کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1370402 981819 2011 5 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Substituted indole-1-acetic acids as potent and selective CRTh2 antagonists—discovery of AZD1981
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Substituted indole-1-acetic acids as potent and selective CRTh2 antagonists—discovery of AZD1981
چکیده انگلیسی

Novel indole-3-thio-, 3-sulfonyl- and 3-oxy-aryl-1-acetic acids are reported which are potent, selective antagonists of the chemoattractant receptor-homologous expressed on Th2 lymphocytes receptor (CRTh2 or DP2). Optimization required maintenance of high CRTh2 potency whilst achieving a concomitant reduction in rates of metabolism, removal of cyp p450 inhibition and minimization of aldose reductase and aldehyde reductase activity. High quality compounds suitable for in vivo studies are highlighted, culminating in the discovery of AZD1981 (22).

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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 21, Issue 21, 1 November 2011, Pages 6288–6292
نویسندگان
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