532422-39-2

Upstream product

• 2393-23-9 4-methoxy-benzylamine 
• 7442-07-1 6-aminobenzo[d]thiazole-2(3H)-thione 
• 144581-86-2 α-Bromo-N-p-methoxybenzylacetamide 
• 4845-58-3 6-nitrobenzo[d]thiazole-2(3H)-thione 
• 149-30-4 2-thioxo-3H-1,3-benzothiazole 
• 137-07-5 2-amino-benzenethiol 
• 7442-07-1 6-amino-2-mercaptobenzothiazole 
• 81494-05-5 2-chloro-N-(4-methoxybenzyl)acetamide 

Downstream Products

• 530150-55-1 N-(2-(2-(4-methoxybenzylamino)-2-oxoethylthio)benzothiazol-6-yl)benzamide 
• 532421-08-2 4-chloro-N-(2-(2-(4-methoxybenzylamino)-2-oxoethylthio)benzothiazol-6-yl)benzamide 
• 531530-49-1 N-(2-(2-(4-methoxybenzylamino)-2-oxoethylthio)benzothiazol-6-yl)-4-nitrobenzamide 
• 532415-23-9 2-(6-acetamidobenzothiazol-2-ylthio)-N-(4-methoxybenzyl)acetamide 
• 1258323-56-6 2-methoxy-N-(2-(2-(4-methoxybenzylamino)-2-oxoethylthio)benzothiazol-6-yl)benzamide 

Relevant academic research and scientific papers

Synthesis and invitro Evaluation of West Nile Virus Protease Inhibitors Based on the 2-{6-[2-(5-Phenyl-4H-{1,2,4]triazol-3-ylsulfanyl)acetylamino]benzothiazol-2-ylsulfanyl}acetamide Scaffold

In recent years, clinical symptoms resulting from West Nile virus (WNV) infection have worsened in severity, with an increased frequency in neuroinvasive diseases among the elderly. As there are presently no successful therapies against WNV for use in humans, continual efforts to develop new chemotherapeutics against this virus are highly desired. The viral NS2B-NS3 protease is a promising target for viral inhibition due to its importance in viral replication and its unique substrate preference. In this study, a WNV NS2B-NS3 protease inhibitor with a 2-{6-[2-(5-phenyl-4H-[1,2,4]triazol-3-ylsulfanyl)acetylamino]benzothiazol-2-ylsulfanyl}acetamide scaffold was identified during screening. Optimization of this initial hit by synthesis and screening of a focused compound library with this scaffold led to the identification of a novel uncompetitive inhibitor (1a24, IC50=3.4±0.2μM) of the WNV NS2B-NS3 protease. Molecular docking of 1a24 into the WNV protease showed that the compound interferes with productive interactions of the NS2B cofactor with the NS3 protease and is an allosteric inhibitor of the WNV NS3 protease.

Synthesis, structure-activity relationships and preliminary antitumor evaluation of benzothiazole-2-thiol derivatives as novel apoptosis inducers

A series of novel benzothiazole-2-thiol derivatives were synthesized, and their anti-proliferative activities on HepG2 and MCF-7 cells were investigated. Most compounds had inhibitory effects on cell growth, and some of them were more effective than cisplatin. Compounds 6m and 6t displayed good inhibitory activities against a panel of different types of human cancer cell lines, with IC50 values in the low micromolar range. Further biological evaluation indicated that 6m induced apoptosis in HepG2 cancer cells. Structure-activity relationships were also proposed.