Studies on Antiulcer Drugs: III: 1) Synthesis and Antiulcer Activities of Imidazo[l,2-a]pyridinylethyl-benzoxazoles and Related Compounds: A Novel Class of Histamine H2-Receptor Antagonists

Abstract

A series of imidazo[l,2-a]pyridinylalkylbenzoxazole derivatives was synthesized and tested for histamine H2-receptor antagonist, gastric antisecretory and antiulcer activities. Some of 2-amino-6-[2-(imidazo[l,2-a]pyr id in-2-yl)ethyl]benzoxazole derivatives were found to have good pharmacological activities. Among them, 2-amino-6-[2-(7-methoxy-3-methylimidazo[l,2-a]pyridin-2-yl)ethyl]benzoxazole (II-11) and 2-acetamido-6-[2-(7-methylimidazo[l,2-a]pyridin-2-yl)ethyl]benzoxazole (11–38) showed potent antisecretory and cytoprotective activity. The structure-activity relationships of these compounds are discussed. © 1992, The Pharmaceutical Society of Japan. All rights reserved.