[对羟基苯乙酮和对羟基丙烯酮的衍生物作为一种潜在的新型β -肾上腺溶解剂]。

Ceskoslovenska farmacie Pub Date : 1990-11-01
R Cizmáriková, A Dingová, J Kozlovský, O Greksáková
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引用次数: 0

摘要

在结构-效应关系研究的框架内,以对羟基苯乙酮和对羟基丙烯酮为原料,在分子亲脂部分有alyloxy甲基和cycloalkyloxy甲基,在碱性氮上亲水部分有异丙基和叔丁基,通过一种经过验证的方法制备了一系列新型的β -肾上腺素潜在解药。通过IR、UV、1H-NMR和质谱分析,确定了药物的结构。所选药物的药理学评价结果表明,这些药物具有β -肾上腺素溶解和抗心律失常活性。从被测试的单个药物的比较的观点来看,芳烯的存在似乎比环己基的存在更有利。通过分配系数、表面张力和急性毒性的测定来补充所制备药物的特性。
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[Derivatives of para-hydroxyacetophenone and para-hydroxypropiophenone as a potential new beta-adrenolytic agent].

Within the framework of the study of the structure-effect relationship, a series of novel potential beta-adrenolytic agents derived from p-hydroxyacetophenone and p-hydroxypropiophenone with an alyloxymethyl and a cycloalkyloxymethyl group in the lipophilic part of the molecule and an isopropyl and a tert-butyl group in the hydrophilic part on the basic nitrogen were prepared by means of a well-tried method. The structure of the prepared drugs was confirmed on the basis of interpretation of the IR, UV, 1H-NMR and mass spectra. The results of pharmacological evaluation of selected drugs show that the agents poses beta-adrenolytic and antiarrhythmic activity. From the viewpoint of comparison of the individual drugs subjected to testing the presence of an alyl seems more advantageous than that of a cyclohexyl. The characteristic of the prepared drugs was supplemented by the determination of their partition coefficients, surface tension and acute toxicity.

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