1-(1H-吡咯-1-基甲基)-4-氮杂三环[5.2.1.0(2,6)]癸-8-烯-3,5-二酮的合成、结构与药理评价
SYNTHESIS, STRUCTURE AND PHARMACOLOGICAL EVALUATION OF 1-(1H-PYRROL-1-YLMETHYL)-4-AZATRICYCLO[5.2.1.0(2,6)] DEC-8-ENE-3,5-DIONE.
作者信息
Pakosińska-Parys Magdalena, Zimniak Andrzej, Chodkowska Anna, Jagiełło-Wójtowicz Ewa, Głowala Marek, Struga Marta
出版信息
Acta Pol Pharm. 2016 Jul;73(4):931-936.
PMID:29648718
Abstract
A set of arylpiperazine derivatives with imide fragments, 1-(1H-pyrrol-1-ylmethyl)-10-oxa-4-azatricyclo[5.2.1.0(2,6)-]dec-8-ene-3,5-dione connected by propyl and butyl linkers, were synthesized and tested for the potential anxiolytic and antidepressant activities. Compounds 3a and 3b demonstrated antidepressant activity in the forced swimming tests in mice and were devoid of neurotoxic effects. (chimney test in mice).
摘要
合成了一组带有酰亚胺片段、通过丙基和丁基连接基相连的1-(1H-吡咯-1-基甲基)-10-氧杂-4-氮杂三环[5.2.1.0(2,6)-]癸-8-烯-3,5-二酮的芳基哌嗪衍生物，并对其潜在的抗焦虑和抗抑郁活性进行了测试。化合物3a和3b在小鼠强迫游泳试验中表现出抗抑郁活性，且无神经毒性作用（小鼠烟囱试验）。
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