[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.
Cizmáriková
R
R
Katedra anorganickej a organickej chémie, Farmaceutickej fakulty, Univerzity Komenského, Bratislava.
Dingová
A
A
Kozlovský
J
J
Greksáková
O
O
D000098:Acetophenones / Q000494:pharmacology* / Q000633:toxicity; D000319:Adrenergic beta-Antagonists; D000818:Animals; D001145:Arrhythmias, Cardiac / Q000139:chemically induced / Q000188:drug therapy / Q000503:physiopathology; D003864:Depression, Chemical; D006168:Guinea Pigs; D006339:Heart Rate / Q000187:drug effects; D006910:Hydroxypropiophenone / Q000494:pharmacology* / Q000633:toxicity; D051379:Mice; D009200:Myocardial Contraction / Q000187:drug effects
D000098:Acetophenones; D000319:Adrenergic beta-Antagonists; D006910:Hydroxypropiophenone; C069170:4-hydroxypropiophenone; C031335:4-hydroxyacetophenone