کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1358093 | 981319 | 2014 | 11 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Synthesis and biological evaluation of all eight stereoisomers of DPP-IV inhibitor saxagliptin
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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 biological evaluation of all eight stereoisomers of DPP-IV inhibitor saxagliptin Synthesis and biological evaluation of all eight stereoisomers of DPP-IV inhibitor saxagliptin](/preview/png/1358093.png)
چکیده انگلیسی
All eight stereoisomers of saxagliptin have been synthesized and evaluated for their inhibitory activity against DPP-IV. It was unambiguously confirmed that the configuration of saxagliptin was critical to potent inhibition of DPP-IV. Docking study was performed to elucidate the configuration–activity relationship of saxagliptin stereoisomers. Tyr662 and Tyr470 have been suggested as the key residues of DPP-IV interacting with the inhibitors. This work provides valuable information for further inhibitor design against DPP-IV.
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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry - Volume 22, Issue 4, 15 February 2014, Pages 1383–1393
Journal: Bioorganic & Medicinal Chemistry - Volume 22, Issue 4, 15 February 2014, Pages 1383–1393
نویسندگان
Jizhe Dong, Yanchun Gong, Jun Liu, Xiangfeng Chen, Xiaoan Wen, Hongbin Sun,