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Bioorg Med Chem Lett. 2011 Mar 1;21(5):1527-31. doi: 10.1016/j.bmcl.2010.12.114. Epub 2010 Dec 28.

II. SAR studies of pyridyl-piperazinyl-piperidine derivatives as CXCR3 chemokine antagonists.

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  • 1Ligand Pharmaceuticals, Cranbury, NJ 08512, USA.


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.

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