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

  • Bioorg Med Chem Lett. 2008 Mar 15;18(6):2006-12. doi: 10.1016/j.bmcl.2008.01.106.
Bertrand Le Bourdonnec  1 ,  William M Barker ,  Serge Belanger ,  Daniel D Wiant ,  Nathalie C Conway-James ,  Joel A Cassel ,  Timothy J O'Neill ,  Patrick J Little ,  Robert N DeHaven ,  Diane L DeHaven-Hudkins ,  Roland E Dolle
Affiliations
  • 1. Department of Chemistry, Adolor Corporation, 700 Pennsylvania Drive, Exton, PA 19341, USA. [email protected]
PMID: 18313920 DOI: 10.1016/j.bmcl.2008.01.106
Abstract

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

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