Effland R C
J Med Chem. 1977 Dec;20(12):1703-5. doi: 10.1021/jm00222a038.
2-Carboxyaryl-substituted dihydrobenz[e]indoles, tetrahydroindoles, and tetrahydrobenzofurans have been synthesized as structural analogues of fendosal, a new antiinflammatory agent, and tested in the carrageenan-induced rat paw edema assay. Two of these, 2-(3-carboxy-4-hydroxyphenyl)-3-phenyl-4,5-dihydrobenz[e]indole and 1-(n-butyl)-2-(3-carboxy-4-hydroxyphenyl)-4,5,6,7-tetrahydroindole, were found to have significant activity, albeit of a lower order than fendosal.
已合成了2-羧基芳基取代的二氢苯并[e]吲哚、四氢吲哚和四氢苯并呋喃,作为新型抗炎药芬多沙的结构类似物,并在角叉菜胶诱导的大鼠足爪水肿试验中进行了测试。其中两种化合物,即2-(3-羧基-4-羟基苯基)-3-苯基-4,5-二氢苯并[e]吲哚和1-(正丁基)-2-(3-羧基-4-羟基苯基)-4,5,6,7-四氢吲哚,被发现具有显著活性,尽管活性比芬多沙低。