Abstract
The structure-human CXCR3 binding affinity relationship of a series of pyridyl-piperazinyl-piperidine derivatives was explored. The optimization campaign highlighted the pronounced effect of 2'-piperazine substitution on CXCR3 receptor affinity. Analog 18j, harboring a 2'(S)-ethylpiperazine moiety, exhibited a human CXCR3 IC(50) of 0.2 nM.
Copyright © 2011 Elsevier Ltd. All rights reserved.
MeSH terms
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Humans
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Inhibitory Concentration 50
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Molecular Structure
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Piperazine
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Piperazines / chemical synthesis*
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Piperazines / chemistry
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Piperazines / pharmacology
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Piperidines / chemical synthesis*
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Piperidines / chemistry
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Piperidines / pharmacology
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Pyridines / chemical synthesis*
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Pyridines / chemistry
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Pyridines / pharmacology
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Receptors, CXCR3 / agonists*
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Structure-Activity Relationship
Substances
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Piperazines
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Piperidines
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Pyridines
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Receptors, CXCR3
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Piperazine
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piperidine