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

Yousuke KATSURA; Yoshikazu INOUE; Sigetaka NISHINO; Masaaki TOMOI; Harunobu ITOH; Hisashi TAKASUGI

doi:10.1248/cpb.40.1424

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

Yousuke KATSURA, Yoshikazu INOUE, Sigetaka NISHINO, Masaaki TOMOI, Harunobu ITOH, Hisashi TAKASUGI

Author information

Keywords: histamine H₂-receptor antagonist, antiulcer activity, cytoprotective activity, antisecretory activity, imidazo[1, 2-a]pyridinylethylbenzoxazole, structure-activity relationship

JOURNAL FREE ACCESS

1992 Volume 40 Issue 6 Pages 1424-1438

DOI https://doi.org/10.1248/cpb.40.1424

Details

Abstract

A series of imidazo[1, 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[1, 2-a]pyridin-2-yl)ethyl]benzoxazole derivatives were found to have good pharmacological activities. Among them, 2-amino-6-[2-(7-methoxy-3-methylimidazo[1, 2-a]pyridin-2-yl)ethyl]benzoxazole (II-11) and 2-acetamido-6-[2-(7-methylimidazo[1, 2-a]pyridin-2-yl)ethyl]benzoxazole (II-38) showed potent antisecretory and cytoprotective activity. The structure-activity relationships of these compounds are discussed.

Corresponding author

Register with J-STAGE for free!