Quantitative Structure-Activity Relationships of Anticonvulsant Aralkyl and Alkyl Carbamates

概要

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A series of aralkyl and alkyl carbamates of the type R_1OCONR_2R_3 (R_1=alkyl or aralkyl, R_2,R_3=H, Me, Et) were prepared and tested for anticonvulsant activity in mice by means of the maximal electroshock seizure test. The ED_<50> values were analyzed in terms of hydrophobic (log P), electronic (σ_1) 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-C_6H_4-CH_2OCONMe_2). The activity depended parabolically on log P with an optimum log P of 1.7,and was negatively correlated with σ_1. It was also found that the potency is reduced when R_1 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.
社団法人日本薬学会の論文
1985-06-25