Design, synthesis and SAR analysis of novel selective σ1 ligands (Part 2)

In order to investigate the molecular features involved in sigma receptors (σ-Rs) binding, new compounds based on arylalkylaminoalcoholic, arylalkenyl- and arylalkylaminic scaffolds were synthesized and their affinity towards σ1- and σ2-Rs subtypes was evaluated. The most promising compounds were also screened for their affinity at μ-opioid, δ-opioid and κ-opioid receptors. Biological results are herein presented and discussed.

Preparation and SAR results of novel σ ligands are herein presented. Among the most σ1-active compounds, (R/S)-1d showed noticeable selectivity towards σ2 subtype and excellent selectivity against opioid receptors.Figure optionsDownload as PowerPoint slide