Yun Jun, Han Minsoo, Song Chiman, Cheon Seung Hoon, Choi Kihang, Hahn Hoh-Gyu
Chemical Kinomics Research Center, Korea Institute of Science and Technology, Seoul 136-791, Republic of Korea; Department of Chemistry, Research Institute for Natural Sciences, Korea University, Seoul 136-701, Republic of Korea.
Chemical Kinomics Research Center, Korea Institute of Science and Technology, Seoul 136-791, Republic of Korea.
Bioorg Med Chem Lett. 2014 Aug 1;24(15):3234-7. doi: 10.1016/j.bmcl.2014.06.026. Epub 2014 Jun 18.
We report the synthesis of 3-phenethylazetidine derivatives 2 and their biological activities against 5-HT, NE and DA transporters as well as microsomal stability, CYP inhibition, and hERG inhibition profiles. Compound 2at showed most potent triple reuptake inhibitor with good selectivity as a candidate for depression.
我们报道了3-苯乙基氮杂环丁烷衍生物2的合成及其对5-羟色胺、去甲肾上腺素和多巴胺转运体的生物活性，以及微粒体稳定性、细胞色素P450抑制和人醚-去极化相关基因（hERG）抑制情况。化合物2at表现出最有效的三重再摄取抑制剂，具有良好的选择性，可作为抑郁症治疗候选药物。
