A quantitative structure-activity relationship (QSAR) analysis of the effects of aromatic substitution on the anticonvulsant activity and toxicity of arylsuccinimides.
Anticonvulsant activity and toxicity of 20 arylsuccinimides were quantitatively correlated with the hydrophobic, electronic and steric parameters of the substituents in the benzene ring and at the nitrogen atom. The activity was highest when the benzene ring substituents X were characterized by hydrophobic fragmental constants fx lying in the 1.0-1.7 range, though toxicity increased with fx.
Lange
J
J
Institute of Organic Technology, Warsaw Polytechnic, Poland.
Kaźmierski
W
W
Daroszewski
J
J
D000818:Animals; D000927:Anticonvulsants / Q000138:chemical synthesis* / Q000494:pharmacology / Q000633:toxicity; D004597:Electroshock; D007928:Lethal Dose 50; D013056:Spectrophotometry, Ultraviolet; D013329:Structure-Activity Relationship; D013388:Succinimides / Q000138:chemical synthesis* / Q000494:pharmacology / Q000633:toxicity
D000927:Anticonvulsants; D013388:Succinimides