Studies on Antiulcer Drugs. II. Synthesis and Antiulcer Activities of Imidazo(1,2-a)pyridinyl-2-alkylaminobenzoxazoles and 5,6,7,8-Tetrahydroimidazo(1,2-a)pyridinyl Derivatives.
作者:Yousuke KATSURA、Shigetaka NISHINO、Yoshikazu INOUE、Masaaki TOMOI、Hisashi TAKASUGI
DOI:10.1248/cpb.40.371
日期:——
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.
合成了一系列咪唑[1, 2-a]吡啶基苯并噁唑(4)和5, 6, 7, 8-四氢咪唑[1, 2-a]吡啶基苯并噁唑(5),并在大鼠中测试了它们的抗压力溃疡活性。发现几种化合物的活性超过了对照化合物舒克糖铝、西咪替丁和雷尼替丁。其中一些化合物对乙醇诱导的胃损伤表现出强效的保护活性。讨论了这些化合物的合成及其构效关系。