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ID: ALA1921678
Journal: Bioorg Med Chem Lett
Title: The discovery of novel cyclohexylamide CCR2 antagonists.
Authors: Lanter JC, Markotan TP, Zhang X, Subasinghe N, Kang FA, Hou C, Singer M, Opas E, McKenney S, Crysler C, Johnson D, Molloy CJ, Sui Z.
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.
CiteXplore: 22061641