130510-70-2

Upstream product

• 106771-59-9 2-(chloromethyl)-N,N-dimethylaniline 
• 1027972-55-9 N-[6-(2-Thioxo-2,3-dihydro-imidazol-1-yl)-pyridin-3-yl]-acetamide 
• 394-35-4 methyl 2-fluorobenzoate 
• 4707-56-6 (2-(dimethylamino)phenyl)methanol 
• 75-36-5 acetyl chloride 
• 117296-28-3 1-(5-amino-pyridin-2-yl)-2-[2-(dimethylamino)benzylthio]imidazole 
• 1027173-69-8 N-{6-[3-(2,2-Diethoxy-ethyl)-thioureido]-pyridin-3-yl}-acetamide 
• 41292-44-8 N-(6-amino-pyridin-3-yl)-acetamide 
• 10072-05-6 methyl 2-(dimethylamino)benzoate 

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.

Pyridyl-substituted imidazoles, compositions containing same and methods of use thereof

Novel imidazole of the formula: STR1 wherein Ring A is pyridyl group or a substituted pyridyl group; Ring B is phenyl group or a substituted phenyl group; R1 and R2 are hydrogen atom or are combined together to form a group of the formula: --(CH2)q --; m is 1 or 2; n is 0, 1 or 2; and q is 3 or 4, or a salt thereof are disclosed. Said derivative (I) and a salt thereof are useful as anti-ulcer agents.