Novel Potassium Channel Activators : Synthesis and Structure-Activity Relationship Studies of 3,4-Dihydro-2H-1,4-benzoxazine Derivatives
スポンサーリンク
概要
- 論文の詳細を見る
Strong potassium channel-activating effects were found among a series of novel 4-substituted 3,4-dihydro-2H-1,4-benzoxazine derivatives. The key step in preparation was the nucleophilic substitution of 3,4-dihydro-2H-1,4-benzoxazine (3) with activated halogenopyridines, such as halogenopyridine N-oxides (15a-c) and the borane adduct (15d) of 4-bromopyridine. Structure-activity relationship studies identified 2-(3,4-dihydro-2,2-dimethyl-6-nitro-2H-1,4-benzoxazin-4-yl)pyridine-1-oxide (16a : YM934) as the optimal compound. This compound (16a) showed a more potent oral antihypertensive effect than cromakalim in conscious spontaneously hypertensive rats.
- 1996-01-15
著者
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FUJITA SHIGEO
Institute for Drug Discovery Research, Yamanouchi Pharmaceutical Co., Ltd.
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松本 宜明
日本大学薬学部臨床薬物動態学ユニット
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UCHIDA Wataru
Institute for Drug Discovery Research, Yamanouchi Pharmaceutical Co., Ltd.
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Fujita Shigeo
Institute For Drug Discovery Research Yamanouchi Pharmaceutical Co. Ltd.
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Uchida W
Yamanouchi Pharmaceutical Co. Ltd. Ibaraki Jpn
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Uchida Wataru
Institute For Drug Discovery Research Yamanouchi Pharmaceutical Co. Ltd.
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増田 明
富山医科薬科大学麻酔科
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Yanagisawa I
Yamanouchi Pharmaceutical Co. Ltd. Ibaraki Jpn
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Yanagisawa Isao
Institute For Drug Discovery Research Yamanouchi Pharmaceutical Co.
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Yanagisawa Isao
山之内製薬
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MATSUHISA Akira
Institute for Drug Discovery Research, Yamanouchi Pharmaceutical Co., Ltd.
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Matsuhisa Akira
Institute For Drug Discovery Research Yamanouchi Pharmaceutical Co. Ltd.
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Matsuhisa Akira
Gastrointestinal Research Laboratories Institute For Drug Discovery Research Yamanouchi Pharmaceutic
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Matsumoto Yoshiaki
Department Of Pharmaceutics Showa College Of Pharmaceutical Sciences
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松本 宣明
Division Of Applied Life Science Graduate School Of Engineering Sojo University
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TSUZUKI Ryuji
Institute for Drug Discovery Research, Yamanouchi Pharmaceutical Co., Ltd.
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Yoden Toru
Institute For Drug Discovery Research Yamanouchi Pharmaceutical Co. Ltd.
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Tsuzuki R
Institute For Drug Discovery Research Yamanouchi Pharmaceutical Co. Ltd.
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Tsuzuki Ryuji
Institute For Drug Discovery Research Yamanouchi Pharmaceutical Co. Ltd.
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Matsumoto Yuzo
Institute For Drug Discovery Research Yamanouchi Pharmaceutical Co.ltd.
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TAKAYAMA Kazuhisa
Institute for Drug Discovery Reserch, Yamanouchi Pharmaceutical Co., Ltd.
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FUJIKURA Takashi
Institute for Drug Discovery Research, Yamanouchi Pharmaceutical Co., Ltd.,
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ASANO Masaharu
Institute for Drug Discovery Research, Yamanouchi Pharmaceutical Co., Ltd.,
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Asano Masaharu
Institute For Drug Discovery Research Yamanouchi Pharmaceutical Co. Ltd.
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Takayama Kazuhisa
Institute For Drug Discovery Research Yamanouchi Pharmaceutical Co. Ltd.
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Fujita S
Institute For Drug Discovery Research Yamanouchi Pharmaceutical Co. Ltd.
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Fujikura T
Institute For Drug Discovery Research Yamanouchi Pharmaceutical Co. Ltd.
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Fujikura Takashi
Institute For Drug Discovery Research Yamanouchi Pharmaceutical Co. Ltd.
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Matsumoto Y
Hoshi Univ. Tokyo Jpn
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Matsuhisa Akira
Institute For Drug Discovery Research Astellas Pharma Inc.
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