کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1374415 981918 2006 6 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Identification of an indole series of prostaglandin D2 receptor antagonists
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Identification of an indole series of prostaglandin D2 receptor antagonists
چکیده انگلیسی

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

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 16, Issue 11, 1 June 2006, Pages 3043–3048
نویسندگان
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