Literature DB >> 22018463

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

Seong Heon Kim1, Gopinadhan N Anilkumar, Lisa Guise Zawacki, Qingbei Zeng, De-Yi Yang, Yuefei Shao, Guizhen Dong, Xiaolian Xu, Wensheng Yu, Yueheng Jiang, Chung-Her Jenh, James W Hall, Carolyn Diianni Carroll, Doug W Hobbs, John J Baldwin, Brian F McGuinness, Stuart B Rosenblum, Joseph A Kozlowski, Bandarpalle B Shankar, Neng-Yang Shih.   

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. Copyright Â
© 2011 Elsevier Ltd. All rights reserved.

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Year:  2011        PMID： 22018463     DOI： 10.1016/j.bmcl.2011.09.120

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  5 in total

1.  Insertion of arynes into N-halo bonds: a direct approach to o-haloaminoarenes.

Authors:  Charles E Hendrick; Stacey L McDonald; Qiu Wang
Journal:  Org Lett       Date:  2013-06-24       Impact factor: 6.005

2.  Amiloride as a new RNA-binding scaffold with activity against HIV-1 TAR.

Authors:  Neeraj N Patwardhan; Laura R Ganser; Gary J Kapral; Christopher S Eubanks; Janghyun Lee; Bharathwaj Sathyamoorthy; Hashim M Al-Hashimi; Amanda E Hargrove
Journal:  Medchemcomm       Date:  2017-03-15       Impact factor: 3.597

3.  A selective and potent CXCR3 antagonist SCH 546738 attenuates the development of autoimmune diseases and delays graft rejection.

Authors:  Chung-Her Jenh; Mary Ann Cox; Long Cui; Eva-Pia Reich; Lee Sullivan; Shu-Cheng Chen; David Kinsley; Shiguang Qian; Seong Heon Kim; Stuart Rosenblum; Joseph Kozlowski; Jay S Fine; Paul J Zavodny; Daniel Lundell
Journal:  BMC Immunol       Date:  2012-01-10       Impact factor: 3.615

4.  Metabolic profiling of ligands for the chemokine receptor CXCR3 by liquid chromatography-mass spectrometry coupled to bioaffinity assessment.

Authors:  Marija Mladic; Danny J Scholten; Maikel Wijtmans; David Falck; Rob Leurs; Wilfried M A Niessen; Martine J Smit; Jeroen Kool
Journal:  Anal Bioanal Chem       Date:  2015-07-12       Impact factor: 4.142

5.  Ligand activation induces different conformational changes in CXCR3 receptor isoforms as evidenced by plasmon waveguide resonance (PWR).

Authors:  K Boyé; C Billottet; N Pujol; I D Alves; A Bikfalvi
Journal:  Sci Rep       Date:  2017-09-06       Impact factor: 4.379
  5 in total

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