Spirosuccinimides as potential anticonvulsants.
A series of spirosuccinimides was synthesized and evaluated for anticonvulsant activity. The study was designed to apply the Topliss approach to structure-activity correlations in this novel series of 2-substituted-2-azaspiro[4.4]nonane-1,3-diones and 2,4-disubstituted-2-azaspiro[4.4]nonane-1,3-diones. While no correlation was noted with the 2-substituted derivatives, a good correlation was obtained in the 2,4-disubstituted series, indicating that anticonvulsant activity was related to increasing tau values. The results of these anticonvulsant tests are presented and a rational approach to the structure-activity relationships of spirosuccinimides is provided.
D000818:Animals; D000927:Anticonvulsants / Q000138:chemical synthesis*; D055598:Chemical Phenomena; D002621:Chemistry; D004597:Electroshock; D008297:Male; D051379:Mice; D010433:Pentylenetetrazole / Q000037:antagonists & inhibitors; D013388:Succinimides / Q000138:chemical synthesis* / Q000494:pharmacology
D000927:Anticonvulsants; D013388:Succinimides; D010433:Pentylenetetrazole