Evaluation of some 2-substituted derivatives of xanthone for anticonvulsant properties.
A series of alkanolamides and alkanoamines derivatives of xanthone were prepared and evaluated for antiepileptic activity in the maximal electroshock seizure (MES) and subcutaneous pentylenetetrazol seizure threshold (ScMet) assays and for neurotoxicity (TOX). Several analogues from the appropriate alkanolamines were found to be active in both the anticonvulsant tests. Most interesting were the anticonvulsant results of the appropriate 2-amino- or 2-N-methylamino-1-butanol derivatives of 7-chloroxanthone 8-11, which displayed anti-MES activity with a protective index (TD50/ED50) in the range 2.84-3.62 for 8-11 corresponding with that for phenytoin, carbamazepine and valproate.
Marona
H
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Department of Chemical Technology of Drugs, Collegium Medicum of the Jagiellonian University, Kraków, Poland.
D000818:Animals; D000927:Anticonvulsants / Q000138:chemical synthesis* / Q000494:pharmacology*; D002855:Chromatography, Thin Layer; D003292:Convulsants / Q000037:antagonists & inhibitors; D004597:Electroshock; D007274:Injections, Intraperitoneal; D008297:Male; D051379:Mice; D010433:Pentylenetetrazole / Q000037:antagonists & inhibitors; D051381:Rats; D017207:Rats, Sprague-Dawley; D012640:Seizures / Q000139:chemically induced / Q000517:prevention & control; D014970:Xanthines / Q000138:chemical synthesis* / Q000494:pharmacology*
D000927:Anticonvulsants; D003292:Convulsants; D014970:Xanthines; D010433:Pentylenetetrazole