Abstract
A series of non-imidazole histamine H(3) receptor antagonists based on the (3-phenoxypropyl)amine motif, which is a common pharmacophore for H(3) antagonists, has been identified. A preliminary SAR study around the amine moiety has identified 8a as a potent H(3) antagonist possessing a good pharmacokinetic profile in the rat.
MeSH terms
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Amines / chemical synthesis*
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Amines / chemistry
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Amines / pharmacology*
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Animals
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Benzimidazoles / chemical synthesis*
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Benzimidazoles / chemistry
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Benzimidazoles / pharmacology*
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Combinatorial Chemistry Techniques
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Molecular Structure
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Rats
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Receptors, Histamine H3 / drug effects*
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Structure-Activity Relationship
Substances
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Amines
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Benzimidazoles
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Receptors, Histamine H3