Abstract
Sulfonamides derived from 4(5)-(omega-aminoalkyl)-1H-imidazoles containing chain lengths of three- to five-carbons were synthesized. Good to moderate H3 receptor binding affinities were observed for several butyl and pentyl homologs, whereas binding affinities were considerably weaker in the propyl series. Separation of the imidazole ring and the sulfonamide unit by a four- or five-carbon tether afforded potent H3 receptor antagonists.
MeSH terms
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Animals
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Brain / metabolism
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Cell Membrane / metabolism
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Drug Design
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Guinea Pigs
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Histamine / analogs & derivatives*
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Histamine / chemical synthesis
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Histamine / chemistry
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Histamine / pharmacology
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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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Kinetics
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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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Receptors, Histamine H3 / physiology*
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Structure-Activity Relationship
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Sulfonamides / chemical synthesis*
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Sulfonamides / chemistry
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Sulfonamides / pharmacology
Substances
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Histamine Antagonists
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Piperidines
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Receptors, Histamine H3
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Sulfonamides
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Histamine
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thioperamide