemia could be very promising.

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.

2-Arylimidazo[2,1-b]benzothiazoles: A new family of amyloid binding agents with potential for PET and SPECT imaging of Alzheimer's brain

We designed and synthesized a small series of 2-aryl-imidazo[2,1-b] benzothiazole, representing a combination of motifs from the two most potent amyloid imaging agents, PIB and IMPY. The binding affinity of the new compounds ranged from 6 to 133 nM. Among the best compounds, 3b (Ki = 6 nM) can be labeled with 11CH3 for PET imaging whereas 3j (K i = 10.9 nM) can be labeled with 123I for SPECT imaging.