Résumé
Objectives: To synthesize dihydro-pyrimidine-5-carbonitrile derivatives [5-23], as an extension of the previous series, and to evaluate their anticonvulsant potential
Methods: The designed compounds were synthesized and characterized using infrared [IR], nuclear magnetic resonance [NMR] and mass spectroscopy and were evaluated for anticonvulsant activity using the maximal electroshock seizure [MES] and subcutaneous pentylenetetrazole [scPTZ] methods. Compounds with appreciable activity were investigated for their neurotoxicity using the rotarod test
Results: Compounds 17 and 23 were found to be most active at a dose of 30 mg kg[-1] at 0.5 h and 4 h in both models and did not exhibit motor impairment activity, even at higher doses
Conclusion: The newer designed compounds were found to be better than previously reported compounds. This study also shows that increased lipophilicity is directly related to the anticonvulsant activity