Abstract
A series of 2-arylbenzimidazoles was synthesized and found to bind with high affinity to the human histamine H(4) receptor. Structure-activity relationships were investigated through library preparation and evaluation as well as traditional medicinal chemistry approaches, leading to the discovery of compounds with single-digit nanomolar affinity for the H(4) receptor.
MeSH terms
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Aldehydes / chemistry
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Amines / chemistry
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Benzimidazoles / chemical synthesis*
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Benzimidazoles / chemistry
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Benzimidazoles / metabolism*
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Catalysis
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Computer Simulation
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Histamine / metabolism
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Humans
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Ligands
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Models, Molecular
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Molecular Structure
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Protein Binding
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Receptors, G-Protein-Coupled / chemistry
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Receptors, G-Protein-Coupled / metabolism*
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Receptors, Histamine / chemistry
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Receptors, Histamine / metabolism*
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Receptors, Histamine H4
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Structure-Activity Relationship
Substances
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Aldehydes
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Amines
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Benzimidazoles
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HRH4 protein, human
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Ligands
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Receptors, G-Protein-Coupled
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Receptors, Histamine
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Receptors, Histamine H4
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Histamine