Studies on antiulcer drugs. II. Synthesis and antiulcer activities of imidazo[1,2-alpha]pyridinyl-2-alkylaminobenzoxazoles and 5,6,7,8-tetrahydroimidazo[1,2-alpha]pyridinyl derivatives.
A series of imidazo[1,2-alpha]pyridinylbenzoxazoles (4) and 5,6,7,8-tetrahydroimidazo[1,2-alpha]pyridinylbenzoxazoles (5) were synthesized and tested for anti-stress ulcer activity in rats. Several compounds were found to be more active than the reference compounds, sucralfate, cimetidine and ranitidine. Some of them exhibited potent protective activity against ethanol-induced gastric lesion. The synthesis and structure-activity relationships of these compounds are discussed.
Katsura
Y
Y
New Drug Research Laboratories, Fujisawa Pharmaceutical Co., Ltd., Osaka, Japan.
Nishino
S
S
Inoue
Y
Y
Tomoi
M
M
Takasugi
H
H
D000818:Animals; D000897:Anti-Ulcer Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D001583:Benzoxazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D002927:Cimetidine / Q000494:pharmacology; D000431:Ethanol / Q000633:toxicity; D007093:Imidazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D009682:Magnetic Resonance Spectroscopy; D011725:Pyridines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D011899:Ranitidine / Q000494:pharmacology; D013276:Stomach Ulcer / Q000139:chemically induced / Q000188:drug therapy*; D013312:Stress, Physiological; D013329:Structure-Activity Relationship; D013392:Sucralfate / Q000494:pharmacology
D000897:Anti-Ulcer Agents; D001583:Benzoxazoles; D007093:Imidazoles; D011725:Pyridines; D000431:Ethanol; D013392:Sucralfate; D002927:Cimetidine; D011899:Ranitidine