Abstract
The synthesis and biological evaluation of a series of substituted dipiperidine alcohols are described. Structure-activity relationship studies led to the discovery of potent CCR2 antagonists displaying IC(50) values in the nanomolar or subnanomolar range. The cinnamoyl compounds had higher binding affinities than the corresponding urea analogs.
MeSH terms
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Alcohols / chemical synthesis
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Alcohols / chemistry
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Alcohols / pharmacology*
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Binding Sites
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Drug Evaluation, Preclinical
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Humans
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Inhibitory Concentration 50
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Molecular Structure
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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 / antagonists & inhibitors*
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Stereoisomerism
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Structure-Activity Relationship
Substances
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Alcohols
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Piperidines
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Receptors, CCR2