Synthesis and Pharmacological Evaluation of New 1-Hydroxy-1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepines as Norepinephrine Potentiators
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概要
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4-Hydroxy-2-methyl-4-phenyl-1,2,3,4-tetrahydroisoquinoline (PI-OH) (1a) and its derivatives form a new class of compounds which possess norepinephrine (NE) potentiating activity. As a new series of compounds, 1-hydroxy-1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepines (2a—f) were synthesized by the intramolecular Barbier reaction of N-[2-(2-iodophenyl)ethyl]phenacylamines (6a—f) with n-BuLi as a key reaction step. The potentiating activities of the benzazepines 2a—f on the contraction of rat anococcygeus muscle induced by NE were tested. Among the compounds tested in this study, compound 2a showed moderate potentiating activity (the activity ratio was 7.3-fold at 3×10−5 M).
著者
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Yamauchi Aiko
Faculty Of Pharmaceutical Sciences Kobe-gakuin University
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Kihara Masaru
Faculty Of Pharmaceutical Sciences The University Of Tokushima:faculty Of Home Economics Shikoku Wom
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IKEUCHI Motoki
Faculty of Pharmaceutical Sciences, The University of Tokushima
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Ikeuchi Miyuki
Faculty of Pharmaceutical Sciences, The University of Tokushima
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Ikuta Masako
Faculty of Pharmaceutical Sciences, The University of Tokushima
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Hariki Miyuki
Faculty of Pharmaceutical Sciences, The University of Tokushima
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Maruyama Shigeki
Faculty of Pharmaceutical Sciences, The University of Tokushima
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Nakase Mari
Faculty of Pharmaceutical Sciences, The University of Tokushima
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Sakamoto Kumiko
Faculty of Pharmaceutical Sciences, The University of Tokushima
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Yoshioka Yasuko
Faculty of Pharmaceutical Sciences, The University of Tokushima
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Yamauchi Aiko
Faculty of Pharmaceutical Sciences, The University of Tokushima
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Kihara Masaru
Faculty of Pharmaceutical Sciences, The University of Tokushima
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