Format

Send to:

Choose Destination
See comment in PubMed Commons below
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.

Author information

  • 1Ligand Pharmaceuticals, Cranbury, NJ 08512, USA. joe.shao@primera-corp.com

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.

PMID:
21277198
[PubMed - indexed for MEDLINE]
PubMed Commons home

PubMed Commons

0 comments
How to join PubMed Commons

    Supplemental Content

    Full text links

    Icon for Elsevier Science
    Loading ...
    Write to the Help Desk