Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 19, Issue 16, Pages 4647-4651Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2009.06.085
Keywords
CRTH2; DP2; Prostaglandin D2; Antagonist; Allergic rhinitis; Mouse sneeze; Binding; Eosinophil; Shape change; Azaindole
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The synthesis of a series of tricyclic antagonists for the prostaglandin D(2) 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. (C) 2009 Elsevier Ltd. All rights reserved.
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