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寻找新型钙离子拮抗剂。亲脂性肟类和膦酸酯类。

Search for new Ca++ antagonists. Lipophilic oximes and phosphonates.

作者信息

Bellucci C, Teodori E, Gualtieri F, Piacenza G

出版信息

Farmaco Sci. 1985 Oct;40(10):730-44.

PMID:3002848
Abstract

On the basis of the reported slow channel-inhibiting activity of oximes and phosphonates a series of compounds bearing such functions on lipophilic carriers were synthesized and studied. Among the compounds studied only (VI b) shows a slight cardiovascular activity. The surprising lack of activity of diethyl 3,4-dimethoxybenzyl-phosphonate (XIV), which is closely related to Fostedil, is discussed.

摘要

基于肟类化合物和膦酸酯类化合物具有报道的慢通道抑制活性,合成并研究了一系列在亲脂性载体上带有此类官能团的化合物。在所研究的化合物中,只有(VI b)表现出轻微的心血管活性。讨论了与福司地尔密切相关的3,4-二甲氧基苄基膦酸二乙酯(XIV)令人惊讶的无活性情况。

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