Synthesis and Structure-Activity Relationships of Antiallergic N-[4-[4-(1H-Indol-3-yl)piperidinoalkyl]-2-thiazolyl]alkanamides Possessing Both Antihistaminic and Anti Slow-Reacting Substance (SRS) Activites

  • 重永 信次
    New Drug Research Laboratories, Fujisawa Pharmaceutical Co., Ltd.,
  • 真鍋 孝司
    New Drug Research Laboratories, Fujisawa Pharmaceutical Co., Ltd.,
  • 松田 博
    New Drug Research Laboratories, Fujisawa Pharmaceutical Co., Ltd.,
  • 藤井 隆
    New Drug Research Laboratories, Fujisawa Pharmaceutical Co., Ltd.,
  • 松尾 昌昭
    New Drug Research Laboratories, Fujisawa Pharmaceutical Co., Ltd.,

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抄録

A series of N-[4-[4-(1H-indol-3-yl)piperidinoalkyl]-2-thiazolyl]alkanamide derivatives were synthesized and tested for in vivo antianaphylactic activity and in vitro anti slow-reacting substance (SRS) activity. Among the compounds synthesized, N-[4-[4-(1H-indol-3-yl)piperidinomethyl]-2-thiazolyl]propanamide (7) was the best balanced compound (antianaphylactic activity, ED_<50>=0.92mg/kg p.o.; anti-SRS activity, IC_<50>=0.89μg/ml). Regarding the biological activities of 7,we ascribe the antianaphylactic activity to its potent antihistaminic activity and the anti SRS activity to the inhibition of 5-lipoxygenase.

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詳細情報 詳細情報について

  • CRID
    1571698602302078080
  • NII論文ID
    110003631242
  • NII書誌ID
    AA00602100
  • ISSN
    00092363
  • 本文言語コード
    en
  • データソース種別
    • CiNii Articles

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