Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10588314 | Bioorganic & Medicinal Chemistry Letters | 2012 | 5 Pages |
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.
Related Topics
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Authors
Rong Jiang, Xinyi Song, Purva Bali, Anthony Smith, Claudia Ruiz Bayona, Li Lin, Michael D. Cameron, Patricia H. McDonald, Paul J. Kenny, Theodore M. Kamenecka,