133485-83-3

Basic information

• Product Name: (E)-3-[2-n-butyl-1-{(2-trifluoromethylphenyl)methyl}-1H-imidazol-5-yl]-2-(thien-2-yl)methyl-2-propenoic acid
• Synonyms: (E)-3-[2-n-butyl-1-{(2-trifluoromethylphenyl)methyl}-1H-imidazol-5-yl]-2-(thien-2-yl)methyl-2-propenoic acid
• CAS NO: 133485-83-3
• Molecular Weight: 448.509
• Mol File: 133485-83-3.mol

Chemical Properties

• CAS DataBase Reference: (E)-3-[2-n-butyl-1-{(2-trifluoromethylphenyl)methyl}-1H-imidazol-5-yl]-2-(thien-2-yl)methyl-2-propenoic acid(CAS DataBase Reference)
• NIST Chemistry Reference: (E)-3-[2-n-butyl-1-{(2-trifluoromethylphenyl)methyl}-1H-imidazol-5-yl]-2-(thien-2-yl)methyl-2-propenoic acid(133485-83-3)
• EPA Substance Registry System: (E)-3-[2-n-butyl-1-{(2-trifluoromethylphenyl)methyl}-1H-imidazol-5-yl]-2-(thien-2-yl)methyl-2-propenoic acid(133485-83-3)

Safety Data

• Hazardous Substances Data: 133485-83-3(Hazardous Substances Data)

Upstream product

• 16862-05-8 methyl 3-(2-thienyl)propanoate 
• 346-06-5 (2-(trifluoromethyl)phenyl)methanol 
• 68283-19-2 2-n-butyl-4-(hydroxymethyl)imidazole 
• 133486-41-6 1-acetyl-4-acetoxymethyl-2-n-butylimidazole 

Downstream Products

• 133486-12-1 (E)-3-[2-n-Butyl-1-{(2-trifloromethylphenyl)methyl}-1H-imidazol-5-yl]-2-(2-thienyl)methyl-2-propenamide 

Relevant articles and documents

Potent Nonpeptide Angiotensin II Receptor Antagonists. 2. (1-Carboxybenzyl)imidazole-5-acrylic Acids

The further evolution of the imidazole-5-acrylic acid series of nonpeptide angiotensin II receptor antagonists is detailed (for Part 1, see: J.Med.Chem. 1992, 35, 3858).Modifications of the N-benzyl ring substitution were undertaken in an effort to mimic the Tyr4 residue of angiotensin II.Introduction of a p-carboxylic acid on the N-benzyl ring resulted in the discovery of compounds with nanomolar affinity for the receptor and good oral activity.SAR studies of these potent antagonists revealed that the thienyl ring, the (E)-acrylic acid, and the imidazole ring in addition to the two acid groups were important for high potency.Also, overlay comparisons of the parent diacid with both angiotensin II and a representative biphenylyltetrazole nonpeptide angiotensin II receptor antagonist are presented.The parent diacid analog, SKF 108566 or (E)-3--2-propenoic acid, is currently in clinical development for the treatment of hypertension.

Imidazolyl-alkenoic acids useful as angiotensin II receptor antagonists

Angiotensin II receptor antagonists having the formula: STR1 which are useful in regulating hypertension and in the treatment of congestive heart failure, renal failure, and glaucoma, pharmaceutical compositions including these antagonists, and methods of using these compounds to produce angiotensin II receptor antagonism in mammals.