کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1371536 | 981847 | 2014 | 5 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Piperazinyl-oxadiazoles as selective sphingosine-1-phosphate receptor agonists
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موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
چکیده انگلیسی
The discovery of a new series of selective S1P1 agonists is described. This series of piperazinyl-oxadiazole derivatives was rapidly optimized starting from high-throughput screening hit 1 to afford potent and selective lead compound 10d. Further SAR studies showed that 10d was converted to the active phosphate metabolite 29 in vivo. Oral administration of compound 10d to rats was shown to induce lymphopenia at 3 mg/kg.
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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 24, Issue 20, 15 October 2014, Pages 4807–4811
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 24, Issue 20, 15 October 2014, Pages 4807–4811
نویسندگان
Joshua C. Horan, Sulagna Sanyal, Younggi Choi, Melissa Hill-Drzewi, Lori Patnaude, Shawn Anderson, Steve Fogal, Can Mao, Brian N. Cook, Kristina Gueneva-Boucheva, Michael B. Fisher, Eugene Hickey, Edward Pack, Lynne C. Bannen, Diva S. Chan,