کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1375785 981944 2008 5 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Identification of prostaglandin D2 receptor antagonists based on a tetrahydropyridoindole scaffold
کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Identification of prostaglandin D2 receptor antagonists based on a tetrahydropyridoindole scaffold
چکیده انگلیسی

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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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 18, Issue 8, 15 April 2008, Pages 2696–2700
نویسندگان
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