18330-64-8

Usage

InChI:InChI=1/C8H6N2O2S/c9-4-13-7-3-5(8(11)12)1-2-6(7)10/h1-3H,10H2,(H,11,12)

Upstream product

• 540-72-7 sodium thiocyanide 
• 150-13-0 4-amino-benzoic acid 
• 333-20-0 potassium thioacyanate 
• 1147550-11-5 ammonium thiocyanate 

Downstream Products

• 1370024-75-1 2-(2-chlorophenyl)-3-(4-methylphenyl)-2,3-dihydroimidazo[2,1-b][1,3]benzothiazole-7-carboxylic acid 
• 1370409-59-8 2-(2-chlorophenyl)-3-(4-methoxyphenyl)-2,3-dihydroimidazo[2,1-b][1,3]benzothiazole-7-carboxylic acid 
• 1370025-25-4 2-(2-chlorophenyl)-3-[4-(methylsulfanyl) phenyl]-2,3-dihydroimidazo[2,1-b][1,3]benzothiazole-7-carboxylic acid 
• 1370024-54-6 2-(4-methoxyphenyl)-3-(4-methylphenyl)imidazo[2,1-b][1,3]benzothiazole-7-carboxylic acid 
• 1280582-32-2 2,3-bis(4-methoxyphenyl)imidazo[2,1-b][1,3]benzothiazole-7-carboxylic acid 
• 1370409-52-1 2-(4-methoxyphenyl)-3-[4-(methylsulfanyl) phenyl]imidazo[2,1-b][1,3]benzothiazole-7-carboxylic acid 
• 1370024-36-4 2-(2,4-dichlorophenyl)-3-(4-methylphenyl)imidazo[2,1-b][1,3]benzothiazole-7-carboxylic acid 
• 1370409-53-2 2-(2,4-dichlorophenyl)-3-(4-methoxyphenyl)imidazo[2,1-b][1,3]benzothiazole-7-carboxylic acid 
• 1370023-99-6 2-(2,4-dichlorophenyl)-3-[4-(methylsulfanyl)phenyl]imidazo[2,1-b][1,3]benzothiazole-7-carboxylic acid 
• 93-85-6 2-aminobenzothiazole-6-carboxylic acid 
• 6285-57-0 2-amino-6-nitrobenzothiazole 
• 1370409-55-4 2-(4-methoxyphenyl)-3-[4-(methylsulfanyl)phenyl]-7-nitroimidazo[2,1b][1,3] benzothiazole 
• 1370409-54-3 2-(2,4-dichlorophenyl)-3-(4-methylphenyl)-7-nitroimidazo[2,1-b][1,3]benzothiazole 
• 1240167-82-1 2,3-bis(4-methoxyphenyl)-7-nitroimidazo[2,1-b][1,3]benzothiazole 

Relevant academic research and scientific papers

Synthesis and preliminary in-vitro cytotoxic activity of novel substituted diaryl-imidazo [2, 1, b]-benzothiazole derivatives

A novel series of substituted diaryl imidazo[2, 1-b]benzothiazole derivatives (8a-y) were synthesized by condensation reaction between 2-amino benzothiazole derivatives (3a-g) and substituted a-bromo-1, 2-(substituted) diaryl-1-ethanones (7a-i). The structures of the synthesized compounds were established by IR, 1H NMR, 13C NMR and mass spectroscopical data. The compounds (8a-y) were evaluated for their in-vitro cytotoxic activity on murine (B16F10) and human (MCF-7) cancer cells by using MTT assay. From the in vitro studies compounds 8p, 8u and 8y were found most effective with an IC50 range of 0.56-27.50 μM in MCF-7 and 2.57-36.54 μM in B16F10 cells.

Synthesis and preliminary in-vitro cytotoxic activity of novel substituted diaryl-imidazo [2,1,b]-benzothiazole derivatives

A novel series of substituted diaryl imidazo[2,1-b]benzothiazole derivatives (8a-y) were synthesized by condensation reaction between 2-amino benzothiazole derivatives (3a-g) and substituted α-bromo-1, 2-(substituted) diaryl-1-ethanones (7a-i). The structures of the synthesized compounds were established by IR, 1H NMR, 13C NMR and mass spectroscopical data. The compounds (8a-y) were evaluated for their in-vitro cytotoxic activity on murine (B16F10) and human (MCF-7) cancer cells by using MTT assay. From the in vitro studies compounds 8p, 8u and 8y were found most effective with an IC50 range of 0.56-27.50 μM in MCF-7 and 2.57-36.54 μM in B16F10 cells.

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.

COMPOUND INHIBITING DIPEPTIDYL PEPTIDASE IV

The invention aims to provide a dipeptidyl peptidase IV inhibitor which is satisfactory in respect of activity, stability and safety and has an excellent action as a pharmaceutical agent. The invention is directed to a compound represented by the following general formula or a pharmaceutically acceptable salt thereof: wherein R1 and R2 each represents hydrogen, an optionally substituted C1-6 alkyl group, or -COOR5 whereupon R5 represents hydrogen or an optionally substituted C1-6 alkyl group, or R1 and R2, together with a carbon atom to which they are bound, represent a 3- to 6-membered cycloalkyl group, R3 represents hydrogen or an optionally substituted C6-10 aryl group, R4 represents a hydrogen or a cyano group, D represents -CONR6-, -CO- or -NR6CO-, R6 represents hydrogen or an optionally substituted C1-6 alkyl group, E represents -(CH2)m- whereupon m is an integer of 1 to 3, -CH2OCH2-, or -SCH2-, n is an integer of 0 to 3, and A represents an optionally substituted bicyclic heterocyclic group or bicyclic hydrocarbon group.