2. Academic Validation
  3. 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
Affiliations

Affiliation

  • 1 Amira Pharmaceuticals, San Diego, CA 92121, USA. brian.stearns@amirapharm.com
PMID: 19608418 DOI: 10.1016/j.bmcl.2009.06.085
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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