Studies on antiulcer drugs. VI. 4-Furyl-2-guanidinothiazoles and related compounds as potent histamine H2-receptor antagonists

DOI: 10.1248/cpb.40.2432

Source and publish data:

Chemical and Pharmaceutical Bulletin p. 2432 - 2441 (1992)

Update date:2022-08-03

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Authors:

Katsura Katsura

Inoue Inoue

Tomishi Tomishi

Itoh Itoh

Ishikawa

Takasugi

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Article abstract of DOI:10.1248/cpb.40.2432

A series of 4-furyl-2-guanidinothiazole derivatives and related compounds were synthesized and evaluated for histamine H₂-receptor antagonist and gastric acid antisecretory activities. Among them, compounds I-17, I-48 and I-49 showed high activities in these tests. In addition, compound I-17 possessed potent inhibitory activities on each of the gastric ulcers induced by stress, ethanol and HCl-aspirin. On the other hand, compound I-48 demonstrated antimicrobial activity against Helicobacter pylori and the potency was far stronger than that of clinically used H₂-antagonists. Some structure-activity relationships are discussed.

Full text of DOI:10.1248/cpb.40.2432

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