Synthesis and biological activity of spiro(isocoumarin-piperidines) and reltaed compounds. I.
作者:MASATOSHI YAMATO、KUNIKO HASHIGAKI、MASAO IKEDA、HIDETOSHI OHTAKE、KENJI TASAKA
DOI:10.1248/cpb.29.402
日期:——
1'-Alkylspiro [isochroman-3, 4'-piperidin]-1-ones (2) and 1'-alkylspiro [isochroman-4, 4'-piperidines] (4 and 5) were prepared and examined for analgesic activity. Several of the 4-spiro compounds (3, 4, and 5) were found to have analgesic activity as potent as that of aminopyrine, while the 3-spiro compounds (2) were inactive. Further pharmacological studies revealed that several of these compounds inhibited the histamine release induced by compound 48/80 from isolated rat peritoneal mast cells.
1'-烷基螺[异香豆素-3, 4'-哌啶]-1-酮(2)和1'-烷基螺[异香豆素-4, 4'-哌啶](4和5)已经被合成并检查其镇痛活性。发现其中几种4-螺化合物(3、4和5)的镇痛活性与氨基吡嗪相当,而3-螺化合物(2)则无活性。进一步的药理研究表明,这些化合物中的几种抑制了由化合物48/80诱导的孤立大鼠腹膜肥大细胞释放组胺。