34551-19-4

Usage

Uses

6-Chloro-N-methyl-2-benzothiazolamine is used as an antituberculous agent.

Upstream product

• 95-24-9 6-chloro-2-aminobenzothiazole 
• 77-78-1 dimethyl sulfate 
• 2740-97-8 1-(4-chloro-phenyl)-3-methyl-thiourea 
• 34551-27-4 (4-chloro-phenyl)-(4-methyl-4H-[1,2,3,4]thiatriazol-5-ylidene)-amine 
• 7726-95-6 bromine 
• 13078-27-8 (4-chloro-phenyl)-[1,2,3,4]thiatriazol-5-yl-amine 
• 2131-55-7 4-Chlorophenyl isothiocyanate 
• 67-56-1 methanol 
• 106-47-8 4-chloro-aniline 
• 3622-23-9 2,6-dichloro-1,3-benzothiazole 
• 74-89-5 methylamine 

Relevant academic research and scientific papers

Synthesis, Type II diabetes inhibitory activity, antimicrobial evaluation and docking studies of indeno[1,2-c]pyrazol-4(1H)-ones

We report a convenient and efficient synthesis of indeno[1,2-c]pyrazol-4(1H)-ones (4a?o) by the reaction of a variety of 2-acyl-(1H)-indene-1,3(2H)-diones (1) and 2-hydrazinylbenzo[d]thiazole/2-hydrazinyl-6-substitutedbenzo[d]thiazoles (2) in the presence of glacial acetic acid in good yields. The structure of the compounds thus prepared were confirmed by analytical and spectral (FT-IR, 1H NMR, 13C NMR, and HRMS) techniques. All the synthesized indeno[1,2-c]pyrazol-4(1H)-ones (4a?o) were assayed for their in vitro Type II diabetes inhibitory activity by using Acarbose as standard drug and in vitro antimicrobial activity utilizing Streptomycin and Fluconazole as reference drugs. Among the synthesized derivatives, 4e (IC50 = 6.71 μg/mL) was found to be more potent against α-glucosidase enzyme as compared with the standard Acarbose (IC50 = 9.35 μg/mL) and 4i (IC50 = 11.90 μg/mL) exhibited good inhibitory activity against α-amylase enzyme as compared with the standard Acarbose (IC50 = 22.87 μg/mL). Also, all the titled compounds showed good antimicrobial activity. In addition, in vitro α-glucosidase and α-amylase inhibition were supported by docking studies performed on the derivatives 4e and 4o, respectively. [Figure not available: see fulltext.].

Chagas Disease Drug Discovery: Multiparametric Lead Optimization against Trypanosoma cruzi in Acylaminobenzothiazole Series

Acylaminobenzothiazole hits were identified as potential inhibitors of Trypanosoma cruzi replication, a parasite responsible for Chagas disease. We selected compound 1 for lead optimization, aiming to improve in parallel its anti-T. cruzi activity (IC50 = 0.63 μM) and its human metabolic stability (human clearance = 9.57 mL/min/g). A total of 39 analogues of 1 were synthesized and tested in vitro. We established a multiparametric structure-activity relationship, allowing optimization of antiparasite activity, physicochemical parameters, and ADME properties. We identified compound 50 as an advanced lead with an improved anti-T. cruzi activity in vitro (IC50 = 0.079 μM) and an enhanced metabolic stability (human clearance = 0.41 mL/min/g) and opportunity for the oral route of administration. After tolerability assessment, 50 demonstrated a promising in vivo efficacy.

THERAPEUTIC COMPOUNDS AND COMPOSITIONS

Compounds of general formula (I) and compositions comprising compounds of general formula I that modulate pyruvate kinase are described herein. Also described herein are methods of using the compounds that modulate pyruvate kinase in the treatment of diseases.

THERAPEUTIC COMPOUNDS AND COMPOSITIONS

Compounds of general formula I: and compositions comprising compounds of general formula I that modulate pyruvate kinase are described herein. Also described herein are methods of using the compounds that modulate pyruvate kinase in the treatment of diseases.

THERAPEUTIC COMPOUNDS AND COMPOSITIONS

Compounds of general formula (I) and compositions comprising compounds of general formula (I) that modulate pyruvate kinase are described herein. Also described herein are methods of using the compounds that modulate pyruvate kinase in the treatment of diseases.

General and efficient method for direct N-monomethylation of aromatic primary amines with methanol

The direct N-monomethylation of aromatic primary amines, including arylamines, arylsulfonamides and amino-azoles, using methanol as a methylating agent has been accomplished in the presence of a [CpIrCl2]2/NaOH system. From both synthetic and environmental points of view, the reaction is highly attractive because of low catalyst loading, broad substrate scope and excellent selectivities.

A facile synthesis of 2-N(methyl amino) benzothiazoles

Reaction of aromatic primary amines with methylisothiocyanate (MITC) yielded N-methyl-N1-(benzelene-1-yl)thioureas which underwent oxidative cyclization in the presence of bromine in acetic acid, at room temperature, affording the title compounds.