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With the aim of applying mast cell-stabilizing agents as antiulcer agents, N-(1H-tetrazol-5-yl)-2-anilino-5-pyrimidinecarboxamides were synthesized, and initially evaluated pharmacologically for activity in the rat passive cutaneous anaphylaxis test by oral administration. The most active compound 6 was proved to inhibit potently the release of histamine from passively sensitized rat peritoneal mast cells in vitro. When compared with other mast cell-stabilizing agents and an antiulcer agent, compound 6 was found to show excellent gastric mucosal protection and gastric antisecretion activities. Furthermore, compound 6 revealed good activity against acidified aspirin ulcer in rats and water-immersion stress ulcer in rats.

chemical and pharmaceutical bulletin/chemical and pharmaceutical bulletin

Studies on Antiulcer Agents. II. Antiulcer Properties of N-(1H-Tetrazol-5-yl)-2-anilino-5-pyrimidinecarboxamides Inhibiting Release of Histamine from Passively Sensitized Rat Peritoneal Mast Cells.