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Cesk Farm ; 39(9): 403-8, 1990 Nov.
Artigo em Eslovaco | MEDLINE | ID: mdl-1982858

RESUMO

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.


Assuntos
Acetofenonas/farmacologia , Antagonistas Adrenérgicos beta , Hidroxipropiofenona/farmacologia , Acetofenonas/toxicidade , Animais , Arritmias Cardíacas/induzido quimicamente , Arritmias Cardíacas/tratamento farmacológico , Arritmias Cardíacas/fisiopatologia , Depressão Química , Cobaias , Frequência Cardíaca/efeitos dos fármacos , Hidroxipropiofenona/toxicidade , Camundongos , Contração Miocárdica/efeitos dos fármacos
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