Synthesis and anticonvulsant activity of 4-bromophenyl substituted aryl semicarbazones

A number of 4-bromophenyl semicarbazones were synthesised and evaluated for anticonvulsant and sedative-hypnotic activities. After intraperitoneal inj ection to mice, the semicarbazone derivatives were examined in the maximal electroshock seizure (MES), subcutaneous pentylenetetrazole (scPTZ), subcut aneous strychnine (scSTY) and neurotoxicity (NT) screens. All the compounds showed anticonvulsant activity in one or more test models. Compound 12 sho wed greatest activity, being active in all the screens with very low neurot oxicity and no sedative-hypnotic activity. All the compounds except 7 had l ower neurotoxicity compared to phenytoin. Three compounds (6, 11 and 14) sh owed greater protection than sodium valproate. The essential structural fea tures responsible for interaction with receptor site are established within a suggested pharmacophore. (C) 2000 Editions scientifiques et medicales El sevier SAS.