期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 21, 期 24, 页码 7496-7501出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2011.09.113
关键词
CCR2 Antagonist; MCP-1; hERG
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. (C) 2011 Published by Elsevier Ltd.
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