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

Article abstract of DOI:10.1248/cpb.45.1177

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.

Full text of DOI:10.1248/cpb.45.1177

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