کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
5222995 | 1383473 | 2009 | 8 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Synthesis and in vitro evaluation of botryllazine B analogues as a new class of inhibitor against human aldose reductase
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
![عکس صفحه اول مقاله: Synthesis and in vitro evaluation of botryllazine B analogues as a new class of inhibitor against human aldose reductase Synthesis and in vitro evaluation of botryllazine B analogues as a new class of inhibitor against human aldose reductase](/preview/png/5222995.png)
چکیده انگلیسی
Botryllazine B analogues of diverse substitution patterns have been prepared, and their in vitro inhibitory activities against recombinant human aldose reductase (h-ALR2) evaluated. Among the 15 compounds tested, 6-(4-aminophenyl)-2-(4-hydroxyphenyl)carbonylpyrazine (7b) proved to be the most potent inhibitor, with IC50=0.91 μM. Kinetic analyses of 7b and botryllazine B (1) revealed that these inhibitors exhibit an unprecedented mixed-type inhibition on h-ALR2 with respect to the substrate d,l-glyceraldehyde, in the presence of NADPH at inhibitor concentrations near the IC50 values.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Tetrahedron - Volume 65, Issue 15, 11 April 2009, Pages 3019-3026
Journal: Tetrahedron - Volume 65, Issue 15, 11 April 2009, Pages 3019-3026
نویسندگان
Ryota Saito, Mai Tokita, Keisuke Uda, Chikako Ishikawa, Mitsutoshi Satoh,