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Bioorg Med Chem Lett. 2011 Dec 1;21(23):6982-6. doi: 10.1016/j.bmcl.2011.09.120. Epub 2011 Oct 5.

III. Identification of novel CXCR3 chemokine receptor antagonists with a pyrazinyl-piperazinyl-piperidine scaffold.

Author information

1
Merck Research Laboratories, Kenilworth, NJ 07033, USA. seong.heon.kim@merck.com

Abstract

The SAR of a novel pyrazinyl-piperazinyl-piperidine scaffold with CXCR3 receptor antagonist activity was explored. Optimization of the DMPK profile and reduction of hERG inhibition is described. Compound 16e with single-digit CXCR3 affinity, good rat PK and hERG profiles has been identified as a lead for further study.

PMID:
22018463
DOI:
10.1016/j.bmcl.2011.09.120
[Indexed for MEDLINE]

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