کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1371007 | 981834 | 2011 | 4 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
New indole amide derivatives as potent CRTH2 receptor antagonists
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موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
چکیده انگلیسی
A new series of indole amide acting as hCRTH2 receptor ligands had been explored and are described herein. Several amide derivatives displaying low nanomolar activity in hCRTH2 binding and whole blood assays were identified. They were found to behave as a full antagonists, exhibiting good selectivity over related prostaglandin receptors. Also, prototypical compounds in this novel series which displayed acceptable CYP profiles and were orally bioavailable in rats were identified.
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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 21, Issue 11, 1 June 2011, Pages 3471–3474
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 21, Issue 11, 1 June 2011, Pages 3471–3474
نویسندگان
Helmi Zaghdane, Michael Boyd, John Colucci, Daniel Simard, Carl Berthelette, Yves Leblanc, Zhaoyin Wang, Robert Houle, Jean François Lévesque, Carmela Molinaro, Martine Hamel, Rino Stocco, Nicole Sawyer, Susan Sillaots, François Gervais, Michel Gallant,