Assuntos
Acetofenonas/síntese química , Antagonistas Adrenérgicos beta/síntese química , Acetofenonas/farmacologia , Acetofenonas/toxicidade , Antagonistas Adrenérgicos beta/farmacologia , Antagonistas Adrenérgicos beta/toxicidade , Animais , Antiarrítmicos/síntese química , Antiarrítmicos/farmacologia , Arritmias Cardíacas/induzido quimicamente , Arritmias Cardíacas/tratamento farmacológico , Fenômenos Químicos , Físico-Química , Epinefrina , Cobaias , Técnicas In Vitro , Isoproterenol/antagonistas & inibidores , Dose Letal Mediana , Camundongos , RatosRESUMO
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.