210988-78-6

Basic information

• Product Name: 2-Butyl-5-[methyl-(3-methyl-but-2-enoyl)-amino]-3-[2'-(1-trityl-1H-tetrazol-5-yl)-biphenyl-4-ylmethyl]-3H-imidazole-4-carboxylic acid 1-ethoxycarbonyloxy-ethyl ester
• Synonyms: 2-Butyl-5-[methyl-(3-methyl-but-2-enoyl)-amino]-3-[2'-(1-trityl-1H-tetrazol-5-yl)-biphenyl-4-ylmethyl]-3H-imidazole-4-carboxylic acid 1-ethoxycarbonyloxy-ethyl ester
• CAS NO: 210988-78-6
• Molecular Weight: 872.036
• Mol File: 210988-78-6.mol
• Article Data: 1

Chemical Properties

• CAS DataBase Reference: 2-Butyl-5-[methyl-(3-methyl-but-2-enoyl)-amino]-3-[2'-(1-trityl-1H-tetrazol-5-yl)-biphenyl-4-ylmethyl]-3H-imidazole-4-carboxylic acid 1-ethoxycarbonyloxy-ethyl ester(CAS DataBase Reference)
• NIST Chemistry Reference: 2-Butyl-5-[methyl-(3-methyl-but-2-enoyl)-amino]-3-[2'-(1-trityl-1H-tetrazol-5-yl)-biphenyl-4-ylmethyl]-3H-imidazole-4-carboxylic acid 1-ethoxycarbonyloxy-ethyl ester(210988-78-6)
• EPA Substance Registry System: 2-Butyl-5-[methyl-(3-methyl-but-2-enoyl)-amino]-3-[2'-(1-trityl-1H-tetrazol-5-yl)-biphenyl-4-ylmethyl]-3H-imidazole-4-carboxylic acid 1-ethoxycarbonyloxy-ethyl ester(210988-78-6)

Safety Data

• Hazardous Substances Data: 210988-78-6(Hazardous Substances Data)

Upstream product

• 210988-74-2 2-Butyl-5-[methyl-(3-methyl-but-2-enoyl)-amino]-3-[2'-(1-trityl-1H-tetrazol-5-yl)-biphenyl-4-ylmethyl]-3H-imidazole-4-carboxylic acid 
• 80196-04-9 ethyl 1-iodoethylcarbonate 
• 3350-78-5 3,3-Dimethylacryloyl chloride 
• 50893-36-2 1-Chloroethyl ethyl carbonate 
• 133614-30-9 N-(N'-cyanovalerimidolyl)glycine ethyl ester 
• 149586-21-0 2-Butyl-5-[methyl-(3-methyl-but-2-enoyl)-amino]-3-[2'-(1H-tetrazol-5-yl)-biphenyl-4-ylmethyl]-3H-imidazole-4-carboxylic acid 
• 149586-20-9 2-Butyl-5-[methyl-(3-methyl-but-2-enoyl)-amino]-3-[2'-(1H-tetrazol-5-yl)-biphenyl-4-ylmethyl]-3H-imidazole-4-carboxylic acid ethyl ester 
• 210988-29-7 5-Amino-2-butyl-3-[2'-(1-trityl-1H-tetrazol-5-yl)-biphenyl-4-ylmethyl]-3H-imidazole-4-carboxylic acid ethyl ester 
• 210988-38-8 2-Butyl-5-(3-methyl-but-2-enoylamino)-3-[2'-(1-trityl-1H-tetrazol-5-yl)-biphenyl-4-ylmethyl]-3H-imidazole-4-carboxylic acid ethyl ester 
• 210988-40-2 2-Butyl-5-[methyl-(3-methyl-but-2-enoyl)-amino]-3-[2'-(1-trityl-1H-tetrazol-5-yl)-biphenyl-4-ylmethyl]-3H-imidazole-4-carboxylic acid ethyl ester 

Relevant articles and documents

Studies on nonpeptide angiotensin II receptor antagonists. IV. Synthesis and biological evaluation of 4-acrylamide-1H-imidazole derivatives

A novel series of nonpeptide angiotensin II antagonists containing the acrylamide group at the 4-position of the imidazole ring was synthesized and their antagonistic activity was examined by functional assay in rabbit aorta. The acrylamide group was selected as a large lipophilic surrogate for the chloro group of EXP3174. A structure-activity relationship study of the acrylamide moiety has shown that substitution at the 4-position with the N- methyl-3,3-dimethylacrylamide group resulted in the optimal compound, 2- butyl-4-[(3,3-dimethylacryloyl)methyl-amino]-1-[[2'-(1H-tetrazol-5- yl)biphenyl-4-yl]methyl]-1H-imidazole-5-carboxylic acid (1), which was superior to EXP3174 in vitro. Since 1 showed only poor activity against angiotensin II-induced pressor response in rats after oral administration, the carboxylic acid function of 1 was converted into prodrug esters (13). Among these, the 1-[(ethoxycarbonyl)oxy]ethyl ester (13a) showed the most potent and longest-lasting activity when given orally to rats. When administered orally to conscious furosemide-treated dogs, 13a showed an approximately 3-fold increased hypotensive activity in comparison with DuP 753. These data suggest that 13a may be an useful agent for the treatment of angiotensin II-dependent diseases, such as hypertension.