STUDIES ON ANTIULCER DRUGS .6. 4-FURYL-2-GUANIDINOTHIAZOLES AND RELATED-COMPOUNDS AS POTENT HISTAMINE-H2-RECEPTOR ANTAGONISTS

A series of 4-furyl-2-guanidinothiazole derivatives and related compounds were synthesized and evaluated for histamine H-2-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 148 demonstrated antimicrobial activity against Helicobacter Pylori and the potency was far stronger than that of clinically used H-2-antagonists. Some structure-activity relationships are discussed.