Faculty of Chemical Engineering and Technology, Institute of Organic Chemistry and Technology, Cracow University of Technology, 24 Warszawska Street, Cracow 31-155, Poland.
Faculty of Chemical Engineering and Technology, Institute of Organic Chemistry and Technology, Cracow University of Technology, 24 Warszawska Street, Cracow 31-155, Poland.
Bioorg Med Chem Lett. 2019 Aug 15;29(16):2236-2242. doi: 10.1016/j.bmcl.2019.06.029. Epub 2019 Jun 20.
More than 300 million people are suffering from depression, one of the civilization diseases in the 21st century. Serotonin 5-HTR and dopamine DR play an important role in the treatment and pathogenesis of depression. Moreover, in recent years, the efficacy of dual 5-HT/D receptors ligands has been demonstrated in the fight against depression. In this work the new bulky arylpiperazine derivatives (LCAP) were synthesized in microwave radiation field. The affinities for the selected serotonin (5-HT,5-HT,5-HT,5-HT) and dopamine (D) receptors have been evaluated in vitro. Compounds 5.3a, 5.4, 5.1c, 5.3d, 5.2a are promising dual 5-HTR/DR ligands. The SAR analysis were additionally supported with molecular docking studies.
超过 3 亿人患有抑郁症，这是 21 世纪文明病之一。5-羟色胺 5-HTR 和多巴胺 DR 在抑郁症的治疗和发病机制中起着重要作用。此外，近年来，双重 5-HT/DR 受体配体的疗效已在抗抑郁方面得到证实。在这项工作中，新型大体积芳基哌嗪衍生物（LCAP）在微波辐射场中合成。在体外评估了对选定的 5-羟色胺（5-HT、5-HT、5-HT、5-HT）和多巴胺（D）受体的亲和力。化合物 5.3a、5.4、5.1c、5.3d、5.2a 是有前途的双重 5-HTR/DR 配体。SAR 分析还得到了分子对接研究的支持。
