当前位置: X-MOL 学术Eur. J. Med. Chem. › 论文详情
Our official English website, www.x-mol.net, welcomes your feedback! (Note: you will need to create a separate account there.)
8-Sulfonyl-substituted tetrahydro-1H-pyrido[4,3-b]indoles as 5-HT6 receptor antagonists
European Journal of Medicinal Chemistry ( IF 6.0 ) Pub Date : 2009-10-31 , DOI: 10.1016/j.ejmech.2009.10.035
Alexandre V. Ivachtchenko , Oleg D. Mitkin , Sergey E. Tkachenko , Ilya M. Okun , Volodymyr M. Kysil

A series of novel 8-sulfonyl-substituted 2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indoles (THPI) has been synthesized and their ability to interact with 5-HT6 receptors evaluated in cell-based and radioligand binding assays. Amongst evaluated THPIs, compounds 9.HCl and 20.HCl have been identified as the most potent 5-HT6 receptor antagonists with Ki values equal to 2.1 nM and 5.7 nM and IC50 values (functional assay) equal to 15 nM and 78 nM, respectively. Affinities of these two compounds for several serotonin receptors in the competitive radioligand binding assays as well as their specificity profiles against a panel of therapeutic targets have been determined.



中文翻译:

8-磺酰基取代的四氢-1 H-吡啶并[4,3- b ]吲哚作为5-HT 6受体拮抗剂

合成了一系列新型的8-磺酰基取代的2,3,4,5-四氢-1 H-吡啶并[4,3- b ]吲哚(THPI),并评估了它们与5-HT 6受体相互作用的能力。基于细胞的和放射性配体结合测定。在评估的THPI中,化合物9 .HCl和20 .HCl被确定为最有效的5-HT 6受体拮抗剂,其K i值等于2.1 nM和5.7 nM,IC 50值(功能测定)分别等于15 nM和78 nM。在竞争性放射性配体结合测定中,已经确定了这两种化合物对几种血清素受体的亲和力,以及它们对一组治疗靶标的特异性。

更新日期:2009-10-31
down
wechat
bug