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
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概要
- 論文の詳細を見る
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.
- 社団法人日本薬学会の論文
- 1994-09-15
著者
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松田 博
New Drug Research Laboratories Fujisawa Pharmaceutical Co. Ltd.
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重永 信次
New Drug Research Laboratories, Fujisawa Pharmaceutical Co., Ltd.,
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真鍋 孝司
New Drug Research Laboratories, Fujisawa Pharmaceutical Co., Ltd.,
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藤井 隆
New Drug Research Laboratories, Fujisawa Pharmaceutical Co., Ltd.,
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松尾 昌昭
New Drug Research Laboratories, Fujisawa Pharmaceutical Co., Ltd.,
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真鍋 孝司
New Drug Research Laboratories Fujisawa Pharmaceutical Co. Ltd.
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松尾 昌昭
New Drug Research Laboratories Fujisawa Pharmaceutical Co. Ltd.
-
重永 信次
New Drug Research Laboratories Fujisawa Pharmaceutical Co. Ltd.
-
藤井 隆
New Drug Research Laboratories Fujisawa Pharmaceutical Co. Ltd.
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