Design, synthesis and anticonvulsive activity of analogs of gamma-vinyl GABA

Farmaco. 2004 May;59(5):381-8. doi: 10.1016/j.farmac.2004.01.011.

Abstract

For the development of new anticonvulsive agents, analogs of gamma-vinyl GABA (vigabatrin) containing GABA, gamma-vinyl GABA, valproic acid, nipecotic acid or isonipecotic acid moieties were prepared and evaluated for their anticonvulsive activities. Most of the prepared compounds showed moderate anticonvulsive activities. Among them compounds 10 and 16 displayed the most potent anticonvulsive activity and a broader spectrum compared to vigabatrin.

Publication types

  • Comparative Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Anticonvulsants / chemical synthesis*
  • Anticonvulsants / therapeutic use
  • Disease Models, Animal
  • Drug Design
  • Isonipecotic Acids / chemistry
  • Isonipecotic Acids / pharmacology
  • Male
  • Mice
  • Nipecotic Acids / chemistry
  • Nipecotic Acids / pharmacology
  • Seizures / chemically induced
  • Seizures / drug therapy*
  • Structure-Activity Relationship
  • Valproic Acid / chemistry
  • Valproic Acid / pharmacology
  • Vigabatrin / chemical synthesis*
  • Vigabatrin / therapeutic use

Substances

  • Anticonvulsants
  • Isonipecotic Acids
  • Nipecotic Acids
  • nipecotic acid
  • Valproic Acid
  • Vigabatrin