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Synthesis and biological evaluation of novel gamma-carboline analogues of Dimebon as potent 5-HT6 receptor antagonists

  作者 Ivachtchenko, AV; Frolov, EB; Mitkin, OD; Kysil, VM; Khvat, AV; Okun, IM; Tkachenko, SE  
  选自 期刊  Bioorganic & Medicinal Chemistry Letters;  卷期  2009年19-12;  页码  3183-3187  
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[摘要]Synthesis, biological evaluation and structure-activity relationships for a series of novel gamma-carboline analogues of Dimebon (TM) are described. Among the studied compounds, gamma-carbolines 3{8} and 3{14} have been identified as potent small molecule antagonists of histamine H-1 (IC50 = 0.1 mu M) and serotonin 5-HT6 (IC50 = 0.37 mu M) receptors, respectively. Published by Elsevier Ltd.

 
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