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一些N-二苯甲基哌嗪衍生物作为钙拮抗剂的合成

Synthesis of some N-benzhydrylpiperazine derivatives as calcium antagonists.

作者信息

Gubert S, Brasó M A, Sacristán A, Ortiz J A

机构信息

Centro de Investigación, Grupo Ferrer, Barcelona, Spain.

出版信息

Arzneimittelforschung. 1987 Oct;37(10):1103-7.

PMID:3435581
Abstract

The preparation of a series of 24 N-benzhydrylpiperazine derivatives is described. Their efficacy as calcium antagonists was examined with reference to changes in the permeability of the cell membrane to extracellular and intracellular calcium. Compounds 14, 15, 17 and 19 were the most powerful when compared with known calcium antagonists such as cinnarizine, flunarizine, and aligeron ([1-diphenylmethyl)-4-(2-propenyl)]-piperazine), and were selected for further study.

摘要

本文描述了一系列24种N - 二苯甲基哌嗪衍生物的制备方法。参照细胞膜对细胞外和细胞内钙通透性的变化,研究了它们作为钙拮抗剂的功效。与桂利嗪、氟桂利嗪和阿立吉仑([1 - 二苯甲基)- 4 -(2 - 丙烯基)] - 哌嗪)等已知钙拮抗剂相比,化合物14、15、17和19活性最强,并被选作进一步研究。

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