Abstract
The design, synthesis, and structure-activity relationship development of naphthalene-derived human CCR8 antagonists is described. In vitro binding assay results of these investigations are reported, critical interactions of the antagonists with CCR8 are defined, and preliminary physicochemical and pharmacokinetic data for the naphthalene scaffold are presented.
MeSH terms
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Administration, Oral
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Animals
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Biological Availability
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Biological Transport
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Calcium / metabolism
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Cell Line
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Cricetinae
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Cricetulus
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Drug Design
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Humans
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Naphthalenes / chemical synthesis*
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Naphthalenes / pharmacokinetics
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Naphthalenes / pharmacology
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Rats
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Receptors, CCR8
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Receptors, Chemokine / antagonists & inhibitors*
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Solubility
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Stereoisomerism
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Structure-Activity Relationship
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Sulfonamides / chemical synthesis*
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Sulfonamides / pharmacokinetics
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Sulfonamides / pharmacology
Substances
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CCR8 protein, human
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Naphthalenes
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Receptors, CCR8
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Receptors, Chemokine
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Sulfonamides
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Calcium