Synthesis and Biological Activities of Optical Isomers of 2-(4-Diphenylmethyl-1-piperazinyl)ethyl Methyl 1,4-Dihydro-2,6-dimethyl-4-(3-nitrophenyl)-3,5-pyridinedicarboxylate (Manidipine) Dihydrochloride
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- 梶野 正博
- Central Research Division, Takeda Chemical Industries, Ltd.,
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- 和田 喜一
- Central Research Division, Takeda Chemical Industries, Ltd.,
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- 永井 康雄
- Central Research Division, Takeda Chemical Industries, Ltd.,
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- 永岡 明伸
- Central Research Division, Takeda Chemical Industries, Ltd.,
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- 目黒 寛司
- Central Research Division, Takeda Chemical Industries, Ltd.,
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説明
Enantiomeric (+)- and (-)-manidipine (1) dihydrochlorides were synthesized by the esterification of the optically active monocarboxylic acids (-)-6 and (+)-6,respectively. The absolute configurations, (S)-(+)-1 and (R)-(-)-1,were unambiguously determined by X-ray crystallographic analysis of (+)-7 derived from (-)-6. The (S)-(+)-1 was about 30 and 80 times as potent as the (R)-(-)-isomer in antihypertensive activity in spontaneously hypertensive rats (SHR), and in the radioligand binding assay using [^3H]nitrendipine, respectively.
収録刊行物
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- Chem. Pharm. Bull.
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Chem. Pharm. Bull. 37 2225-2228, 1989
公益社団法人日本薬学会
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詳細情報 詳細情報について
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- CRID
- 1570854177484898048
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- NII論文ID
- 110003627962
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- NII書誌ID
- AA00602100
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- ISSN
- 00092363
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- 本文言語コード
- en
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- データソース種別
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- CiNii Articles