14678-99-0

Upstream product

• 15001-11-3 ethyl 5-amino-1-(p-tolyl)-1H-pyrazole-4-carboxylate 
• 539-44-6 N-4-methylphenylhydrazine 
• 1820-80-0 3-aminopyrazole 
• 624-31-7 4-tolyl iodide 

Downstream Products

• 1003597-19-0 7-chloro-4-[(3-methyl-1-methylphenyl-1H-pyrazol-5-yl)amino]quinoline 
• 15001-22-6 4-acetylamino-N-(2-p-tolyl-2H-pyrazol-3-yl)-benzenesulfonamide 
• 1443247-33-3 1-[(1S,4R)-4-(3-isopropyl-[1,2,4]triazolo[4,3-a]pyridin-6-yloxy)-1,2,3,4-tetrahydro-naphthalen-1-yl]-3-(2-p-tolyl-2H-pyrazol-3-yl)-urea 
• 1443248-32-5 (2-p-tolyl-2H-pyrazol-3-yl)-carbamic acid 2,2,2-trichloro-ethyl ester 

Relevant academic research and scientific papers

The optimization and characterization of functionalized sulfonamides derived from sulfaphenazole against Mycobacterium tuberculosis with reduced CYP 2C9 inhibition

In this study, a series of sulfonamide compounds was designed and synthesized through the systematic optimization of the antibacterial agent sulfaphenazole for the treatment of Mycobacterium tuberculosis (M. tuberculosis). Preliminary results indicate that the 4-aminobenzenesulfonamide moiety plays a key role in maintaining antimycobacterial activity. Compounds 10c, 10d, 10f and 10i through the optimization on phenyl ring at the R2 site on the pyrazole displayed promising antimycobacterial activity paired with low cytotoxicity. In particular, compound 10d displayed good activity (MIC = 5.69 μg/mL) with low inhibition of CYP 2C9 (IC50 > 10 μM), consequently low potential risk of drug-drug interaction. These promising results provide new insight into the combination regimen using sulfonamide as one component for the treatment of M. tuberculosis.

Copper(I)/Copper(II)-Assisted Tandem Catalysis: The Case Study of Ullmann/Chan-Evans-Lam N1,N3-Diarylation of 3-Aminopyrazole

Unprecedented CuI/CuII-assisted tandem catalysis allowing an Ullmann/Chan-Evans-Lam sequence was achieved. This three-component, one-pot reaction triggered by a change in the oxidation state of the metal leads to the selective N1,N3-diarylation of 3-aminopyrazole. This new method should be a valuable tool for small-molecule drug discovery that requires suitable regio- and/or chemoselective strategies for the N-arylation of nitrogen-containing heterocycles. Tandem power: The first assisted tandem copper-catalyzed process, triggered by a change in the oxidation state of the metal, is developed to allow a one-pot Ullman/Chan-Evans-Lam sequence leading to the selective N1,N3-diarylation of 3-aminopyrazole.

TETRAZOLE COMPOUNDS AS OREXIN RECEPTOR ANTAGONISTS

The invention relates to tetrazole compounds of formula (I) wherein X, Y, Z, R1, R2 and R3 are as described in the description; to pharmaceutically acceptable salts thereof, and to the use of such compounds use as medicaments, especially as orexin receptor antagonists.

TETRAZOLE COMPOUNDS AS OREXIN RECEPTOR ANTAGONISTS

The invention relates to tetrazole compounds of formula (I) wherein X, Y, Z, R1, R2 and R3 are as described in the description; to pharmaceutically acceptable salts thereof, and to the use of such compounds use as medicaments, especially as orexin receptor antagonists.