Synthesis, anticonvulsant and toxicity screening of newer pyrimidine semicarbazone derivatives

Eur J Med Chem. 2010 Jun;45(6):2467-72. doi: 10.1016/j.ejmech.2010.02.031. Epub 2010 Feb 18.

Abstract

A number of N-(4,6-substituted diphenylpyrimidin-2-yl) semicarbazones (4a-t) were synthesized and tested for their anticonvulsant activity against the two seizure models, maximal electroshock seizure (MES) and subcutaneous pentylenetetrazole (scPTZ). All the synthesized compounds possessed the four essential pharmacophoric elements for good anticonvulsant activity. Most of the compounds displayed good anticonvulsant activity with lesser neurotoxicity. To assess the unwanted effects of the compounds on liver, estimation of enzymes and proteins was carried out.

MeSH terms

  • Animals
  • Anticonvulsants / chemical synthesis
  • Anticonvulsants / chemistry
  • Anticonvulsants / pharmacology*
  • Anticonvulsants / toxicity*
  • Drug Evaluation, Preclinical / methods*
  • Drug Synergism
  • Epilepsy / drug therapy
  • Liver / drug effects
  • Liver / enzymology
  • Liver / metabolism
  • Mice
  • Nervous System / drug effects
  • Pyrimidines / chemistry*
  • Semicarbazones / chemical synthesis
  • Semicarbazones / chemistry
  • Semicarbazones / pharmacology*
  • Semicarbazones / toxicity*

Substances

  • Anticonvulsants
  • Pyrimidines
  • Semicarbazones
  • pyrimidine