Novel trans-3,4-dimethyl-4-(3-hydroxyphenyl)piperidines as μ opioid receptor antagonists with improved opioid receptor selectivity profiles

A series of N-substituted trans-3,4-dimethyl-4-(3-hydroxyphenyl)piperidines, μ opioid receptor antagonists, analogs of alvimopan, were prepared using solid phase methodology. This study led to the identification of a highly selective μ opioid receptor antagonist, which interacts selectively with μ peripheral receptors.

Graphical abstractThe discovery and SAR studies of a series of N-substituted trans-3,4-dimethyl-4-(3-hydroxyphenyl)piperidines as novel μ opioid receptor antagonists, analogs of alvimopan, are reported.Figure optionsDownload full-size imageDownload as PowerPoint slide