Benzylpiperazine Derivatives. VIII. Syntheses, Antiulcer and Cytoprotective Activities of 1-(Aminocarbonylalkyl)-4-benzylpiperazine Derivatives and Related Compounds

Abstract

From a search for antiulcer agents with cytoprotective activity by random screening, 1-(pyrrolidinocarbonylmethyl)-4-(2, 3, 4-trimethoxybenzyl) piperazine dimaleate (4h) was found as a lead compound. Analogues of 4h were synthesized and evaluated for antiulcer activity as well as toxicity. Four compounds (4h, p, w, x) exhibited potent antiulcer activity in several gastric ulcer models and low toxicity without any antisecretory activity. The antiulcer activity of these compounds was considered to be based on the cytoprotective activity.