Diastereoselective synthesis of 1,4,8-trisubstituted perhydroquinolines as novel kappa receptor agonists

Key Points

• The aim is to develop novel kappa-opioid receptor agonists for therapeutic use in pain management and inflammatory diseases.
• Synthesis of 1,4,8-trisubstituted perhydroquinolines through diastereoselective methods.
• Evaluation of agonist activity at the kappa-opioid receptor.
• Analysis of pharmacophoric properties of new compounds.
• Identified several novel kappa agonists with enhanced binding affinity.
• Demonstrated effective pain relief in preclinical models, suggesting significant therapeutic potential.