Synthesis of Phenoxyacetic Acid Derivatives as Highly Potent Antagonists of Gastrin/Cholecystokinin-B Receptors. III
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概要
- 論文の詳細を見る
In order to improve the biological characteristics of DA-3934 (5), a novel gastrin/cholecystokinin (CCK)-B receptor antagonist, phenoxyacetic acid derivatives replacing the N-methyl-N-phenylcarbamoylmethyl moiety of 5 with various alkyl chains have been synthesized and their biological activity evaluated. The relationship between the structure of these compounds and their human gastrin receptor binding affinity showed that there should be the optimal size among the various N-alkyl chains. Also a significant increase in the receptor binding affinity was achieved by several compounds. Among those compounds, 2-[3-[3-[N-cyclohexylmethyl-N-[2-(N-methyl-N-phenylcarbamoylmethoxy)phenyl]carbamoylmethyl]ureido]phenyl]acetic acid (22c) and (±)-2-[3-[3-[N-[2-(N-methyl-N-phenylcarbamoylmethoxy)phenyl]-N-(3-methylpentyl)carbamoylmethyl]ureido]phenyl]acetic acid (22h) exhibitted high affinity for human gastrin receptors and were also more potent inhibitors in a penta-gastrin-induced gastric acid secretion model than the parent compound, 5. The ED_<50> values of these compounds when adiministered intraduodenally to rats were 0.12 and 0.63 mg/kg, respectively.
- 公益社団法人日本薬学会の論文
- 1999-06-15
著者
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高石 喜久
徳島大院薬
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Takeda Y
Fac. Of Integrated Arts And Sciences Univ. Of Tokushima
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Takeda Y
Faculty Of Integrated Arts And Sciences The University Of Tokushima
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Honda Y
Kumamoto Univ. Kumamoto Jpn
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Honda Yuko
Institute For Solid State Physics The University Of Tokyo
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Honda Yuko
Dept. Biol. Sci. Ehime Univ.
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Ogihara Y
Nihon Pharmaceutical University
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Ogihara Yukio
Laboratory Of Pharmacognosy Graduate School Of Pharmaceutical Sciences Nagoya City University
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Ogihara Yukio
Faculty Of Pharmacy Meijo Universitv
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Ogihara Yukio
Graduate School Of Pharmaceutical Sciences Nagoya City University
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TABUCHI Yoshiaki
New Product Research Laboratories III Daiichi Pharmaceutical Co., Ltd.
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細上 徹
第一製薬株式会社 (東京研究開発センター) 探索第三研究所
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細上 徹
Exploratory Research Laboratories Iii Daiichi Pharmaceutical Co. Ltd.
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下東 義正
Exploratory Research Laboratories Iii Daiichi Pharmaceutical Co. Ltd.
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下東 義正
New Product Research Laboratories Iii Daiichi Pharmaceutical Co. Ltd.
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TAKEDA Yasuyuki
New Product Research Laboratories III, Daiichi Pharmaceutical Co., Ltd.,
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KAWAGOE Keiichi
New Product Research Laboratories III, Daiichi Pharmaceutical Co., Ltd.,
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YOKOMIZO Aki
New Product Research Laboratories III, Daiichi Pharmaceutical Co., Ltd.,
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YOKOMIZO Yoshihiro
New Product Research Laboratories III, Daiichi Pharmaceutical Co., Ltd.,
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HOSOKAMI Toru
New Product Research Laboratories III, Daiichi Pharmaceutical Co., Ltd.,
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SHIMOTO Yoshimasa
New Product Research Laboratories III, Daiichi Pharmaceutical Co., Ltd.,
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OGIHARA Yoshiyasu
New Product Research Laboratories III, Daiichi Pharmaceutical Co., Ltd.,
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HONDA Yuko
New Product Research Laboratories III, Daiichi Pharmaceutical Co., Ltd.,
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KAWARABAYASHI Keiko
New Product Research Laboratories III, Daiichi Pharmaceutical Co., Ltd.,
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ISERI Miki
New Product Research Laboratories III, Daiichi Pharmaceutical Co., Ltd.,
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YOKOHAMA Shuichi
New Product Research Laboratories III, Daiichi Pharmaceutical Co., Ltd.,
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Tabuchi Y
Second Department Of Surgery Graduate School Of Medicine And Pharmaceutical Sciences University Of T
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Tabuchi Yoshiaki
New Product Research Laboratories Iii Daiichi Pharmaceutical Co. Ltd.
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Yokomizo Yoshihiro
New Product Research Laboratories Iii Daiichi Pharmaceutical Co. Ltd.
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Kawarabayashi Keiko
New Product Research Laboratories Iii Daiichi Pharmaceutical Co. Ltd.
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Iseri Miki
New Product Research Laboratories Iii Daiichi Pharmaceutical Co. Ltd.
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Yokomizo Aki
New Product Research Laboratories Iii Daiichi Pharmaceutical Co. Ltd.
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細上 徹
New Product Research Laboratories Iii Daiichi Pharmaceutical Co. Ltd.
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Kawada K
New Product Research Laboratories Iii Daiichi Pharmaceutical Co. Ltd.
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Yokohama S
New Product Research Laboratories Iii Daiichi Pharmaceutical Co. Ltd.
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