|
|||||
|
|
The discovery of novel cyclohexylamide CCR2 antagonists |
|
| Authors: | Lanter James C Markotan Thomas P Zhang Xuqing Subasinghe Nalin Kang Fu-An Hou Cuifen Singer Monica Opas Evan McKenney Sandra Crysler Carl Johnson Dana Molloy Christopher J Sui Zhihua |
| Institution: | Johnson & Johnson Pharmaceutical Research and Development, Welsh & McKean Roads, Spring House, PA 19002, USA |
| 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. |
| Keywords: | CCR2 Antagonist MCP-1 hERG |
| 本文献已被 ScienceDirect PubMed 等数据库收录！ | |