Neuropharmacological activity of newly-synthesized derivatives of 3,3-diethyl-2,4-pyridinedione. V. Relation between chemical structure and pharmacological activity
Belcheva, I.; Stoytchev, T.
Acta Physiologica et Pharmacologica Bulgarica 9(4): 37-47
1983
ISSN/ISBN: 0323-9950 PMID: 6677062 Document Number: 211880
On the basis of neuropharmacological screening of newly-synthesized derivatives of 3,3-diethyl-2,4-pyridinedione (Pyrithylidione) 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-aminomethyl, 5-acyloxymethyl and 5-aminomethyl. The derivatives tested were biologically active substances with central depressant action differing from that of pyridinedione. 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 (LD50).