912962-74-4

Basic information

• Product Name: 3-(3-((1H-imidazol-1-yl)methyl)phenyl)-N-(tert-butyl)-5-isobutylthiophene-2-sulfonamide
• Synonyms: 3-(3-((1H-imidazol-1-yl)methyl)phenyl)-N-(tert-butyl)-5-isobutylthiophene-2-sulfonamide
• CAS NO: 912962-74-4
• Molecular Weight: 431.623
• Mol File: 912962-74-4.mol
• Article Data: 3

Chemical Properties

• CAS DataBase Reference: 3-(3-((1H-imidazol-1-yl)methyl)phenyl)-N-(tert-butyl)-5-isobutylthiophene-2-sulfonamide(CAS DataBase Reference)
• NIST Chemistry Reference: 3-(3-((1H-imidazol-1-yl)methyl)phenyl)-N-(tert-butyl)-5-isobutylthiophene-2-sulfonamide(912962-74-4)
• EPA Substance Registry System: 3-(3-((1H-imidazol-1-yl)methyl)phenyl)-N-(tert-butyl)-5-isobutylthiophene-2-sulfonamide(912962-74-4)

Safety Data

• Hazardous Substances Data: 912962-74-4(Hazardous Substances Data)

Upstream product

• 823-78-9 meta-bromobenzyl bromide 
• 72459-47-3 1-(3-bromobenzyl)-1H-imidazole 
• 146013-28-7 N-(tert-butyl)-5-isobutylthiophene-2-sulphonamide 
• 286932-39-6 5-bromothiophene-2-sulphonic acid tert-butylamide 
• 163520-14-7 5-isobutyl-2 -(tert-butylaminosulfonyl)-3-thiopheneboronic acid 
• 15852-73-0 (3-Bromophenyl)methanol 
• 912942-72-4 3-(3-hydroxymethylphenyl)-5-isobutylthiophene-2-(N-tert-butyl)sulfonamide 

Relevant articles and documents

A convenient transesterification method for synthesis of AT2 receptor ligands with improved stability in human liver microsomes

A series of AT2R ligands have been synthesized applying a quick, simple, and safe transesterification-type reaction whereby the sulfonyl carbamate alkyl tail of the selective AT2R antagonist C38 was varied. Furthermore, a limited number of compounds where acyl sulfonamides and sulfonyl ureas served as carboxylic acid bioisosteres were synthesized and evaluated. By reducing the size of the alkyl chain of the sulfonyl carbamates, ligands 7a and 7b were identified with significantly improved in vitro metabolic stability in both human and mouse liver microsomes as compared to C38 while retaining the AT2R binding affinity and AT2R/AT1R selectivity. Eight of the compounds synthesized exhibit an improved stability in human microsomes as compared to C38.

NEW TRICYCLIC ANGIOTENSIN II AGONISTS

There is provided compounds of Formula (I), wherein A, X1, X2, X3, X4, Y1, Y2, Y3, Y4, Z1, Z2, R4 and R5 have meanings given in the description, and pharmaceuticalfy-acceptable salts thereof, which compounds are useful as selective agonists of the AT2 receptor, and thus, in particular, in the treatment of inter alia gastrointestinal conditions, such as dyspepsia, IBS and MOF, and cardiovascular disorders.