Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10587910 | Bioorganic & Medicinal Chemistry Letters | 2013 | 4 Pages |
Abstract
A novel series of CCR1 antagonists based on the 1-(4-phenylpiperazin-1-yl)-2-(1H-pyrazol-1-yl)ethanone scaffold was identified by screening a compound library utilizing CCR1-expressing human THP-1 cells. SAR studies led to the discovery of the highly potent and selective CCR1 antagonist 14 (CCR1 binding IC50Â =Â 4Â nM using [125I]-CCL3 as the chemokine ligand). Compound 14 displayed promising pharmacokinetic and toxicological profiles in preclinical species.
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Authors
Andrew M.K. Pennell, James B. Aggen, Subhabrata Sen, Wei Chen, Yuan Xu, Edward Sullivan, Lianfa Li, Kevin Greenman, Trevor Charvat, Derek Hansen, Daniel J. Dairaghi, J.J. Kim Wright, Penglie Zhang,