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Bioorg Med Chem Lett. 2008 Apr 15;18(8):2696-700. doi: 10.1016/j.bmcl.2008.03.015. Epub 2008 Mar 10.

Identification of prostaglandin D2 receptor antagonists based on a tetrahydropyridoindole scaffold.

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  • 1Department of Medicinal Chemistry, Merck Frosst Canada & Co., 16711 Trans Canada Hwy, Kirkland, Que., Canada. christian_beaulieu@merck.com


A new series of indole-based antagonists of the PGD(2) receptor subtype 1 (DP1 receptor) was identified and the progress of the structure-activity relationship study to the identification of potent and selective antagonists is presented. Selective DP1 antagonists with high potency and selectivity were prepared. Of particular interest is the DP1 antagonist 26 with a K(i) value of 1 nM for the DP1 receptor and an IC(50) value of 4.6 nM in a DP1 functional assay for the inhibition of the PGD(2) induced cAMP production in platelet rich plasma (PRP).

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