Chemical and Pharmaceutical Bulletin p. 2432 - 2441 (1992)
Update date:2022-08-03
Topics:
Katsura
Inoue
Tomishi
Itoh
Ishikawa
Takasugi
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.
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