Synthesis and Gastrointestinal Prokinetic Activity of Novel Benzamide Derivatives with Amphoteric Side Chains
スポンサーリンク
概要
- 論文の詳細を見る
Novel benzamide derivatives(19-24, 32a-c, 43d-f), each possessing a cycloaminoalkanecarboxylic acid side chian, were synthesized and their gastrointestinal prokinetic and dopamine D_2 receptor antagonist activities were evaluated. 4-[(4-Amino-5-chloro-2-methoxybenzoyl)amino]-1-piperidineacetic acid(19)exhibited the most potent gastro- and colon-prokinetic activities, through intravenous administration to conscious dogs, and also showed the reduced dopamine D_2 receptor antagonistic activity. However, 19 showed only weak gastrointestinal prokinetic activity after oral administration. Several ester prodrugs(44-62)of 19 were tested for pharmacological activities as well as physicochemical and metabolic stability ; the butyl ester(46)was consequently selected as a promising gastrointestinal prokinetic agent with reduced side effects.
- 公益社団法人日本薬学会の論文
- 2001-04-01
著者
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斎藤 徹
Faculty Of Pharmaceutical Sciences Kanazawa University
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花岡 美代次
金沢大学薬学部
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HANAOKA Miyoji
Faculty of Pharmaceutical Sciences, Kanazawa University
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Suzuki T
Drug Discovery Research Laboratory Sanwa Kagaku Kenkyusho Co. Ltd.
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Sakaguchi J
Research Division Hokuriku Seiyaku Co. Ltd.
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Hanaoka Miyoji
Faculty Of Pharmaceutical Sciences Kanazawa University
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Kato H
Research And Development Headquarters Hokurikit Seiyaku Co. Ltd.
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Suzuki T
Laboratory Of Biopharmaceutics Faculty Of Pharmaceutical Sciences Chiba University
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KATO Hideo
Research and Development Division, Hokuriku Seiyaku Co., Ltd.,
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SAITO Takaharu
Research and Development Headquarters, Hokurikit Seiyaku, Co., Ltd.
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IWANAGA Yuji
Research and Development Headquarters, Hokurikit Seiyaku, Co., Ltd.
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SAKAGUCHI Jun
Research Division, Hokuriku Seiyaku Co., Ltd.
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IWASAKI Nobuhiko
Research Division, Hokuriku Seiyaku Co., Ltd.
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TAKAHARA Eiji
Research Division, Hokuriku Seiyaku Co., Ltd.
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Saito T
Research And Development Headquarters Hokurikit Seiyaku Co. Ltd.
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Saito Takako
Research And Development Laboratories Maruho Co. Ltd.
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Suzuki Toshikazu
Discovery Research Laboratory Tanabe Seiyaku Co. Ltd.
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Kato Hideo
Research And Development Division Hokuriku Seiyaku Co. Ltd.
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Kato Hideo
Nihon Bioresearch Inc.
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Iwanaga Y
Research And Development Headquarters Hokurikit Seiyaku Co. Ltd.
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Takahara E
Research Division Hokuriku Seiyaku Co. Ltd.
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Takahara Eiji
Research Division Hokuriku Seiyaku Co. Ltd.
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Iwasaki N
Research And Development Division Hokuriku Seiyaku Co. Ltd.
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Suzuki T
Research Unit Of Pharmaceutics College Of Pharmacy Nihon University
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Sugihara T
Faculty Of Pharmaceutical Sciences Tokushima Bunri University
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Saito T
Research And Development Laboratories Maruho Co. Ltd.
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Hattori Masao
Metabolic Engineering Institute Of Natural Medicine University Of Toyama
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Iwanaga Yuji
Research And Development Headquarters Hokurikit Seiyaku Co. Ltd.
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Kato Hideo
Yamaguchi Univ. Yamaguchi Jpn
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花岡 美代次
Institute Of Natural Medicine University Of Toyama
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Iwasaki Nobuhiko
Research and Development Division, Hokuriku Seiyaku Co., Ltd.
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Iwanaga Yuji
Research and Development Division, Hokuriku Seiyaku, Co., Ltd.
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