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

@article{Canney1991SynthesisAS,
  title={Synthesis and structure-activity studies of alkyl-substituted gamma-butyrolactones and gamma-thiobutyrolactones: ligands for the picrotoxin receptor.},
  author={Daniel J. Canney and Katherine D. Holland and James A. Levine and Amy McKeon and James A. Ferrendelli and Douglas F Covey},
  journal={Journal of medicinal chemistry},
  year={1991},
  volume={34 4},
  pages={1460-7}
}
A series of gamma-butyrolactones and gamma-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 alpha-position. For convulsant potency, a similar dependence on the size of the alkyl chain… CONTINUE READING