| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1378665 | Bioorganic & Medicinal Chemistry Letters | 2006 | 4 Pages |
Abstract
Herein, we report the discovery of an effective strategy to modulate liabilities related to affinity of previously disclosed bicyclohexane MCHR-1 antagonists for the hERG channel. This paper describes one of several strategies incorporated to limit hERG binding via modifications of a terminal aryl group in an otherwise promising bicyclohexyl urea series.
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Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
![Bicyclo[3.1.0]hexyl urea melanin concentrating hormone (MCH) receptor-1 antagonists: Impacting hERG liability via aryl modifications](/preview/png/1378665.png "First Page Preview: Bicyclo[3.1.0]hexyl urea melanin concentrating hormone (MCH) receptor-1 antagonists: Impacting hERG liability via aryl modifications")
Authors
Mark D. McBriar, Henry Guzik, Sherry Shapiro, Ruo Xu, Jaroslava Paruchova, John W. Clader, Kim O’Neill, Brian Hawes, Steve Sorota, Michael Margulis, Kristal Tucker, Daniel J. Weston, Kathleen Cox,