Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1370463 | Bioorganic & Medicinal Chemistry Letters | 2011 | 5 Pages |
Abstract
This report discloses the development of a series of tricyclic histamine H4 receptor antagonists. Starting with a low nanomolar benzofuranopyrimidine HTS hit devoid of pharmaceutically acceptable properties, we navigated issues with metabolism and solubility to furnish a potent, stable and water soluble tricyclic histamine H4 receptor antagonist with desirable physiochemical parameters which demonstrated efficacy a mouse ova model.
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Related Topics
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Authors
Brad M. Savall, Laurent Gomez, Frank Chavez, Michael Curtis, Steven P. Meduna, Aaron Kearney, Paul Dunford, Jeffery Cowden, Robin L. Thurmond, Cheryl Grice, James P. Edwards,