کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1363546 | 981515 | 2010 | 5 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Synthesis and structure–activity relationships of a series of 3-aryl-4-isoxazolecarboxamides as a new class of TGR5 agonists
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موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله

چکیده انگلیسی
A series of 3-aryl-4-isoxazolecarboxamides identified from a high-throughput screening campaign as novel, potent agonists of the human TGR5 G-protein-coupled receptor is described. Many analogues were readily accessible via solution-phase synthesis which resulted in the rapid identification of key structure–activity relationships (SAR), and the discovery of potent exemplars (up to pEC50 = 9). Details of the SAR and optimization of this series are presented herein.
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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 20, Issue 4, 15 February 2010, Pages 1363–1367
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 20, Issue 4, 15 February 2010, Pages 1363–1367
نویسندگان
Brian W. Budzik, Karen A. Evans, David D. Wisnoski, Jian Jin, Ralph A. Rivero, George R. Szewczyk, Channa Jayawickreme, David L. Moncol, Hongshi Yu,