Ruhoğlu Ozan, Ozdemir Zuhal, Caliş Unsal, Gümüşel Bülent, Bilgin Abdullah Altan
Hacettepe University, Faculty of Pharmacy, Department of Pharmaceutical Chemistry, Ankara, Turkey.
Arzneimittelforschung. 2005;55(8):431-6.
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.
合成了18种1-苯基-、1-硫代甲酰基-和1-N-取代硫代甲酰基-3-苯基-5-杂芳基-2-吡唑啉衍生物，并对其抗抑郁和抗惊厥活性进行了测试。通过光谱和微量分析证实了它们的化学结构。通过“强迫游泳试验”研究了这些化合物的抗抑郁活性。结果表明，化合物II-a、b、c、III-1b、1c、4a表现出与用作参考抗抑郁药物的盐酸帕吉林（CAS 306-07-0）和硫酸反苯环丙胺（CAS 13492-01-8）相当或更高的活性。根据抗癫痫药物开发计划的I期试验，通过小鼠最大电休克惊厥（MES）、皮下注射戊四氮（ScMet.）和转棒毒性试验测定了这些化合物的抗惊厥活性。发现化合物I-a、II-a、b、c、III-1b、2a、2c对MES有保护作用，III-1b、1c、2a、2c对ScMet.有保护作用。
