STUDIES ON ANTIULCER AGENTS .1. SYNTHESIS AND PHARMACOLOGICAL PROPERTIES OF ETHYL YLMETHYL]-4-DIMETHYLAMINO-5-PYRIMIDINECARBOXYLATE, A NEW H+ K+-ATPASE INHIBITOR POSSESSING MUCOSAL PROTECTIVE ACTIVITY/

Ethyl nylmethyl]-4-dimethylamino-5-pyrimidinecarboxylate (2) has been synthesized and evaluated for antiulcer properties. Compound 2 is a H/K+-ATPase inhibitor that affords mucosal protection against absolute ethanol-induced gastric lesions in rats after oral and parenteral admi nistrations. On the other hand, omeprazole, a representative H+/K+-ATP ase inhibitor, showed mucosal protective action only after oral admini stration, indicating that it required gastric acid secretion to genera te activity. The antiulcer activity of 2 in animal models, such as wat er-immersion Stress-induced gastric ulcer in rats and acidified aspiri n-induced gastric ulcer in rats, was three times higher than that of c imetidine.