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用于抑制组胺释放的螺[异苯并二氢吡喃哌啶]类似物的合成及其构效关系

Synthesis and structure-activity relationship of spiro[isochromanpiperidine] analogues for inhibition of histamine release.

作者信息

Yamato M, Hashigaki K, Ikeda M, Ohtake H, Tasaka K

出版信息

J Med Chem. 1981 Feb;24(2):194-8. doi: 10.1021/jm00134a013.

DOI:10.1021/jm00134a013
PMID:6162958
Abstract

Two types of 1'-alkylspiro[isochroman-3,4-piperidines] and 1'-alkylspiro[isochroman-4,4'-piperidines] were prepared and examined for their biological activity. Several of the compounds inhibited the compound 48/80 induced histamine release from isolated rat peritoneal mast cells. The structural requirements for this activity in the present series are discussed.

摘要

制备了两种类型的1'-烷基螺[异苯并二氢吡喃-3,4-哌啶]和1'-烷基螺[异苯并二氢吡喃-4,4'-哌啶]，并对其生物活性进行了研究。其中几种化合物抑制了化合物48/80诱导的离体大鼠腹膜肥大细胞组胺释放。讨论了本系列中该活性的结构要求。

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