کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1374415 | 981918 | 2006 | 6 صفحه PDF | دانلود رایگان |

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.
A novel indole series of PGD2 receptor (DP receptor) antagonists are presented. Optimization led to the identification of the potent and selective DP receptor antagonists 35 and 36.Figure optionsDownload as PowerPoint slide
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 16, Issue 11, 1 June 2006, Pages 3043–3048