國家衛生研究院 NHRI:Item 3990099045/11509
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    题名: Synthesis and biological evaluation of N-glucosyl indole derivatives as sodium-dependent glucose co-transporter 2 inhibitors
    作者: Chu, KF;Song, JS;Chen, CT;Yeh, TK;Hsieh, TC;Huang, CY;Wang, MH;Wu, SH;Yao, CH;Chao, YS;Lee, JC
    贡献者: Institute of Biotechnology and Pharmaceutical Research
    摘要: Sodium-dependent glucose co-transporter 2 (SGLT2) inhibition has been demonstrated to efficiently control hyperglycemia via an insulin secretion-independent pathway. The unique mode of action eliminates the risk of hypoglycemia and makes SGLT2 inhibitors an attractive option for the treatment of type 2 diabetes. In a continuation of our previous studies on SGLT2 inhibitors bearing different sugar moieties, sixteen new N-glucosyl indole derivatives were designed, synthesized, and evaluated for their inhibitory activity against hSGLT2. Of these sixteen, acethydrazide-containing N-glucosyl indole 9d was found to be the most potent SGLT2 inhibitor, and caused a significant elevation in urine glucose excretion in rats at 50mg/kg, relative to the vehicle control.
    日期: 2019-03
    關聯: Bioorganic Chemistry. 2019 Mar;83:520-525.
    Link to: http://dx.doi.org/10.1016/j.bioorg.2018.11.006
    JIF/Ranking 2023: http://gateway.webofknowledge.com/gateway/Gateway.cgi?GWVersion=2&SrcAuth=NHRI&SrcApp=NHRI_IR&KeyISSN=0045-2068&DestApp=IC2JCR
    Cited Times(WOS): https://www.webofscience.com/wos/woscc/full-record/WOS:000458609100053
    Cited Times(Scopus): https://www.scopus.com/inward/record.url?partnerID=HzOxMe3b&scp=85056762960
    显示于类别:[李靜琪] 期刊論文
    [趙宇生(2002-2013)] 期刊論文
    [葉燈光] 期刊論文
    [陳炯東] 期刊論文

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