Abstract
This communication reports SARs for the first orexin-1 receptor antagonist series of 1-aryl-3-quinolin-4-yl and 1-aryl-3-naphthyridin-4-yl ureas. One of these compounds, 31 (SB-334867), has excellent selectivity for the orexin-1 receptor, blood-brain barrier permeability and shows in vivo activity following ip dosing.
MeSH terms
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Animals
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Benzoxazoles / chemical synthesis
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Benzoxazoles / pharmacology*
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Blood-Brain Barrier*
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CHO Cells
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Central Nervous System / metabolism
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Cricetinae
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Humans
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Indoles / chemistry
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Infusions, Intravenous
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Naphthyridines / chemical synthesis
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Naphthyridines / pharmacokinetics*
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Orexin Receptors
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Permeability
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Quinolines / chemistry
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Receptors, G-Protein-Coupled
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Receptors, Neuropeptide / antagonists & inhibitors*
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Sensitivity and Specificity
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Structure-Activity Relationship
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Urea / analogs & derivatives*
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Urea / chemical synthesis
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Urea / pharmacology*
Substances
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1-(2-methylbenzoxazol-6-yl)-3-(1,5)naphthyridin-4-yl urea
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Benzoxazoles
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Indoles
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Naphthyridines
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Orexin Receptors
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Quinolines
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Receptors, G-Protein-Coupled
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Receptors, Neuropeptide
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indole
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Urea
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quinoline