A Quantitative Structure-Activity Study of Anticonvulsant Phenylacetanilides

概要

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A series of o-, m-, and p-substituted anilides of phenylacetic acid were tested for anticonvulsant activity in mice by means of the maximal electroshock seizure test and structure-activity relationships were quantitatively studied by Hansch analysis. The potencies (-log ED_<50>) for meta derivatives were shown to depend parabolically on log P (P is the 1-octanol-H_2O partition coefficient) and linearly on the Hammett σ values. The derived correlation predicted that the maximum activity would be obtained when log P is about 2. 3 and an electron-donating substituent is introduced. This conclusion is consistent with the structural requirements recently reported for m-and p-substituted benzyl N, N-dimethylcarbamates. Most of the o-and p-substituted compounds exhibited lower activities than m-derivatives. The effects of ortho and para substitutions are discussed.
社団法人日本薬学会の論文
1984-12-25