694473-93-3

Upstream product

• 825661-08-3 ethyl 4-[(1,1-dioxide-3-oxo-2H-benzo[d]isothiazol-2-yl)methyl]benzoate 
• 81-07-2 saccharin 
• 1612763-46-8 tert-butyl 4-[(1,1,3-trioxo-2,3-dihydro-1λ,2-benzothiazol-2-yl)methyl]benzoate 
• 108052-76-2 4-(bromomethyl)benzoic acid 1,1-dimethylethyl ester 
• 6232-88-8 4-bromomethylbenzoic Acid 

Downstream Products

• 1612763-47-9 4-[(1,1,3-Trioxo-2,3-dihydro-1λ⁶,2-benzothiazol-2-yl)methyl]benzoyl chloride 
• 1428073-16-8 4-[(1,1,3-trioxo-2,3-dihydro-1λ⁶,2-benzothiazol-2-yl)methyl]benzamide 
• 1612763-48-0 tert-butyl N-[(tert-butoxy)carbonyl]-N-{4-[(1,1,3-trioxo-2,3-dihydro-1λ⁶,2-benzothiazol-2-yl)methyl]benzoyl}carbamate 
• 1612763-49-1 N-methyl-4-[(1,1,3-trioxo-2,3-dihydro-1λ⁶,2-benzothiazol-2-yl)methyl]benzamide 
• 1612763-50-4 tert-butyl N-methyl-N-{4-[(1,1,3-trioxo-2,3-dihydro-1λ⁶,2-benzothiazol-2-yl)methyl]benzoyl}carbamate 
• 1612763-51-5 N-[2-(Furan-2-yl)ethyl]-4-[(1,1,3-trioxo-2,3-dihydro-1λ⁶,2-benzothiazol-2-yl)methyl]benzamide 
• 1612763-52-6 tert-Butyl N-[2-(furan-2-yl)ethyl]-N-{4-[(1,1,3-trioxo-2,3-dihydro-1λ⁶,2-benzothiazol-2-yl)methyl]benzoyl}carbamate 
• 1612763-53-7 N-(furan-2-ylmethyl)-N-methyl-4-[(1,1,3-trioxo-2,3-dihydro-1λ⁶,2-benzothiazol-2-yl)methyl]benzamide 
• 1612763-54-8 tert-Butyl N-{4-[(1,1,3-trioxo-2,3-dihydro-1λ⁶,2-benzothiazol-2-yl)methyl]benzoyl}carbamate 
• 1612763-55-9 methyl N-(furan-2-ylmethyl)-N-{4-[(1,1,3-trioxo-2,3-dihydro-1λ⁶,2-benzothiazol-2-yl)methyl]benzoyl}carbamate 
• 1612763-56-0 N-acetyl-N-(furan-2-ylmethyl)-4-[(1,1,3-trioxo-2,3-dihydro-1λ⁶,2-benzothiazol-2-yl)methyl]benzamide 
• 1001349-42-3 4-((1,1-dioxido-3-oxobenzo[d]isothiazol-2(3H)-yl)methyl)-N-hydroxylbenzamide 

Relevant academic research and scientific papers

Design, synthesis and biological evaluation of saccharin-based N-hydroxybenzamides as histone deacetylases (HDACs) inhibitors

We report the development of a novel series of saccharin-based N-hydroxybenzamides as histone deacetylases inhibitors. Among them, 6j exhibited potent HDACs inhibitory activity against Hela nuclear extract. Further biological evaluation found 6i showed similar antiproliferative activities in vitro compared with the approved SAHA.

Saccharin derivatives as inhibitors of interferon-mediated inflammation

A series of novel, saccharin-based antagonists have been identified for the interferon signaling pathway. Through in vitro high-throughput screening with the Colorado Center for Drug Discovery (C2D2) Pilot Library, we identified hit compound 1, which was the basis for extensive structure-activity relationship studies. Our efforts produced a lead anti-inflammatory compound, tert-butyl N-(furan-2-ylmethyl)-N-{4-[(1,1,3-trioxo-2,3-dihydro-1λ6,2- benzothiazol-2-yl)methyl]benzoyl}carbamate CU-CPD103 (103), as a potent inhibitor using an established nitric oxide (NO) signaling assay. With further studies of its inhibitory mechanisms, we demonstrated that 103 carries out this inhibition through the JAK/STAT1 pathway, providing a drug-like small molecule inflammation suppressant for possible therapeutic uses.

DERIVATIVES OF BENZO[D] ISOTHIAZOLES AS HISTONE DEACETYLASE INHIBITORS

The invention relates to derivatives of benzo[d]isothiazoles as histone deacetylase inhibitors, selected from among compounds of general formula (Ia) and (Ib) or one of the salts thereof, particularly one of the pharmaceutically acceptable salts thereof,