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Bioorg Med Chem Lett. 2012 Jun 15;22(12):3890-4. doi: 10.1016/j.bmcl.2012.04.122. Epub 2012 May 4.

Disubstituted piperidines as potent orexin (hypocretin) receptor antagonists.

Author information

1
Department of Molecular Therapeutics, and Translational Research Institute, The Scripps Research Institute, Scripps Florida, 130 Scripps Way #2A1, Jupiter, FL 33458, USA.

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.

PMID:
22617492
PMCID:
PMC3383661
DOI:
10.1016/j.bmcl.2012.04.122
[Indexed for MEDLINE]
Free PMC Article

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