Synthesis of and pharmacological studies on the antidepressant and anticonvulsant activities of some 1,3,5-trisubstituted pyrazolines

Ruhoǧlu O., Özdemir Z., Çaliş Ü., Gümüşel B., Bilgin A. A.

Arzneimittel-Forschung/Drug Research, cilt.55, sa.8, ss.431-436, 2005 (SCI-Expanded) identifier identifier

  • Yayın Türü: Makale / Tam Makale
  • Cilt numarası: 55 Sayı: 8
  • Basım Tarihi: 2005
  • Doi Numarası: 10.1055/s-0031-1296884
  • Dergi Adı: Arzneimittel-Forschung/Drug Research
  • Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus
  • Sayfa Sayıları: ss.431-436
  • Anahtar Kelimeler: Anticonvulsants, Antidepressants, Pyrazolines, anticonvulsant activity, antidepressant activity, mouse, synthesis
  • Lokman Hekim Üniversitesi Adresli: Hayır

Özet

Eighteen 1-phenyl-, 1-thiocarbamoyl- and 1-N-substitutedthiocarbamoyl-3- phenyl-5-heteroaryl-2-pyrazoline derivatives were synthesized and tested for their antidepressant and anticonvulsant activities. Their chemical structures were proved by spectral and microanalysis. The antidepressant activities of the compounds were investigated by the "forced swimming test". Results showed that compounds II-a,b,c, III-1b,1c,4a showed activities equivalent to or higher than pargyline hydrochloride (CAS 306-07-0) and tranylcypromine sulfate (CAS 13492-01-8) that were used as reference antidepressant drugs. Anticonvulsant activities of the compounds were determined by maximal electroshock seizure (MES), subcutaneous metrazol (ScMet.) and rotarod toxicity tests in mice according to the phase I tests of the Antiepileptic Drug Development programme. Compounds I-a, II-a,b,c, III-1b,2a,2c were found protective against MES and III-1b,1c,2a,2c were found protective against ScMet. © ECV · Editio Cantor Verlag.