Abstract
High-throughput screening of an encoded combinatorial aryl piperazine library led to the identification of a novel series of potent piperazinyl-piperidine based CXCR3 antagonists. Analogs of the initial hit were synthesized via solid and solution phase methods to probe the influence of structure on the CXCR3 binding of these molecules. Various functional groups were found to contribute to the overall potency and essential molecular features were identified.
MeSH terms
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Anti-Inflammatory Agents / chemical synthesis
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Anti-Inflammatory Agents / chemistry*
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Anti-Inflammatory Agents / pharmacology
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Combinatorial Chemistry Techniques
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Humans
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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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Receptors, CXCR3 / antagonists & inhibitors*
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Receptors, CXCR3 / metabolism
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Structure-Activity Relationship
Substances
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Anti-Inflammatory Agents
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Piperazines
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Piperidines
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Receptors, CXCR3