[The search for new anticonvulsant agents based on nicotinamide].
The electron structural analogs nicomorpholine and azethylnicotinate possessing a high anticonvulsant activity in experiment were synthesized on the basis of nicotinamide. The new substances antagonized the convulsant effect of corasole in the doses less by a factor of 10 than nicotinamide, with the therapeutic protective index of the test agents being 3-4 times higher than that of nicotinamide and being equal to the index of phenobarbital and diazepam. Analysis of the anticonvulsive activity with the aid of pro- and anticonvulsants disclosed that nicotinamide and its analogs are more effective in relation to bikukullin, thiosemicarbazide and picrotoxin than to corasole. Nicomorpholine like nicotinamide is capable of suppressing the epileptic foci in various zones of the cerebral cortex. The data obtained evidence that the spectrum of the activity of nicotinamide and its analogs differ from that of the classic anticonvulsants and antiepileptic drugs of the diphenin and phenobarbital series, resembling, to a greater degree, benzodiazepine tranquilizers with the predominant influence on the GABA-ergic system.
Akhundov
R A
RA
Dzhafarova
S A
SA
Aliev
A N
AN
D000818:Animals; D000927:Anticonvulsants / Q000627:therapeutic use*; D002415:Cats; D004353:Drug Evaluation, Preclinical; D004569:Electroencephalography / Q000187:drug effects; D004827:Epilepsy / Q000139:chemically induced / Q000517:prevention & control; D008297:Male; D051379:Mice; D009536:Niacinamide / Q000031:analogs & derivatives* / Q000627:therapeutic use*; D012640:Seizures / Q000139:chemically induced / Q000517:prevention & control; D013329:Structure-Activity Relationship
D000927:Anticonvulsants; D009536:Niacinamide
Izyskanie novykh protivosudorozhnykh sredstv na osnove nikotinamida.