Abstract
A series of novel tetrahydronaphthyridine-based histamine H(3) ligands that have serotonin reuptake transporter inhibitor activity is described. The 1,2,3,4-tetrahydro-2,6-naphthyridine scaffold is assembled via the addition of a nitrostyrene to a metalated pyridine followed by reduction and cyclization to form the naphthyridine. In vitro biological data for these novel compounds are discussed.
MeSH terms
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Animals
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Chemistry, Pharmaceutical / methods*
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Drug Design
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Histamine / chemistry*
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Histamine Antagonists / chemical synthesis*
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Histamine Antagonists / pharmacology*
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Humans
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Models, Chemical
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Molecular Conformation
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Naphthyridines / chemical synthesis*
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Naphthyridines / pharmacology
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Rats
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Receptors, Histamine H3 / chemistry*
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Selective Serotonin Reuptake Inhibitors / chemical synthesis*
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Selective Serotonin Reuptake Inhibitors / pharmacology
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Serotonin / metabolism
Substances
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Histamine Antagonists
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Naphthyridines
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Receptors, Histamine H3
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Serotonin Uptake Inhibitors
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Serotonin
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Histamine