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Disubstituted piperidines as potent orexin (hypocretin) receptor antagonists.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2012 Jun 15; Vol. 22 (12), pp. 3890-4. Date of Electronic Publication: 2012 May 04. - Publication Year :
- 2012
-
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.<br /> (Copyright © 2012 Elsevier Ltd. All rights reserved.)
- Subjects :
- Animals
Antipsychotic Agents pharmacokinetics
Brain drug effects
Brain metabolism
Humans
Liver drug effects
Liver metabolism
Mice
Microsomes, Liver drug effects
Microsomes, Liver metabolism
Molecular Structure
Orexin Receptors
Piperidines pharmacokinetics
Rats
Receptors, G-Protein-Coupled metabolism
Receptors, Neuropeptide metabolism
Structure-Activity Relationship
Substance-Related Disorders drug therapy
Antipsychotic Agents chemical synthesis
Piperidines chemical synthesis
Receptors, G-Protein-Coupled antagonists & inhibitors
Receptors, Neuropeptide antagonists & inhibitors
Subjects
Details
- Language :
- English
- ISSN :
- 1464-3405
- Volume :
- 22
- Issue :
- 12
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 22617492
- Full Text :
- https://doi.org/10.1016/j.bmcl.2012.04.122