Piperidineacrylate Derivatives as Potential Antiallergy Agents

Mitsuo SUGIYAMA; Toshiaki SAKAMOTO; Yumiko KAMIGAKI; Hiroshi FUKUMI; Kazuhiro ITOH; Yumiko SATOH; Takeshi YAMAGUCHI

doi:10.1248/cpb.41.882

Mitsuo SUGIYAMA, Toshiaki SAKAMOTO, Yumiko KAMIGAKI, Hiroshi FUKUMI, Kazuhiro ITOH, Yumiko SATOH, Takeshi YAMAGUCHI

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Keywords: antiallergic agent, piperidineacrylate, structure-activity relationship, anti-passive cutaneous anaphylaxis activity, IgG₁-mediated bronchoconstriction inhibitory activity

JOURNAL FREE ACCESS

1993 Volume 41 Issue 5 Pages 882-888

DOI https://doi.org/10.1248/cpb.41.882

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Abstract

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-piperidimeacrylate (1a) was more potent than oxatomide and terfenadine in this assay, and was selected for further study. Some pharmacological properties of 1a are presented.

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