181820-94-0

Upstream product

• 181822-48-0 2-[(4-methoxy-α-methylbenzyl)thio]-N-(4-pyridinyl)-3-pyridinecarboxamide 
• 504-24-5 4-aminopyridine 
• 38521-46-9 3-carboxy-2-mercaptopyridine 
• 3319-15-1 rac-1-(4-methoxyphenyl)-ethanol 
• 181824-11-3 2-[1-(4-Methoxy-phenyl)-ethylsulfanyl]-nicotinic acid 

Relevant academic research and scientific papers

Nicotinamide derivatives as a new class of gastric (H+/K+)-ATPase inhibitors. III. Synthesis and gastric antisecretory activity of 2-[(2- and 4-aminobenzyl, and α-methylbenzyl)sulfinyl]-N-(4-pyridinyl)-3- pyridinecarboxamides

A new series of 2-[(2-aminobenzyl, 4-aminobenzyl and α- methylbenzyl)sulfinyl]-N-(4-pyridinyl)-3-pyridinecarboxamides was synthesized and evaluated for gastric antisecretary activities. Several of the compounds synthesized exhibited potent inhibitory activities against [14C]aminopyrine accumulation stimulated by dibutyryl cyclic AMP in isolated rabbit parietal cells and histamine-induced gastric acid secretion in pylorus-ligated rats by intraduodenal administration. In particular, the more polar diastereoisomer of 2-[(4-methoxy-α-methylbenzyl)sulfinyl]-N-(4-pyridinyl)-3- pyridinecarboxamide (13b) showed in vivo inhibitory activity equivalent or superior to that of omeprazole and was a more selective (H+/K+)-ATPase inhibitor than omeprazole.

A convenient synthesis of n-substituted 2,3-dihydro-3-oxoisothiazolo[5,4-b]pyridines in acidic conditions

A novel and convenient synthesis of N-substituted 2,3-dihydro-3-oxoisothiazolo[5,4-b]pyridines which possess potent in vitro inhibitory activity against gastric (H+/K+)-ATPase is reported. Compared with the methods reported previously, the compounds were synthesized more readily in relatively high yields by conversion of N-substituted 2-(benzyl-, 1-phenylethyl-, and benzhydrylsulfinyl)nicotinamides (17d-l) in a diluted hydrochloric acid-methanol solution at room temperature.