Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1375785 | Bioorganic & Medicinal Chemistry Letters | 2008 | 5 Pages |
Abstract
A new series of indole-based antagonists of the PGD2 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 Ki value of 1 nM for the DP1 receptor and an IC50 value of 4.6 nM in a DP1 functional assay for the inhibition of the PGD2 induced cAMP production in platelet rich plasma (PRP).
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Christian Beaulieu, Daniel Guay, Zhaoyin Wang, Yves Leblanc, Patrick Roy, Claude Dufresne, Robert Zamboni, Carl Berthelette, Stephen Day, Nancy Tsou, Danielle Denis, Gillian Greig, Marie-Claude Mathieu, Gary O’Neill,