Design of dual acting anticonvulsant-antimuscarinic succinimide and hydantoin derivatives

A series of 4-dialkylamino-2-butynyl-succinimide and -hydantoin derivatives were designed containing pharmacophoric elements for dual acting anticonvulsant and antimuscarinic activity. Potent anticonvulsant agents were identified with an extremely rapid onset of protective activity. Succinimides 13 and 13 exhibited ED50 values of 20 and 9.6 mg/kg 10 minutes after administration in the MES seizure model and also exhibited good binding affinity for the M1 muscarinic receptor.