کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1373179 | 981891 | 2011 | 4 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Synthesis of N-alkylated noeurostegines and evaluation of their potential as treatment for Gaucher’s disease
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موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
![عکس صفحه اول مقاله: Synthesis of N-alkylated noeurostegines and evaluation of their potential as treatment for Gaucher’s disease Synthesis of N-alkylated noeurostegines and evaluation of their potential as treatment for Gaucher’s disease](/preview/png/1373179.png)
چکیده انگلیسی
The potent and selective inhibitor of β-glucosidases, noeurostegine, was evaluated as an inhibitor of glucocerebrosidase (GCase) to give an IC50 value of 0.4 μM, being 250- and 150-fold better than N-butyl and N-nonyl noeurostegine, respectively. The parent noeurostegine and its N-butyl and N-nonyl alkylated congeners were also tested as pharmacological chaperones against a N370S GCase mutant. Of these, only noeurostegine, was found to increase enzyme activity, which in potency was comparable to that previously reported for isofagomine.
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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 21, Issue 5, 1 March 2011, Pages 1519–1522
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 21, Issue 5, 1 March 2011, Pages 1519–1522
نویسندگان
Tina S. Rasmussen, Sarah Allman, Gabriele Twigg, Terry D. Butters, Henrik H. Jensen,