Neuropharmacological activity of newly-synthesized derivatives of 3,3-diethyl-2,4-pyridinedione. V. Relation between chemical structure and pharmacological activity.

On the basis of neuropharmacological screening of newly-synthesized derivatives of 3,3-diethyl-2,4-pyridinedione ( Pyrithyldion ) some regularities are pointed out, related to the link between the chemical structure and the pharmacological activity of the pyridinedione derivatives. The following groups of compounds were studied: N-acyl, N-alkyl, N-amino-methyl, 5- acyloxymethyl and 5-aminomethyl. The derivatives tested were found to be biologically active substances with central depressant action differing from that of pyridinedione. Most generally, it may be stated that substitution of the pyridinedione nucleus with N-alkyl and 5-aminomethyl radicals results in compounds with analgesic action without soporific effect, while substitution with N-aminomethyl radicals leads to compounds with marked anticonvulsive activity and manifestation of soporific effect in high doses (1/2 of the lethal doses).