Abstract
We report the discovery of novel histamine H(3) receptor antagonists based on 4-[(1H-imidazol-4-yl)methyl]piperidine. The most potent compounds in the series (e.g., 7) result from the attachment of a substituted aniline amide to the main pharmacophore piperidine via a two-methylene linker.
MeSH terms
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Cytochrome P-450 CYP2D6 Inhibitors
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Drug Evaluation, Preclinical
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Histamine Antagonists / chemical synthesis
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Histamine Antagonists / chemistry
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Histamine Antagonists / pharmacology*
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Humans
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Imidazoles / chemical synthesis
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Imidazoles / chemistry
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Imidazoles / pharmacology*
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In Vitro Techniques
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Molecular Structure
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Piperidines / chemical synthesis
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Piperidines / chemistry
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Piperidines / pharmacology*
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Receptors, Histamine H3 / drug effects*
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Structure-Activity Relationship
Substances
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Cytochrome P-450 CYP2D6 Inhibitors
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Histamine Antagonists
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Imidazoles
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Piperidines
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Receptors, Histamine H3
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4-(1H-imidazol-4-ylmethyl)piperidine