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

  • Bioorg Med Chem Lett. 2009 Jun 15;19(12):3183-7. doi: 10.1016/j.bmcl.2009.04.128.
Alexandre V Ivachtchenko  1 ,  Eugene B Frolov ,  Oleg D Mitkin ,  Volodymyr M Kysil ,  Alexander V Khvat ,  Ilya M Okun ,  Sergey E Tkachenko
Affiliations
  • 1. Department of Organic Chemistry, Chemical Diversity Research Institute, 114401 Khimki, Moscow Reg., Russia. [email protected]
PMID: 19443217 DOI: 10.1016/j.bmcl.2009.04.128
Abstract

Synthesis, biological evaluation and structure-activity relationships for a series of novel gamma-carboline analogues of Dimebon 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) (IC(50)=0.1 microM) and serotonin 5-HT(6) (IC(50)=0.37 microM) receptors, respectively.