构象受限的同型色胺。第5部分：3-（反式-2-氨甲基环戊基）吲哚作为强效选择性5-羟色胺再摄取抑制剂。
Conformationally restricted homotryptamines. Part 5: 3-(trans-2-aminomethylcyclopentyl)indoles as potent selective serotonin reuptake inhibitors.
作者信息
Denhart Derek J, Deskus Jeffrey A, Ditta Jonathan L, Gao Qi, Dalton King H, Kozlowski Edward S, Meng Zhaoxing, LaPaglia Melissa A, Mattson Gail K, Molski Thaddeus F, Taber Matthew T, Lodge Nicholas J, Mattson Ronald J, Macor John E
机构信息
Bristol-Myers SquibbPharmaceutical Research Institute, 5 Research Parkway, Wallingford, CT 06492-7660, USA.
出版信息
Bioorg Med Chem Lett. 2009 Aug 1;19(15):4031-3. doi: 10.1016/j.bmcl.2009.06.026. Epub 2009 Jun 13.
A series of racemic 3-(trans-2-aminomethylcyclopentyl)indoles was synthesized and found to have potent binding to the human serotonin transporter (hSERT). The most active analog was synthesized stereospecifically and the active enantiomer was shown to have high affinity binding to hSERT.
合成了一系列外消旋的3-(反式-2-氨甲基环戊基)吲哚，发现它们与人血清素转运体(hSERT)有很强的结合力。以立体定向方式合成了活性最高的类似物，结果表明活性对映体与hSERT具有高亲和力结合。
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