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Bioorg Med Chem Lett. 2009 Sep 1;19(17):5205-8. doi: 10.1016/j.bmcl.2009.07.020. Epub 2009 Jul 9.

Novel CXCR3 antagonists with a piperazinyl-piperidine core.

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  • 1Ligand Pharmaceuticals, 3000 Eastpark Boulevard, Cranbury, NJ 08512, USA.


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.

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