1. Academic Validation
  2. Novel tricyclic antagonists of the prostaglandin D2 receptor DP2 with efficacy in a murine model of allergic rhinitis

Novel tricyclic antagonists of the prostaglandin D2 receptor DP2 with efficacy in a murine model of allergic rhinitis

  • Bioorg Med Chem Lett. 2009 Aug 15;19(16):4647-51. doi: 10.1016/j.bmcl.2009.06.085.
Brian A Stearns 1 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 Jill M Scott Nicholas S Stock Yen P Truong
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Affiliation

Abstract

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.

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