Title of article
Identification of prostaglandin D2 receptor antagonists based on a tetrahydropyridoindole scaffold
Author/Authors
Christian Beaulieu، نويسنده , , Daniel Guay، نويسنده , , Zhaoyin Wang، نويسنده , , Yves Leblanc، نويسنده , , Patrick Roy، نويسنده , , Claude Dufresne، نويسنده , , Robert Zamboni، نويسنده , , Carl Berthelette، نويسنده , , Stephen Day، نويسنده , , Nancy Tsou، نويسنده , , Danielle Denis، نويسنده , , Gillian Greig، نويسنده , , Marie-Claude Mathieu، نويسنده , , Gary O’Neill، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2008
Pages
5
From page
2696
To page
2700
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).
Keywords
Prostanoid , Tetrahydropyridoindole , PGD2 antagonist , Indole , PGD2 receptor , DP1 antagonist
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2008
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
799433
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