Synthesis of and pharmacological studies on the antidepressant and anticonvulsant activities of some 1,3,5-trisubstituted pyrazolines.
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.
Ruhoğlu
Ozan
O
Hacettepe University, Faculty of Pharmacy, Department of Pharmaceutical Chemistry, Ankara, Turkey.
Ozdemir
Zuhal
Z
Caliş
Unsal
U
Gümüşel
Bülent
B
Bilgin
Abdullah Altan
AA
D000818:Animals; D000927:Anticonvulsants / Q000138:chemical synthesis* / Q000494:pharmacology*; D000928:Antidepressive Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D003292:Convulsants; D004597:Electroshock; D007202:Indicators and Reagents; D009682:Magnetic Resonance Spectroscopy; D008297:Male; D051379:Mice; D009043:Motor Activity / Q000187:drug effects; D020258:Neurotoxicity Syndromes / Q000503:physiopathology / Q000523:psychology; D010433:Pentylenetetrazole; D004856:Postural Balance / Q000187:drug effects; D011720:Pyrazoles / Q000138:chemical synthesis* / Q000494:pharmacology*; D012640:Seizures / Q000139:chemically induced / Q000517:prevention & control; D013056:Spectrophotometry, Ultraviolet; D013550:Swimming / Q000523:psychology
D000927:Anticonvulsants; D000928:Antidepressive Agents; D003292:Convulsants; D007202:Indicators and Reagents; D011720:Pyrazoles; D010433:Pentylenetetrazole