Thromboxane A_2 Synthetase Inhibitors with Histamine H_1-Blocking Activity : Synthesis and Evaluation of a New Series of Indole Derivatives
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概要
- 論文の詳細を見る
A novel series of N-substituted 3-(1H-imidazol-1-ylmethyl)indole carboxylic acid derivatives were prepared and evaluated for thromboxane A_2 (TXA_2) synthetase-inhibitory and histaminergic H_1-blocking activity. Among the compounds synthesized, indole-6-carboxylic acid derivatives showed higher activities than the other positioal isomers of carboxylic acid. 1-[3-(4-Benzhyrdyl-1-piperazinyl)propyl]-3-(1H-imidazol-1-ylmethyl)-1H-indole-6-carboxylic acid (12) had the strongest thromboxane synthetase inhibitory activity (IC_<50>=5×10^<-8>M) and H_1-blocking activity (IC_<50>=8×10^<-9>M).
- 公益社団法人日本薬学会の論文
- 1995-10-15
著者
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松井 博
Research Laboratories Kyoto Pharmaceutical Industries Ltd.
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神田 守
Research Laboratories Kyoto Pharmaceutical Industries Ltd.
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掛谷 宣治
Research Laboratories Kyoto Pharmaceutical Industries Ltd.
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白波瀬 弘明
Research Laboratories Kyoto Pharmaceutical Industries Ltd.
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神谷 尚治
Research Laboratories Kyoto Pharmaceutical Industries Ltd.
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Kamiya Shoji
Research Laboratories Kyoto Pharmaceutical Industries Ltd.
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白波瀬 弘明
京都大学・riセンター・薬理学研究室
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中村 正平
Research Laboratories Kyoto Pharmaceutical Industries Ltd.
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中村 正平
京都薬品・研究部
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和田 勝夫
Research Laboratories Kyoto Pharmaceutical Industries Ltd.
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Wada Katsuo
Research Laboratories Kyoto Pharmaceutical Industries Ltd.
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嶋路 久延
Research Laboratories, Kyoto Pharmaceutical Industries, Ltd.,
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嶋路 久延
Research Laboratories Kyoto Pharmaceutical Industries Ltd.
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