Synthesis and biological activity of spiro[isocoumarin-piperidines] and related compounds. I
摘要:
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.
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关键词:
isocoumarin isochroman piperidine analgesic activity histaminerelease inhibition structure-activity relationship spiro compound
DOI:
10.1248/cpb.29.402
被引量:
年份:
1981
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