Synthesis and structure-activity studies of alkyl-substituted. gamma.-butyrolactones and. gamma.-thiobutyrolactones: ligands for the picrotoxin receptor

…, JA Levine, AC McKeon, JA Ferrendelli…

Index: Canney; Holland; Levine; McKeon; Ferrendelli; Covey Journal of Medicinal Chemistry, 1991 , vol. 34, # 4 p. 1460 - 1467

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Citation Number: 33

Abstract

A series of y-butyrolactones and y-thiobutyrolactones possessing a variety of alkyl groups and alkyl-substitution patterns was prepared and evaluated for anticonvulsant and convulsant activity. Behavioral studies performed on these compounds suggest that maximal anticonvulsant activity (against maximal electroshock and pentylenetetrazol) results when three or four carbon atoms are present at the a-position. For convulsant potency, a similar ...