Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10588317 | Bioorganic & Medicinal Chemistry Letters | 2012 | 5 Pages |
Abstract
A novel N-aryl piperazine-1-carboxamide series of human CCR2 chemokine receptor antagonists was discovered. Early analogues were potent at CCR2 but also inhibited the hERG cardiac ion channel. Structural modifications which decreased lipophilicity and basicity resulted in the identification of a sub-series with an improved margin over hERG. The pharmacological and pharmacokinetic properties of the lead compound from this series, N-(3,4-dichlorophenyl)-4-[(2R)-4-isopropylpiperazine-2-carbonyl]piperazine-1-carboxamide, are described.
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Authors
John G. Cumming, Justin F. Bower, David Waterson, Alan Faull, Philip J. Poyser, Paul Turner, Benjamin McDermott, Andrew D. Campbell, Julian Hudson, Michael James, Jon Winter, Christine Wood,