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Bioorg Med Chem Lett. 2011 Nov 1;21(21):6608-12. doi: 10.1016/j.bmcl.2011.01.024. Epub 2011 Jan 11.

Discovery and optimization of a biphenylacetic acid series of prostaglandin D2 receptor DP2 antagonists with efficacy in a murine model of allergic rhinitis.

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Amira Pharmaceuticals, 9535 Waples Street, Suite 100, San Diego, CA 92121, USA.


Biphenylacetic acid (5) was identified through a library screen as an inhibitor of the prostaglandin D(2) receptor DP2 (CRTH2). Optimization for potency and pharmacokinetic properties led to a series of selective CRTH2 antagonists. Compounds demonstrated potency in a human DP2 binding assay and a human whole blood eosinophil shape change assay, as well as good oral bioavailability in rat and dog, and efficacy in a mouse model of allergic rhinitis following oral dosing.

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