| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1370175 | Bioorganic & Medicinal Chemistry Letters | 2011 | 6 Pages |
Abstract
As a result of further SAR studies on a piperidinyl piperidine scaffold, we report the discovery of compound 44, a potent, orally bioavailable CCR2 antagonist. While having some in vitro hERG activity, this molecule was clean in an in vivo model of QT prolongation. In addition, it showed excellent efficacy when dosed orally in a transgenic murine model of acute inflammation.
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
James C. Lanter, Thomas P. Markotan, Xuqing Zhang, Nalin Subasinghe, Fu-An Kang, Cuifen Hou, Monica Singer, Evan Opas, Sandra McKenney, Carl Crysler, Dana Johnson, Christopher J. Molloy, Zhihua Sui,