Abstract
A series of 2-(1,4'-bipiperidine-1'-yl)thiazolopyridines was synthesized and evaluated as a new lead of non-imidazole histamine H(3) receptor antagonists. Introduction of diversity at the 6-position of the pyridine ring was designed to enhance in vitro potency and decrease hERG activity. The structure-activity relationships for these new thiazolopyridine antagonists are discussed.
MeSH terms
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Animals
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Haplorhini
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Histamine Antagonists / chemical synthesis
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Histamine Antagonists / chemistry*
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Histamine Antagonists / pharmacokinetics
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Humans
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Mice
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Mice, Inbred ICR
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Microsomes, Liver / metabolism
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Pyridines / chemical synthesis
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Pyridines / chemistry*
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Pyridines / pharmacokinetics
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Rats
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Receptors, Histamine H3 / chemistry*
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Receptors, Histamine H3 / metabolism
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Recombinant Proteins / chemistry
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Recombinant Proteins / metabolism
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Structure-Activity Relationship
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Trans-Activators / metabolism
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Transcriptional Regulator ERG
Substances
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ERG protein, human
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Histamine Antagonists
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Pyridines
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Receptors, Histamine H3
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Recombinant Proteins
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Trans-Activators
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Transcriptional Regulator ERG