2. Academic Validation
  3. Disubstituted piperidines as potent orexin (hypocretin) receptor antagonists

Disubstituted piperidines as potent orexin (hypocretin) receptor antagonists

  • Bioorg Med Chem Lett. 2012 Jun 15;22(12):3890-4. doi: 10.1016/j.bmcl.2012.04.122.
Rong Jiang 1,  Xinyi Song,  Purva Bali,  Anthony Smith,  Claudia Ruiz Bayona,  Li Lin,  Michael D Cameron,  Patricia H McDonald,  Paul J Kenny,  Theodore M Kamenecka
Affiliations

Affiliation

  • 1 Department of Molecular Therapeutics, and Translational Research Institute, The Scripps Research Institute, Scripps Florida, 130 Scripps Way #2A1, Jupiter, FL 33458, USA.
PMID: 22617492 DOI: 10.1016/j.bmcl.2012.04.122
Abstract

A series of orexin receptor antagonists was synthesized based on a substituted piperidine scaffold. Through traditional medicinal chemistry structure-activity relationships (SAR), installation of various groups at the 3-6-positions of the piperidine led to modest enhancement in receptor selectivity. Compounds were profiled in vivo for plasma and brain levels in order to identify candidates suitable for efficacy in a model of drug addiction.

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