کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
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1368586 | 981704 | 2016 | 4 صفحه PDF | دانلود رایگان |
Poor pharmacokinetic stability is one of the issues of O-glucoside SGLT2 inhibitors in clinical trials, hence C-glucoside inhibitors have been developed and extensively applied. Herein, we provided an alternative approach to improve the pharmacokinetic stability of such inhibitors. Nine derivatives of Sergliflozin-A with modifications on the O-glucoside fragment were prepared, among which the 4-O-methyl derivative exhibited similar pharmacodynamics potency in excreted glucose urine test. Most attractively, significantly increased pharmacokinetic stability was observed for 4-O-methyl derivative of O-glucosides. This work proved that modification on the O-glucoside fragment could be a promising approach to the future SGLT2 inhibitor design.
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Journal: Bioorganic & Medicinal Chemistry Letters - Volume 26, Issue 9, 1 May 2016, Pages 2170–2173