| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1373297 | Bioorganic & Medicinal Chemistry Letters | 2009 | 5 Pages |
Abstract
The synthesis of a series of tricyclic antagonists for the prostaglandin D2 receptor DP2 (CRTH2) is disclosed. The activities of the compounds were evaluated in a human DP2 binding assay and a human whole blood eosinophil shape change assay. Potential metabolic liabilities of the compounds were addressed through in vitro CYP studies. The lead compound was demonstrated to have efficacy in a mouse model of allergic rhinitis following oral dosing.
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Related Topics
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Organic Chemistry
Authors
Brian A. Stearns, Christopher Baccei, Gretchen Bain, Alex Broadhead, Ryan C. Clark, Heather Coate, Jilly F. Evans, Patrick Fagan, John H. Hutchinson, Christopher King, Catherine Lee, Daniel S. Lorrain, Peppi Prasit, Pat Prodanovich, Angelina Santini,