Abstract
The preparation and biological evaluation of a series of indolopiperidine CCR2B receptor antagonists possessing a conformationally restricted C-5 linker chain in combination with a restricted piperidine ring are described. Compared to the parent compound 1, analogue 8 shows a dramatic improvement in selectivity against a range of 5-HT and dopaminergic receptors.
MeSH terms
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Dopamine Antagonists / chemical synthesis
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Dopamine Antagonists / chemistry
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Dopamine Antagonists / pharmacology
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Indoles / chemical synthesis
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Indoles / chemistry
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Indoles / pharmacology*
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Molecular Conformation
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Piperidines / chemical synthesis
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Piperidines / chemistry
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Piperidines / pharmacology*
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Receptors, CCR2
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Receptors, Chemokine / antagonists & inhibitors*
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Receptors, Chemokine / metabolism
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Serotonin Antagonists / chemical synthesis
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Serotonin Antagonists / chemistry
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Serotonin Antagonists / pharmacology
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Structure-Activity Relationship
Substances
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Dopamine Antagonists
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Indoles
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Piperidines
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Receptors, CCR2
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Receptors, Chemokine
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Serotonin Antagonists
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indolopiperidine