某些1-硫代甲酰基-3,5-二苯基-2-吡唑啉的合成与抗抑郁活性研究
Studies on the synthesis and antidepressant activity of some 1-thiocarbamoyl-3,5-diphenyl-2-pyrazolines.
作者信息
Bilgin A A, Palaska E, Sunal R
机构信息
Hacettepe University, Faculty of Pharmacy, Department of Pharmaceutical Chemistry, Ankara, Turkey.
出版信息
Arzneimittelforschung. 1993 Oct;43(10):1041-4.
Several 1-thiocarbamoyl-3,5-diphenyl-2-pyrazoline derivatives have been synthesized by reacting 1,3-diphenyl-2-propen-1-one (chalcones) with thiosemicarbazide, or hydrazine hydrate and then with various isothiocyanates. Their chemical structures have been proven by UV, IR, 1H-NMR and elemental analysis. Antidepressant activities were investigated by "Porsolt's Behavioural Despair Test". 1-Thiocarbamoyl-3-(phenyl and 4-chlorophenyl-5-(4-methyl and 4-methoxyphenyl-2-pyrazoline (compounds III, IV, VII, VIII) and 3-(4-methylphenyl)-5-(4-methoxyphenyl)-2-pyrazoline (compound XII) showed equivalent or higher activity than pargyline hydrochloride and tranylcypromine sulfate.
通过使1,3 - 二苯基 - 2 - 丙烯 - 1 - 酮（查耳酮）与硫代氨基脲或水合肼反应，然后再与各种异硫氰酸酯反应，合成了几种1 - 硫代氨基甲酰基 - 3,5 - 二苯基 - 2 - 吡唑啉衍生物。它们的化学结构已通过紫外光谱、红外光谱、1H - 核磁共振和元素分析得到证实。通过“波索尔特行为绝望试验”研究了它们的抗抑郁活性。1 - 硫代氨基甲酰基 - 3 -（苯基和4 - 氯苯基）- 5 -（4 - 甲基和4 - 甲氧基苯基）- 2 - 吡唑啉（化合物III、IV、VII、VIII）和3 -（4 - 甲基苯基）- 5 -（4 - 甲氧基苯基）- 2 - 吡唑啉（化合物XII）显示出与盐酸帕吉林和硫酸反苯环丙胺相当或更高的活性。
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