405262-60-4

Basic information

• Product Name: Ethenesulfonamide, 2-(2,6-dimethylphenyl)-, (1E)-
• CAS NO: 405262-60-4
• Molecular Formula: C10H13NO2S
• Molecular Weight: 211.285
• Mol File: 405262-60-4.mol
• Article Data: 1

Chemical Properties

• CAS DataBase Reference: Ethenesulfonamide, 2-(2,6-dimethylphenyl)-, (1E)-(CAS DataBase Reference)
• NIST Chemistry Reference: Ethenesulfonamide, 2-(2,6-dimethylphenyl)-, (1E)-(405262-60-4)
• EPA Substance Registry System: Ethenesulfonamide, 2-(2,6-dimethylphenyl)-, (1E)-(405262-60-4)

Safety Data

• Hazardous Substances Data: 405262-60-4(Hazardous Substances Data)

Upstream product

• 2386-58-5 vinyl sulfonamide 
• 576-22-7 2-Bromo-m-xylene 

Relevant articles and documents

Synthesis and structure-activity relationships in a series of ethenesulfonamide derivatives, a novel class of endothelin receptor antagonists

In the previous paper, we described a series of the 2-arylethenesulfonamide derivatives, a novel class of ETA-selective endothelin (ET) receptor antagonists, including the compounds 1a, b. Compound 1a showed excellent oral antagonistic activities and pharmacokinetic profiles, and the monopotassium salt of 1 (YM-598 monopotassium) is in clinical trials. In this paper, we wish to report the investigation of the further details of structure-activity relationships (SARs) of the 2-phenylethenesulfonamide region in 1a. It was found that methyl substitutions at the 2-, 4- and 6-positions of the phenyl group in 1a led to the discovery of the ETA/ETB mixed antagonist (6s) with an IC50 of 2.2 nM for the ETA receptor. We also found that introduction of an ethyl group to the 1-position of the ethenyl group in 1a gave the ETA selective antagonist (6u) with an oral endothelin antagonistic activity in rats.