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3-位和5-位含硝氧基烷基酯部分的新型1,4-二氢吡啶衍生物的合成及降压活性

Synthesis and antihypertensive activities of new 1,4-dihydropyridine derivatives containing nitrooxyalkylester moieties at the 3- and 5-positions.

作者信息

Ogawa T, Nakazato A, Tsuchida K, Hatayama K

机构信息

Research Center, Taisho Pharmaceutical Co., Ltd., Saitama, Japan.

出版信息

Chem Pharm Bull (Tokyo). 1993 Jun;41(6):1049-54. doi: 10.1248/cpb.41.1049.

Abstract

We have synthesized new 1,4-dihydropyridine derivatives having nitrooxyalkylester moieties at the 3- and 5-positions in order to develop potent and long-lasting vasodilators. The antihypertensive activities of these compounds were compared with that of nifedipine. One of them, 2-nitrooxypropyl 3-nitrooxypropyl 2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydro-3,5- pyridinedicarboxylate (CD-349) was selected for further development. The structure-activity relationship is discussed.

摘要

为了开发强效且长效的血管舒张剂,我们合成了在3位和5位带有硝氧基烷基酯部分的新型1,4 - 二氢吡啶衍生物。将这些化合物的抗高血压活性与硝苯地平的抗高血压活性进行了比较。其中之一,2 - 硝氧基丙基3 - 硝氧基丙基2,6 - 二甲基 - 4 - (3 - 硝基苯基)-1,4 - 二氢 - 3,5 - 吡啶二羧酸酯(CD - 349)被选用于进一步研发。讨论了构效关系。

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