SYNTHESIS OF SOME NEW 1,3,5-TRESUBSTITUTED PYRAZOLINES WITH ANTIDEPRESSANT AND ANTICONVULSANT ACTIVITIES


Iyidogan P., Ozdemir Z., Kandilci B., Gumusel B., Calis U., Bilgin A. A.

ISTANBUL JOURNAL OF PHARMACY, vol.38, no.1, pp.47-56, 2005 (Peer-Reviewed Journal) identifier

  • Publication Type: Article / Article
  • Volume: 38 Issue: 1
  • Publication Date: 2005
  • Journal Name: ISTANBUL JOURNAL OF PHARMACY
  • Journal Indexes: Emerging Sources Citation Index, TR DİZİN (ULAKBİM)
  • Page Numbers: pp.47-56

Abstract

Twelve 1-phenyl-, 1-thiocarbamoyl-, 1-N-substituted thiocarbamoyl- and 1(4'-pbenylthiazol-2'-yl)-3-(2-naphty1)-5-phenyl/(2-fury1)-2-pyrazoline derivatives were synthesized and tested for their antidepressant and anticonvulsant activities. Their chemical structures were proved by spectral data and microanalysis. The antidepressant activities of the compounds were investigated by the "forced swimming test". Compounds 1, 10, 11 and 12 had equivalent or higher activities than tranylcypromine sulfate that was used as reference antidepressant drug. Anticonvulsant activity and neurotoxicity of the compounds were determined by maximal electroshock seizure (MES), subcutaneous metrazol (SeMet.) and rotarod toxicity tests according to the phase 1 tests of Antiepileptic Drug Development (ADD) programme Compounds 1, 2, 4, 7, 9,11 and 12 were active against MES and ScMet. at 30-300 mg/kg dose levels. 7 and 9 were found as the highest protective compounds against ScMet.s at 30 mg/kg dose at four hours.