Abstract
A series of aralkyl and alkyl carbamates of the type R1OCONR2R3 (R1=alkyl or aralkyl, R2, R3=H, Me, Et) were prepared and tested for anticonvulsant activity in mice by means of the maximal electroshock seizure test. The ED50 values were analyzed in terms of hydrophobic (log P), electronic (σ1) and other parameters by regression analysis. The results are essentially the same as those for previously studied m-and p-substituted benzyl N, N-dimethylcarbamates (X-C6H4-CH2OCONMe2). The activity depended parabolically on log P with an optimum log P of 1.7, and was negatively correlated with σ1. It was also found that the potency is reduced when R1 is an alkyl group or includes a hydrogen-bonding group. Structural requirements for the optimal potency and the aromatic ring contribution to the activity are discussed.
