210988-74-2

Upstream product

• 3350-78-5 3,3-Dimethylacryloyl chloride 
• 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 
• 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 
• 210988-29-7 5-Amino-2-butyl-3-[2'-(1-trityl-1H-tetrazol-5-yl)-biphenyl-4-ylmethyl]-3H-imidazole-4-carboxylic acid ethyl ester 
• 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 
• 133614-30-9 N-(N'-cyanovalerimidolyl)glycine ethyl ester 
• 76-83-5 trityl chloride 
• 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 

Downstream Products

• 210988-88-8 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 3-oxo-1,3-dihydro-isobenzofuran-1-yl ester 
• 210988-82-2 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 2,2-dimethyl-propionyloxymethyl ester 
• 210988-85-5 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 5-methyl-2-oxo-[1,3]dioxol-4-ylmethyl ester 
• 210988-78-6 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 

Relevant academic research and scientific papers

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.