During the last fifteen years semicarbazones have been extensively investigated for their anticonvulsant properties. 4-(4-Flurophenoxy) benzaldehyde semicarbazone (C0102862, V102862) has been discovered as a lead molecule and is being developed as a potent antiepileptic drug, with maximal electroskock (MES) ED50 (i.p. 12.9 mg kg1). In MES (oral screen), this compound has protective index (PI = TD50/ED50 >315) higher than carbamazepine (PI 101), phenytoin (PI >21.6) and valproate (PI 2.17). This compound is a potent sodium channel blocker. Other semicarbazones have demonstrated activity in various chemoshock screens, like subcutaneous pentylenetetrazole (ScPTZ), subcutaneous strychnine (ScSTY), subcutaneous picrotoxine (ScPIC) and subcutaneous bicculline (ScBIC). Semicarbazones are also GABA-transaminase inhibitors. Extensive structure-activity relationship has demonstrated that F, Cl, Br and NO2 substitutents in the arylhydrophobic pocket and a hydrogen bonding domain (HBD) are generally found in active anticonvulsant agents.Tijekom posljednjih petnaest godina intenzivno su istraživana antikonvulzivna svojstva semikarbazona. 4-(4-Flurofenoksi)benzaldehid semikarbazon (C0102862, V102862) otkriven je kao vodeći spoj iz kojeg je razvijen antiepileptik s maksimalnom elektrošok aktivnošću (MES) ED50 12,9 mg kg1 (i.p.) i zaštitnim indeksom (PI = TD50/ED50 > 315) većim od karbamazepina (PI 101), fenitoina (PI > 21,6) i valproata (PI 2,17). Spoj je snažni blokator natrijevih kanala. Drugi su se semikarbazoni pokazali učinkovitima u različitim kemo-šok testovima, kao što su supkutana primjena pentilentetrazola, strihnina, pikrotoksina i bikukulina. Semikarbazoni su također inhibitori GABA-transaminaze. Opširne studije odnosa strukture i djelovanja pokazale su da je za antikonvulzivno djelovanje bitna prisutnost F, Cl, Br i NO2 supstituenata u arilhidrofobnom džepu i domena za vezanje vodikovim vezama (HBD)
