Determination of the lipophilicity of active anticonvulsant N-substituted amides of alpha-arylalkylamine-gamma-hydroxybutyric acid.

: The lipophilicities of fourteen anticonvulsant active N-substituted amides of alpha-arylalkylamine-gamma-hydroxybutyric acid [I-XIV] have been determined by reversed-phase thin-layer chromatography with a mixture of methanol, TRIS buffer, and acetic acid as the solvent system. The RM value of each compound decreased linearly with increasing concentration of methanol. The partition coefficients (log P) of the amides were calculated by use of the Prolog P module of the Pallas system. Comparison of RM and log P enabled clog P values to be calculated. It was found that the anticonvulsant activity of amides [I-XIV] can be explained on the basis of their lipophilicity.