141541-65-3

Upstream product

• 141541-48-2 [2-(1H-Imidazol-2-ylsulfanylmethyl)-4-methoxy-phenyl]-(2-methoxy-ethyl)-amine 
• 32382-72-2 4-methoxy-N-(2-methoxyethyl)aniline 
• 141564-64-9 (2-Methanesulfinylmethyl-4-methoxy-phenyl)-(2-methoxy-ethyl)-amine 

Relevant academic research and scientific papers

Anti-ulcer composition containing imidazole derivative

Disclosed is an anti-ulcer composition to be dissolved in stomach to become directly into contact with walls of the stomach which comprises 100 weight parts of an imidazole derivative of the formula: wherein each of R1 and R2 is hydrogen, substituted or unsubstituted alkyl, alkoxyalkyl, cycloalkyl, aryl, aralkyl, or R1 and R2 are combined to form hetero ring; each of R3, R4, R5 and R6 is hydrogen, halogen, substituted or unsubstituted alkoxy, substituted or unsubstituted alkyl, aryl, aryloxy, alkoxycarbonyl, nitro, amino, acyl, or R3 is combined with R2 to form heteroring; R7 is hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted aryl, substituted or unsubstituted arylcarbonyl, or S-containing heteroring; and each of R8 and R9 is hydrogen, halogen, substituted or unsubstituted alkoxy, unsubstituted or substituted alkyl, alkoxycarbonyl, aralkyl, nitro, amino, acyl, substituted or unsubstituted aryl, or R8 and R9 are combined to form alkylene, and 50 - 2,000 weigt parts of a basic material.

Synthesis and structure-activity relationships of substituted 2-[(2-imidazolylsulfinyl)methyl]anilines as a new class of gastric H+/K+-ATPase inhibitors. II.

A series of 2-[(2-imidazolylsulfinyl)methyl]anilines (2) having various substituents on their imidazole and aniline rings was synthesized and examined for their H+/K+-ATPase (adenosine triphosphatase) inhibitory effects and antisecretory activity against histamine-stimulated gastric acid secretions in Heidenhain pouch dogs. Although substitutions on the imidazole ring did not enhance biological activity, substitution on the aniline ring by electrondonating substituents potently enhanced the enzyme inhibitory activity and also showed an inhibitory effect on histamine-stimulated gastric acid secretion after oral administration. In particular, the in vitro activity of the dimethyl (2u-w) and trimethyl (2ac) derivatives was about 10 times that of omeprazole. Also, 4-methyl (2k), 4-methoxy-5-methyl (2y) and 3,5-dimethyl-4-methoxy (2ab) derivatives showed a potent antisecretory effect of more than 80% after oral administration at 6 mg/kg. Although these aniline derivatives have relatively low stabilities in aqueous solution, replacement of the isobutyl group at the aniline nitrogen atom with N-(2-methoxyethyl) group enhanced the stability.