1027262-54-9

Upstream product

• 113805-35-9 (2-Chloromethyl-phenyl)-diethyl-amine 
• 1027173-39-2 6a-Hydroxy-1-pyridin-4-yl-hexahydro-cyclopentaimidazole-2-thione 
• 87066-93-1 (2-Diethylamino-phenyl)-methanol 
• 76105-84-5 pyridin-4-yl isothiocyanate 
• 91563-72-3 N,N-diethylanthranilic acid methyl ester 
• 394-35-4 methyl 2-fluorobenzoate 
• 504-24-5 4-aminopyridine 

Relevant academic research and scientific papers

2-[(2-Aminobenzyl)sulfinyl]-1-(2-pyridyl)-1,4,5,6- tetrahydrocyclopent[d]imidazoles as a novel class of gastric H+/K+-ATPase inhibitors

Substituted 2-sulfinylimidazoles were synthesized and investigated as potential inhibitors of gastric H+/K+-ATPase. The 4,5-unsubstituted imidazole series 6-11 and the 1,4,5,6-tetrahydrocyclopent[d]imidazole series 12 were found to be potent inhibitors of the acid secretory enzyme H+/K+- ATPase. Structure-activity relationships indicate that the substitution of 2- pyridyl groups at the 1-position of the imidazole moiety combined with (2- aminobenzyl)sulfinyl groups at the 2-position leads to highly active compounds with a favorable chemical stability. Other substitution patterns in the imidazole moiety result in reducing biological activities. 2-[(2- Aminobenzyl)sulfinyl]-1-[2-(3-methylpyridyl)]-1,4,5,6- tetrahydrocyclopent[d]imidazole (12h, T-776) was selected for further development as a potential clinical candidate. Extensive study on the acid degradation of 12h indicates a mechanism of action different from that of omeprazole, the first H+/K+-ATPase inhibitor introduced to the market.