title: Synthesis and anticonvulsant activity of some 4-nitro-N-phenylbenzamides.
abstract: A short series of 4-nitro-N-phenylbenzamides was synthesized and evaluated for anticonvulsant properties and neurotoxicity. In mice dosed intraperitoneally, three of the four 4-nitro-N-phenylbenzamides were efficient in the maximal electroshock-induced seizure (MES) test, especially N-(2,6-dimethylphenyl)-4-nitrobenzamide (ED(50) value in the MES test = 31.8 μmol/kg, TD(50) = 166.9 μmol/kg, protective index [PI] = 5.2) and N-(2-chloro-6-methylphenyl)-4-nitrobenzamide (ED(50) value in the MES test = 90.3 μmol/kg, TD(50) = 1.068 μmol/kg, PI = 11.8). The latter 4-nitro-N-phenylbenzamide was also found to be active against seizures induced by subcutaneous pentylenetetrazole (sc Ptz) and was selected for further evaluation in rats dosed orally. In these conditions, N-(2-chloro-6-methylphenyl)-4-nitrobenzamide was found to be, in the MES test, three times more active than phenytoin and 4-amino-N-(2,6-dimethylphenyl)benzamide, two potent anti-MES agents.
authors.affiliation: North France Center for the Study of Childhood Epilepsy, Service du Professeur Jean-Pierre Nuyts, Centre Hospitalier & Universitaire de Lille, Hôpital B, 59037 Lille Cedex, France.
authors.forename: V
authors.initials: V
authors.lastname: Bailleux
authors.forename: L
authors.initials: L
authors.lastname: Vallée
authors.forename: J
authors.initials: J
authors.lastname: Nuyts
authors.forename: G
authors.initials: G
authors.lastname: Hamoir
authors.forename: J
authors.initials: J
authors.lastname: Poupaert
authors.forename: J
authors.initials: J
authors.lastname: Stables
authors.forename: J
authors.initials: J
authors.lastname: Vamecq