کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1379724 982037 2005 5 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Discovery of diphenylcarbamate derivatives as highly potent and selective IP receptor agonists: Orally active prostacyclin mimetics. Part 3
کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Discovery of diphenylcarbamate derivatives as highly potent and selective IP receptor agonists: Orally active prostacyclin mimetics. Part 3
چکیده انگلیسی

The new classes of diphenylcarbamate derivatives with a tetrahydronaphthalene skeleton as highly potent and selective IP agonists have been discovered. The optimized diphenylcarbamate type compound FK-788: (R)-4 exhibited potent antiaggregative potency with an IC50 of 18 nM and high binding affinity for the human recombinant IP receptor with Ki values of 20 nM and selectivity for human IP over all other members of the human prostanoid receptor family. Compound (R)-4 was shown to exhibit good pharmacokinetic properties in rats and dogs, and also good bioavailability in healthy volunteers.

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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 15, Issue 12, 15 June 2005, Pages 3091–3095
نویسندگان
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