Structure and anticonvulsant activity relationship of phthalimides

Abstract

Phthalimides, bis-phthalimides and analogues were synthesized and screened for the possibility of finding compounds possessing anticonvulsant activity. Condensation reaction between selected anhydrides and various interested amines leads to the accomplishment of the preparation of sixty-four phthalimides, twelve bis-phthalimides, six analogues. Synthesized phthalimides were subjected to test with MES (Maximal Electroshock Seizure) test, a preliminary screening test for anticonvulsant activity compared with phenytoin. It was disclosed that the best patterns require amino substitution on the N-phenyl moiety. The most potent compounds found were those contained 4-amino, 2-chloro-4-amino and 2-methyl-4-amino, respectively, substituted of the N-phenyl ring.