1215012-74-0

Basic information

• Product Name: 2,6-dichloro-N-(difluoromethyl)-4-(3-(1-methylpiperidin-4-yl)propyl)-N-(1,3,5-trimethyl-1H-pyrazol-4-yl)benzenesulfonamide
• Synonyms: 2,6-dichloro-N-(difluoromethyl)-4-(3-(1-methylpiperidin-4-yl)propyl)-N-(1,3,5-trimethyl-1H-pyrazol-4-yl)benzenesulfonamide
• CAS NO: 1215012-74-0
• Molecular Weight: 523.475
• Mol File: 1215012-74-0.mol

Chemical Properties

• CAS DataBase Reference: 2,6-dichloro-N-(difluoromethyl)-4-(3-(1-methylpiperidin-4-yl)propyl)-N-(1,3,5-trimethyl-1H-pyrazol-4-yl)benzenesulfonamide(CAS DataBase Reference)
• NIST Chemistry Reference: 2,6-dichloro-N-(difluoromethyl)-4-(3-(1-methylpiperidin-4-yl)propyl)-N-(1,3,5-trimethyl-1H-pyrazol-4-yl)benzenesulfonamide(1215012-74-0)
• EPA Substance Registry System: 2,6-dichloro-N-(difluoromethyl)-4-(3-(1-methylpiperidin-4-yl)propyl)-N-(1,3,5-trimethyl-1H-pyrazol-4-yl)benzenesulfonamide(1215012-74-0)

Safety Data

• Hazardous Substances Data: 1215012-74-0(Hazardous Substances Data)

Usage

Uses

Used in Pharmaceutical Industry:
2,6-dichloro-N-(difluoromethyl)-4-(3-(1-methylpiperidin-4-yl)propyl)-N-(1,3,5-trimethyl-1H-pyrazol-4-yl)benzenesulfonamide is used as a potential pharmaceutical agent for its possible biological activity, attributed to the presence of functional groups commonly found in drug molecules. The sulfonamide and pyrazolyl groups may contribute to its interaction with specific biological targets, while the difluoromethyl group could enable selective binding to fluorine-sensitive proteins or enzymes, making it a candidate for the development of new therapeutic agents.
Used in Biochemical Research:
In the field of biochemical research, 2,6-dichloro-N-(difluoromethyl)-4-(3-(1-methylpiperidin-4-yl)propyl)-N-(1,3,5-trimethyl-1H-pyrazol-4-yl)benzenesulfonamide serves as a valuable compound for studying the effects of structural modifications on biological activity. Its unique combination of functional groups allows researchers to investigate the role of each group in modulating interactions with biological targets, potentially leading to insights into the design of more effective drugs.

Upstream product

• 206446-47-1 4-(prop-2-en-1-yl)-1-t-butoxycarbonylpiperidine 
• 5261-66-5 4-allyl-1-methylpiperidine 
• 1215013-18-5 4-bromo-2,6-dichloro-N-(difluoromethyl)-N-(1,3,5-trimethyl-1H-pyrazol-4-yl)benzenesulfonamide 
• 28466-21-9 1,3,5-trimethyl-1H-pyrazol-4-amine 
• 351003-54-8 4-bromo-2,6-dichlorobenzenesulfonyl chloride 
• 1215009-29-2 4-bromo-2,6-dichloro-N-(1,3,5-trimethyl-1H-pyrazol-4-yl)-benzenesulfonamide 

Relevant articles and documents

Lead optimization of a pyrazole sulfonamide series of trypanosoma brucei N -myristoyltransferase inhibitors: Identification and evaluation of CNS penetrant compounds as potential treatments for stage 2 human african trypanosomiasis

Trypanosoma brucei N-myristoyltransferase (TbNMT) is an attractive therapeutic target for the treatment of human African trypanosomiasis (HAT). From previous studies, we identified pyrazole sulfonamide, DDD85646 (1), a potent inhibitor of TbNMT. Although this compound represents an excellent lead, poor central nervous system (CNS) exposure restricts its use to the hemolymphatic form (stage 1) of the disease. With a clear clinical need for new drug treatments for HAT that address both the hemolymphatic and CNS stages of the disease, a chemistry campaign was initiated to address the shortfalls of this series. This paper describes modifications to the pyrazole sulfonamides which markedly improved blood-brain barrier permeability, achieved by reducing polar surface area and capping the sulfonamide. Moreover, replacing the core aromatic with a flexible linker significantly improved selectivity. This led to the discovery of DDD100097 (40) which demonstrated partial efficacy in a stage 2 (CNS) mouse model of HAT.

N-Myristoyl Transferase Inhibitors

The present invention relates to N-heterocyclic sulphonamide compounds, in particular pyrazole sulphonamide compounds, and their use as N-myristoyl transferase inhibitors.