Syntheses and Biological Activities of Renin Inhibitors Containign Statine Analogues
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概要
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Syntheses and biological activities of dipeptide renin inhibitors that contain statine analogues are described. The key steps fo the synthetic approach to dipeptide renin inhibitors are the asymmetric synthesls of 2(R)-substituted-3-aminocarbonylpropionic acids and the diastereoselective syntheses of (3S, 4S)-statine analogues. These inhibitors (2,14-40) inhibited human renin in the 3-140 nM range. Inhibitor ES 6864 (2) was found to be a highly potent inhibitor of human renin (IC_<50> : 4.6×10^<-9>M) and showed high enzyme specificity. Oral administration of ES 6864 at 3 mg/kg to conscious, sodium-depleted marmosets inhibted plasma renin activity (PRA) more than 80% after 1h.
- 社団法人日本薬学会の論文
- 1990-01-25
著者
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小池 博之
Sankyo Biological Research Laboratories Sankyo Co. Ltd.
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桜井 満也
Exploratory Chemistry Research, Sankyo Co., Ltd.,
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東田 勧
Exploratory Chemistry Research, Sankyo Co., Ltd.,
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桜井 満也
New Lead Research, Sankyo Co., Ltd.,
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東田 勧
New Lead Research, Sankyo Co., Ltd.,
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西 剛秀
Medicinal Chemistry Research, Sankyo Co., Ltd.,
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斉藤 冨士夫
Medicinal Chemistry Research, Sankyo Co., Ltd.,
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矢部 裕一郎
New Lead Research, Sankyo Co., Ltd.,
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桜井 満也
Exploratory Chemistry Research Sankyo Co. Ltd.
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永堀 均
Medicinal Chamistry Reseaerch
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片岡 満
Medicinal Chemistry Research
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森沢 靖弘
Medicinal Chemistry Research
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庄子 真知子
New Lead Research
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松下 洋一
New Lead Research
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飯島 康輝
New Lead Research
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大泉 喜代志
Biological Research
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小池 博之
Biological Research
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片岡 満
三共・中央研
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片岡 満
Medicinal Chemistry Research:laboratories Sankyo Co. Ltd.
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松下 洋一
三共研究開発セ
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飯島 康輝
三共研究開発セ
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大泉 喜代志
Sankyo Biological Research Laboratories, Sankyo Co., Ltd.
-
斉藤 冨士夫
Medicinal Chemistry Research Sankyo Co. Ltd.
-
東田 勧
Exploratory Chemistry Research Sankyo Co. Ltd.
-
森沢 靖弘
Medicinal Chemistry Research:laboratories Sankyo Co. Ltd.
-
矢部 裕一郎
Exploratory Chemistry Research Sankyo Co. Ltd.
-
大泉 喜代志
Sankyo Biological Research Laboratories Sankyo Co. Ltd.
-
西 剛秀
三共(株)化学研究所
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庄子 真知子
New Lead Research:laboratories Sankyo Co. Ltd.
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永堀 均
Medicinal Chamistry Reseaerch:laboratories Sankyo Co. Ltd.
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