Chemical Kinomics Research Center, Korea Institute of Science and Technology, Wolsong-gil 5, Seongbuk-gu, Seoul, Republic of Korea; Department of Chemistry, Sogang University, Baekbeomno 35, Mapogu, Seoul, Republic of Korea.
Bioorg Med Chem Lett. 2013 Oct 15;23(20):5515-8. doi: 10.1016/j.bmcl.2013.08.062. Epub 2013 Aug 26.
A series of 3,4-diarylpyrrolidin-2-one was designed, prepared and evaluated as triple reuptake inhibitors for antidepressant. Most compounds exhibited comparable in vitro efficacy as norepinephrine and dopamine transporter reuptake inhibitors. Especially, 2i showed better potency than GBR-12909 (IC50=14 nM) which was used as reference compound for dopamine transporter. In addition, 2a and 2b showed inhibition (5.17 μM-85.6 nM) for three transporters.
设计、合成并评价了一系列 3,4-二芳基吡咯烷-2-酮类化合物作为抗抑郁药的三重再摄取抑制剂。大多数化合物表现出与去甲肾上腺素和多巴胺转运体再摄取抑制剂相当的体外活性。特别是，化合物 2i 对多巴胺转运体的抑制活性强于作为参比化合物的 GBR-12909（IC50=14 nM）。此外，化合物 2a 和 2b 对三种转运体均表现出抑制作用（5.17 μM-85.6 nM）。
