1365036-73-2

Basic information

• Product Name: N-(2-(4-(1,2-benzothiazol-3-yl)piperazin-1-yl)ethyl)-3-methylbenzenesulphonamide
• Synonyms: N-(2-(4-(1,2-benzothiazol-3-yl)piperazin-1-yl)ethyl)-3-methylbenzenesulphonamide
• CAS NO: 1365036-73-2
• Molecular Weight: 416.568
• Mol File: 1365036-73-2.mol
• Article Data: 3

Chemical Properties

• CAS DataBase Reference: N-(2-(4-(1,2-benzothiazol-3-yl)piperazin-1-yl)ethyl)-3-methylbenzenesulphonamide(CAS DataBase Reference)
• NIST Chemistry Reference: N-(2-(4-(1,2-benzothiazol-3-yl)piperazin-1-yl)ethyl)-3-methylbenzenesulphonamide(1365036-73-2)
• EPA Substance Registry System: N-(2-(4-(1,2-benzothiazol-3-yl)piperazin-1-yl)ethyl)-3-methylbenzenesulphonamide(1365036-73-2)

Safety Data

• Hazardous Substances Data: 1365036-73-2(Hazardous Substances Data)

Upstream product

• 1899-93-0 3-methylphenylsulfonyl chloride 
• 676115-71-2 2-[4-(1,2-benzothiazol-3-yl)piperazin-1-yl]ethan-1-amine 
• 87691-87-0 3-(1-piperazinyl)-1,2-benzisothiazole 

Relevant articles and documents

Novel arylsulfonamide derivatives with 5-HT6/5-HT7 receptor antagonism targeting behavioral and psychological symptoms of dementia

In order to target behavioral and psychological symptoms of dementia (BPSD), we used molecular modeling-assisted design to obtain novel multifunctional arylsulfonamide derivatives that potently antagonize 5-HT 6/7/2A and D2 receptors, without interacting with M 1 receptors and hERG channels. In vitro studies confirmed their antagonism of 5-HT7/2A and D2 receptors and weak interactions with key antitargets (M1R and hERG) associated with side effects. Marked 5-HT6 receptor affinities were also observed, notably for 6-fluoro-3-(piperidin-4-yl)-1,2-benzoxazole derivatives connected by a 3-4 unit alkyl linker with mono- or bicyclic, lipophilic arylsulfonamide moieties. N-[4-[4-(6-Fluoro-1,2-benzoxazol-3-yl)piperidin-1-yl]butyl] benzothiophene-2-sulfonamide (72) was characterized in vitro on 14 targets and antitargets. It displayed dual blockade of 5-HT6 and D2 receptors and negligible interactions at hERG and M1 receptors. Unlike reference antipsychotics, 72 displayed marked antipsychotic and antidepressant activity in rats after oral administration, in the absence of cognitive or motor impairment. This profile is particularly attractive when targeting a fragile, elderly BPSD patient population.

ARYLOSULFONAMIDES FOR THE TREATMENT OF CNS DISEASES

Arylsulphonamide derivatives of formula (I) and pharmaceutically acceptable salts thereof. The compounds may be useful for the treatment and/or prevention of disorders of the central nervous system.