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

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

  • Bioorg Med Chem Lett. 2011 Dec 1;21(23):6982-6. doi: 10.1016/j.bmcl.2011.09.120.
Seong Heon Kim 1,  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 3rd,  Carolyn Diianni Carroll,  Doug W Hobbs,  John J Baldwin,  Brian F McGuinness,  Stuart B Rosenblum,  Joseph A Kozlowski,  Bandarpalle B Shankar,  Neng-Yang Shih
Affiliations

Affiliation

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

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