Piperidineacrylate Derivatives as Potential Antiallergy Agents.
作者:Mitsuo SUGIYAMA、Toshiaki SAKAMOTO、Yumiko KAMIGAKI、Hiroshi FUKUMI、Kazuhiro ITOH、Yumiko SATOH、Takeshi YAMAGUCHI
DOI:10.1248/cpb.41.882
日期:——
A new series of piperidineacrylate derivatives was prepared and evaluated for antiallergic activity. Most of the compounds showed potent activities in the rat passive cutaneous anaphylaxis (PCA) assay. In particular, ethyl 1-[2-bis(4-fluorophenyl)methoxyethyl]-4-piperidineacrylate (1a) was more potent than oxatomide and terfenadine in this assay, and was selected for further study. Some pharmacological
制备了一系列新的哌啶丙烯酸酯衍生物,并评估了其抗过敏活性。大多数化合物在大鼠被动皮肤过敏反应(PCA)分析中显示出有效的活性。特别地,在该测定法中,乙基1- [2-双(4-氟苯基)甲氧基乙基] -4-哌啶丙烯酸酯(1a)比氧原子化物和特非那定更有效,因此被选作进一步研究。介绍了1a的一些药理特性。