STUDIES ON ANTIULCER DRUGS .2. SYNTHESIS AND ANTIULCER ACTIVITIES OF IMIDAZO[1,2-A]PYRIDINYL-2-ALKYLAMINOBENZOXAZOLES AND 5,6,7,8-TETRAHYDROIMIDAZO[1,2-A]PYRIDINYL DERIVATIVES

被引:64
作者
KATSURA, Y [1 ]
NISHINO, S [1 ]
INOUE, Y [1 ]
TOMOI, M [1 ]
TAKASUGI, H [1 ]
机构
[1] FUJISAWA PHARMACEUT CO LTD, PROD DEV LABS, OSAKA 532, JAPAN
关键词
ANTISTRESS ULCER ACTIVITY; ETHANOL-INDUCED GASTRIC LESION; CYTOPROTECTIVE ACTIVITY; IMIDAZO[1,2-A]PYRIDINYLBENZOXAZOLE; 5,6,7,8-TETRAHYDROIMIDAZO[1,2-A]PYRIDINYLBENZOXAZOLE; SUCRALFATE; CIMETIDINE; RANITIDINE; STRUCTURE-ACTIVITY RELATIONSHIP;
D O I
10.1248/cpb.40.371
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
A series of imidazo[1,2-a]pyridinylbenzoxazoles (4) and 5,6,7,8-tetrahydroimidazo[1,2-a]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.
引用
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页码:371 / 380
页数:10
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