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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| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3383661 | PMC |
| http://dx.doi.org/10.1016/j.bmcl.2012.04.122 | DOI Listing |
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