Synthesis and biological evaluation of 3-phenethylazetidine derivatives as triple reuptake inhibitors
Synthesis and biological evaluation of 3-phenethylazetidine derivatives as triple reuptake inhibitors
复制标题
DOI：
10.1016/j.bmcl.2014.06.026
复制
发表时间：
2014-08-01
影响因子：
2.7
通讯作者：
Hahn, Hoh-Gyu
中科院分区：
文献类型：
--
作者：
Yun, Jun;Han, Minsoo;Hahn, Hoh-Gyu
本文报道了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，以及对微粒体的稳定性、CYP抑制和HERG抑制谱。化合物2AT是最有效的三重再摄取抑制剂，具有良好的选择性，可作为抑郁症的候选药物。(C)2014爱思唯尔有限公司。保留所有权利。
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. (C) 2014 Elsevier Ltd. All rights reserved.