Chemical and Pharmaceutical Bulletin · 1992 · 67 citations · 0 references
PharmacyMedicinal ChemistryPharmacologyDrug DiscoveryStructure-activity RelationshipsSynthetic Medicinal ChemistryGastrointestinal PharmacologyStructure-activity Relationship AnalysisChemical Structure-activity RelationshipsGastric Ulcer PreventionGastroprotective AgentsPyrazole Chemistry
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.