Synthesis and Antihypertensive Activities of 1,4-Dihydropyridine-5-phosphonate Derivatives. II(Medicinal Chemistry,Chemical)

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概要

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• A series of 1,4-dihydropyridine-5-cyclic phosphonate derivatives, designed as analogues of 1,4-dihydropyridine-3,5-dicarboxylate calcium antagonists, was synthesized and examined for antihypertensive activity. Several compounds were proved to have activities superior or comparable to that of nifedipine in lowering blood pressure in normotensive and spontaneously hypertensive rats (SHR). Among these compounds, methyl 2,6-dimethyl-5-(2-oxo-1,3,2-dioxaphosphorinan-2-yl)-4(2-nitrophenyl)-1,4-dihydropyridine-3-carboxylate (31, DHP-218) was approximately 7 times more active than nifedipine in SHR and was selected for further development and clinical evaluation. The structure-activity relationships are discussed.

• 公益社団法人日本薬学会の論文
• 1987-10-25

著者

• 黄瀬 正博

  Research Laboratories, Nippon Shinyaku Co., Ltd.

• 木村 喜代史

  Research Laboratories Nippon Shinyaku Co. Ltd.

• 黄瀬 正博

  Nippon Shinyaku Company, Ltd.,

• 但田 信一

  Research Laboratories, Nippon Shinyaku Co., Ltd.

• 黄瀬 正博

  Nippon Shinyaku Company Ltd.

• 但田 信一

  日本新薬

• 森田 岩男

  Research Laboratories, Nippon Shinyaku Co., Ltd.

• 黄瀬 正博

  Research Center Sumitomo Pharmaceuticals Co. Ltd

• 国本 克俊

  Research Laboratories, Nippon Shinyaku Co., Ltd.

• 津田 正己

  Research Laboratories, Nippon Shinyaku Co., Ltd.

• 森田 岩男

  Research Laboratories Nippon Shinyaku Co. Ltd.

• 津田 正己

  Research Laboratories Nippon Shinyaku Co. Ltd.

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