Chemical and Pharmaceutical Bulletin p. 1027 - 1038 (1997)
Update date:2022-08-02
Topics:
Terauchi, Hideo
Tanitame, Akihiko
Tada, Keiko
Nakamura, Keiji
Seto, Yasuhiro
Nishikawa, Yoshinori
Members of a new series of 2-[(2,4-dimethoxybenzyl)sulfinyl]-N-(4- pyridinyl)pyridine-3-carboxamides were synthesized and evaluated for their gastric antisecretory activity and the ability to inhibit cytochrome P450- dependent O-dealkylation of 7-ethoxycoumarin (7-EC) in rat liver microsomes. Several of the compounds synthesized exhibited potent inhibitory activities against both [14C]aminopyrine accumulation stimulated by dibutyryl cyclic AMP in isolated rabbit parietal cells and histamine-induced gastric acid secretion in pylorus-ligated rats when administered intraduodenally; their inhibitory activities were equivalent to or superior to those of the parent compound [2[(2,4-dimethoxybenzyl)sulfinyl]-N-(4-pyridinyl)pyridine-3- carboxamide] and omeprazole. Among the compounds having potent antisecretory activity in vitro and in vivo, 2-[(2,4-dimethoxybenzyl)sulfinyl]-N-(2,5- dimethyl-4-pyridinyl)pyridine-3-carboxamide and 2-[(2,4- dimethoxybenzyl)sulfinyl]-N-(2,6-dimethyl-4-pyridinyl)pyridine-3-carboxamide in particular showed lower inhibitory activity against the 7-EC deethylase than omeprazole. It seems probable that, unlike omeprazole, these compounds do not interact with a metabolism of other drugs in vivo. These compounds, therefore, are considered to be more promising candidate agents for treating acid-related gastrointestinal disorders than the parent compound reported previously.
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