کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1374570 | 981921 | 2010 | 6 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Stereochemistry–activity relationship of orally active tetralin S1P agonist prodrugs
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
چکیده انگلیسی
Modifying FTY720, an immunosuppressant modulator, led to a new series of well phosphorylated tetralin analogs as potent S1P1 receptor agonists. The stereochemistry effect of tetralin ring was probed, and (−)-(R)-2-amino-2-((S)-6-octyl-1,2,3,4-tetrahydronaphthalen-2-yl)propan-1-ol was identified as a good SphK2 substrate and potent S1P1 agonist with good oral bioavailability.
The synthesis, characterization and stereochemistry activity relationship of tetralin S1P agonist prodrugs is reported. (2R,2′S)-5 (ED50 = 0.1 mg/kg) was identified as a good SphK2 substrate and potent S1P1 agonist with good oral bioavailability.Figure optionsDownload as PowerPoint slide
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 20, Issue 7, 1 April 2010, Pages 2264–2269
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 20, Issue 7, 1 April 2010, Pages 2264–2269
نویسندگان
Bin Ma, Kevin M. Guckian, Edward Yin-Shiang Lin, Wen-Cherng Lee, Daniel Scott, Gnanasambandam Kumaravel, Timothy L. Macdonald, Kevin R. Lynch, Cheryl Black, Sowmya Chollate, Kyungmin Hahm, Gregg Hetu, Ping Jin, Yi Luo, Ellen Rohde, Anthony Rossomando,