Synthesis of 1,4-Dihydropyridine-5-phosphonates and Their Calcium-Antagonistic and Antihypertensive Activities : Novel Calcium-Autagonist 2-[Benzy(phenyl)amino]ethyl 5-(5,5-Dimethyl-2-oxo-1,3,2-dioxaphosphorinan-2-yl)-1,4-dihydro-2,6-dimethyl-4-(3-nitroph

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概要

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• The effect of the 3-carboxylic-ester variation in 2,2-dimethyltrimethylene 3-alkoxycarbonyl-4-aryl-1,4-dihydro-2,6-dimethyl-5-pyridinephosphonates (1) was investigated with relation to the calcium-antagonistic and antihypertensive activities : the analogs contaning the alkyl groups of not more than 12 carbons and an amino functionality in the carboxylic-ester moiety were synthesized to be examined for biological activities. Among them, 2-[benzyl(phenyl)amino]-ethyl 5(5,5-dimethyl-2-oxo-1,3,2-dioxaphosphorinan-2-yl)-1,4-dihydro-2,6-dimethyl-4-(3-nitrophenyl)-3-phridine-carboxylate hydrochloride ethanol (NZ-105) showed particularly beneficial activities and was selected for further pharmacological studies and clinical development. Some aspects of the structure-activity relationships and solid-state structure of NZ-105 by X-ray crystallographic analysis were described.

• 1992-09-25

著者

• 瀬戸 淨智

  Central Research Institute Nissan Chemical Ind. Co. Ltd.

• 迫田 良三

  Central Research Institute, Nissan Chemical Ind. Ltd.

• 上川路 益昌

  Central Research Institute, Nissan Chemical Ind.Co., Ltd.

• 迫田 良三

  Central Research Institute Nissan Chemical Industries Ltd.

• 上川路 益昌

  Central Research Institute Nissan Chemical Industries Ltd.

• Sakoda R

  Central Research Institute Nissan Chemical Industries Ltd.

関連論文

• Transformation of 1,4-Dihydropyridine Ring of Calcium Antagonist NZ-105 into Cyclohexenone Ring
• Sythesis and Crystal Structure of Optically Active 2-[Benzyl(phenyl)amino]ethyl 5-(5,5-Dimethyl-2-oxo-1,3,2-dioxaphosphorinan-2-yl)-1,4-dihydro-2,6-dimethyl-4-(3-nitrophenyl)-3-pyridinecarboxylate (NZ-105)
• Synthesis and Biological Activities of Optical Isomers of 2-(4-Diphenylmethyl-1-piperazinyl)ethyl 5-(4,6-Dimethyl-2-oxo-1,3,2-dioxaphosphorinan-2-yl)-1,4-dihydro-2,6-dimethyl-4-(3-nitrophenyl)-3-pyridinecarboxylate Dihydrochloride (NIP-101)
• Synthesis of 1,4-Dihydropyridine-5-phosphonates and Their Calcium-Antagonistic and Antihypertensive Activities : Novel Calcium-Autagonist 2-[Benzy(phenyl)amino]ethyl 5-(5,5-Dimethyl-2-oxo-1,3,2-dioxaphosphorinan-2-yl)-1,4-dihydro-2,6-dimethyl-4-(3-nitroph

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