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

Synthesis, biological evaluation and structure–activity relationships for a series of novel γ-carboline analogues of Dimebon™ are described. Among the studied compounds, γ-carbolines 3{8} and 3{14} have been identified as potent small molecule antagonists of histamine H1 (IC50 = 0.1 μM) and serotonin 5-HT6 (IC50 = 0.37 μM) receptors, respectively.

Graphical abstractSynthesis, biological evaluation and structure–activity relationships for a series of novel γ-carboline analogues of Dimebon™.Figure optionsDownload full-size imageDownload as PowerPoint slide