886371-24-0Relevant articles and documents
Disubstituted piperidines as potent orexin (hypocretin) receptor antagonists
Jiang, Rong,Song, Xinyi,Bali, Purva,Smith, Anthony,Bayona, Claudia Ruiz,Lin, Li,Cameron, Michael D.,McDonald, Patricia H.,Kenny, Paul J.,Kamenecka, Theodore M.
scheme or table, p. 3890 - 3894 (2012/07/13)
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.