A quantitative structure-activity study of anticonvulsant phenylacetanilides.

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Abstract
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 ED50) for m-derivatives depended parabolically on log P (P is the 1-octanol-H2O partition coefficient) and linearly on the Hammett .sigma. 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 o- and p-substitutions are discussed.

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