Chemical and Pharmaceutical Bulletin p. 1177 - 1182 (1997)
Update date:2022-08-03
Topics:
Terauchi, Hideo
Tanitame, Akihiko
Tada, Keiko
Nakamura, Keiji
Seto, Yasuhiro
Nishikawa, Yoshinori
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.
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