[Preparation and anticonvulsant activity of new potential beta-adrenoreceptor blockers]

Within the framework of a structure-effect relationships study in a group of new beta-adrenoreceptor blockers, a series of new derivatives derived from p-hydroxyacetophenone with modifications in the basic moiety of the side chain was prepared. The initial p-hydroxyacetophenone prepared by Fries rearrangement of phenylacetate in a reaction with 2-(chloromethyl)oxirane yields 1-[4-(2-oxiranylmetoxy)phenyl]-1-etanone, which combines with the appropriate amines to produce final substances. They were isolated either in the form of free bases, or salts with fumaric acid. Their structure was confirmed by interpretations of the IR, 1H-NMR and 13C-NMR-spectra. Within the framework of pharmacological evaluation of the prepared agents, the anticonvulsive effect as a protective effect against pentetrazole spasms was examined. The results of the evaluation were compared with the values of their distribution coefficients.