Acrylamide Derivatives as Antiallergic Agents. I. : Synthesis and Structure-Activity Relationship of N-[(4-Substituted 1-piperazinyl)alkyl]-3-(aryl and heteroaryl)acrylamides
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概要
- 論文の詳細を見る
A new series of acrylamide derivatives (7-10) were synthesized. Antiallergic activity of these compounds was evaluated and their structure-activity relationships were examined. Compounds 10d, N[4-(4-diphenylmethyl-1-piperazinyl)buthyl]3-(3-pyridyl)acrylamide, showed antiallergic activity equivalent or superior to that of ketotifen in the rat passive cutaneous anaphylaxis (PCA) test by oral administration. Compound 10d, unlike ketotifen, had more potent in vitro 5-lipoxygenase inhibitory activity than caffeic acid, whereas its in vitro antihistamine activity was weaker than that of ketotifen. In addition, its inhibitory activity against histamine release from rat mast cells was approximately two-thirds as potent as that of disodium cromoglycate (DSCG). Compound 10d is a promising agent for treating a variety of allergic diseases.
- 公益社団法人日本薬学会の論文
- 1989-01-25
著者
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中村 秀雄
Research Laboratories Dainippon Pharmaceutical Co. Ltd.
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宇野 準
Research Laboratories, Dainippon Pharmaceutical Co., Ltd.,
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石井 勝美
Research Laboratories Dainippon Pharmaceutical Co. Ltd.
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西川 義則
Research Laboratories, Dainippon Pharmaceutical Co., Ltd.,
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新藤 徳彦
Research Laboratories, Dainippon Pharmaceutical Co., Ltd.,
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近 達也
Research Laboratories, Dainippon Pharmaceutical Co., Ltd.,
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宇野 準
大日本製薬株式会社
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近 達也
Research Laboratories Dainippon Pharmaceutical Co. Ltd.
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宇野 準
Research Laboratories Dainippon Pharmaceutical Co. Ltd.
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西川 義則
Research Laboratories Dainippon Pharmaceutical Co. Ltd.
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新藤 徳彦
Research Laboratories Dainippon Pharmaceutical Co. Ltd.
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