Synthesis, anticonvulsant and toxicity screening of newer pyrimidine semicarbazone derivatives

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.

Various pyrimidine incorporated semicarbazones (4a–t) have been synthesized keeping in view the structural requirements of the proposed pharmacophore model. Some compounds showed promising anticonvulsant activity with less neurotoxicity and hepatotoxicity.Figure optionsDownload as PowerPoint slide