Spirosuccinimides as potential anticonvulsants

Article abstract of DOI:10.1002/jps.2600740721

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]nonae-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 π values. The results of these anticonvulsant tests are presented and a rational approach to the structure-activity relationships of spirosuccinimides is provided.