Design, synthesis and anticonvulsive activities of potential prodrugs linked by two-carbon chain

Arch Pharm Res. 2003 Oct;26(10):785-95. doi: 10.1007/BF02980021.

Abstract

For the development of new anticonvulsive agents, GABAmimetics such as nipecotic acid, isonipecotic acid, gamma-aminobutyric acid (GABA), gamma-vinyl GABA (vigabatrin) and valproic acid were covalently coupled through an ester bond by a two-carbon linker chain as potential pro-drugs and evaluated for their anticonvulsive activities.

Publication types

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

MeSH terms

  • Animals
  • Anticonvulsants / chemical synthesis*
  • Anticonvulsants / pharmacology*
  • Carbon / chemistry*
  • Convulsants / administration & dosage
  • Convulsants / adverse effects
  • Convulsants / antagonists & inhibitors
  • Dimerization*
  • Drug Design*
  • Electroshock / adverse effects
  • Injections, Intraperitoneal
  • Injections, Subcutaneous
  • Isonipecotic Acids / administration & dosage
  • Isonipecotic Acids / chemistry
  • Isonipecotic Acids / pharmacokinetics
  • Ligands
  • Male
  • Mice
  • Mice, Inbred ICR
  • Nipecotic Acids / administration & dosage
  • Nipecotic Acids / chemistry
  • Nipecotic Acids / pharmacokinetics
  • Prodrugs / chemical synthesis*
  • Prodrugs / metabolism
  • Prodrugs / pharmacology*
  • Seizures / chemically induced
  • Seizures / drug therapy
  • Seizures / physiopathology
  • Valproic Acid / administration & dosage
  • Valproic Acid / chemistry
  • Valproic Acid / pharmacokinetics
  • Vigabatrin / administration & dosage
  • Vigabatrin / chemistry
  • Vigabatrin / pharmacokinetics
  • gamma-Aminobutyric Acid / administration & dosage
  • gamma-Aminobutyric Acid / chemistry
  • gamma-Aminobutyric Acid / pharmacokinetics

Substances

  • Anticonvulsants
  • Convulsants
  • Isonipecotic Acids
  • Ligands
  • Nipecotic Acids
  • Prodrugs
  • gamma-Aminobutyric Acid
  • Valproic Acid
  • Carbon
  • Vigabatrin