A selective delta opioid receptor antagonist based on a stilbene core

Bioorg Med Chem Lett. 2015 Dec 1;25(23):5532-5. doi: 10.1016/j.bmcl.2015.10.059.

Alyssa M Hartung ¹, Hernan A Navarro ², David F Wiemer ¹, Jeffrey D Neighbors ³

Affiliations

1 Department of Chemistry, The University of Iowa, Chemistry Building, Iowa City, IA 52242-1294, United States.
2 Discovery Sciences, RTI International, Research Triangle Park, NC 27709, United States.
3 Department of Chemistry, The University of Iowa, Chemistry Building, Iowa City, IA 52242-1294, United States; Department of Pharmacology, Pennsylvania State University Hershey College of Medicine, Hershey, PA 17033, United States; Penn State Hershey Cancer Institute, Hershey, PA 17033, United States.

PMID: 26525865 DOI: 10.1016/j.bmcl.2015.10.059

Abstract

Studies of directed ortho metalation reactions on an aromatic substrate with multiple potential directing groups have identified conditions that favor either of two regioisomers. One of these regioisomers has been converted to an analogue of the stilbene pawhuskin A, and been shown to have high selectivity as an antagonist of the delta Opioid Receptor. Docking studies have suggested that this compound can adopt a conformation similar to naltrindole, a known delta antagonist.

Keywords

Delta receptor; Directed ortho metalation; Docking; Opioid; Pawhuskin.

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