کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
10584790 | 981353 | 2014 | 12 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
The design and synthesis of novel SGLT2 inhibitors: C-glycosides with benzyltriazolopyridinone and phenylhydantoin as the aglycone moieties
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
چکیده انگلیسی
The sodium glucose co-transporter 2 (SGLT2) has received considerable attention in recent years as a target for the treatment of type 2 diabetes mellitus. This report describes the design, synthesis and structure-activity relationship (SAR) of C-glycosides with benzyltriazolopyridinone and phenylhydantoin as the aglycone moieties as novel SGLT2 inhibitors. Compounds 5p and 33b demonstrated high potency in inhibiting SGLT2 and high selectivity against SGLT1. The in vitro ADMET properties of these compounds will also be discussed.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry - Volume 22, Issue 13, 1 July 2014, Pages 3414-3422
Journal: Bioorganic & Medicinal Chemistry - Volume 22, Issue 13, 1 July 2014, Pages 3414-3422
نویسندگان
Cheng Guo, Min Hu, Russell J. DeOrazio, Alexander Usyatinsky, Kevin Fitzpatrick, Zhenjun Zhang, Jun-Ho Maeng, Douglas B. Kitchen, Susan Tom, Michele Luche, Yuri Khmelnitsky, Andrew J. Mhyre, Peter R. Guzzo, Shuang Liu,