Preliminary evaluation of anticonvulsant activity of some aroxyacetamides and aroxyethylamines.
A series of aroxyacetamides and aroxyethylamines were prepared and evaluated for anticonvulsant activity in the maximal electroshock seizure (MES) and subcutaneous pentylenetetrazole seizure threshold (ScMet) assays and for neurotoxicity (TOX). Most of them exhibited anticonvulsant activity in the MES screen (mice, i.p.) in the doses up to 300 mg/kg b.w. The most active compound was XVI, which given in the dose 100 mg/kg b.w. produced 100% anticonvulsant protection after 0.5 h without neurotoxicity. The most promising compound in the VIa phase (rats, p.o.) was VIII, which produced higher anticonvulsant protection (to 75% at 0.5 h).
Marona
Henryk
H
Department of Technology and Biotechnology of Drugs, Medical College, Jagiellonian University, 9 Medyczna Str., 30-688 Kraków, Poland.
Waszkielewicz
Anna M
AM
Szneler
Edward
E
D000081:Acetamides / Q000138:chemical synthesis* / Q000494:pharmacology*; D000818:Animals; D000927:Anticonvulsants / Q000138:chemical synthesis* / Q000494:pharmacology*; D003292:Convulsants; D004597:Electroshock; D005021:Ethylamines / Q000138:chemical synthesis* / Q000494:pharmacology*; D051379:Mice; D010433:Pentylenetetrazole; D012640:Seizures / Q000139:chemically induced / Q000209:etiology / Q000517:prevention & control
D000081:Acetamides; D000927:Anticonvulsants; D003292:Convulsants; D005021:Ethylamines; D010433:Pentylenetetrazole