| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1372137 | Bioorganic & Medicinal Chemistry Letters | 2011 | 5 Pages |
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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Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Seong Heon Kim, 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 III, Carolyn DiIanni Carroll, Doug W. Hobbs, John J. Baldwin,