Katsura Y, Nishino S, Inoue Y, Tomoi M, Takasugi H
New Drug Research Laboratories, Fujisawa Pharmaceutical Co., Ltd., Osaka, Japan.
Chem Pharm Bull (Tokyo). 1992 Feb;40(2):371-80. doi: 10.1248/cpb.40.371.
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.
合成了一系列咪唑并[1,2-α]吡啶基苯并恶唑（4）和5,6,7,8-四氢咪唑并[1,2-α]吡啶基苯并恶唑（5），并在大鼠中测试了其抗应激性溃疡活性。发现几种化合物比参比化合物硫糖铝、西咪替丁和雷尼替丁更具活性。其中一些化合物对乙醇诱导的胃损伤表现出强效保护活性。讨论了这些化合物的合成及构效关系。
