Author/Authors :
Claudio F. Sturino، نويسنده , , Nicolas Lachance، نويسنده , , Michael Boyd، نويسنده , , Carl Berthelette، نويسنده , , Marc Labelle، نويسنده , , Lianhai Li، نويسنده , , Bruno Roy، نويسنده , , John Scheigetz، نويسنده , , Nancy Tsou، نويسنده , , Christine Brideau، نويسنده , , Elizabeth Cauchon، نويسنده , , Marie-Claude Carrière، نويسنده , , Danielle Denis، نويسنده , , Gillian Greig، نويسنده , , Stacia Kargman، نويسنده , , Sonia Lamontagne، نويسنده , , Marie-Claude Mathieu، نويسنده , , Nicole Sawyer، نويسنده , , Deborah Slipetz، نويسنده , , Gary O’Neill، نويسنده , , et al.، نويسنده ,
Abstract :
A novel indole series of PGD2 receptor (DP receptor) antagonists is presented. Optimization of this series led to the identification of potent and selective DP receptor antagonists. In particular, antagonists 35 and 36 were identified with Ki values of 2.6 and 1.8 nM, respectively. These two antagonists are also potent in a DP functional assay where they inhibit the PGD2 induced cAMP production in platelet rich plasma with IC50 values of 7.9 and 8.6 nM, respectively. The structure–activity relationships of this indole series of DP receptor antagonists will also be discussed.
Keywords :
Prostaglandin D2 , PGD2 , DP receptor antagonist , Indole
