國家衛生研究院 NHRI:Item 3990099045/9641
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    题名: N-Indolylglycosides bearing modifications at the glucose C6-Position as Sodium-Dependent Glucose Co-transporter 2 inhibitors
    作者: Chu, KF;Yao, CH;Song, JS;Chen, CT;Yeh, TK;Hsieh, TC;Huang, CY;Wang, MH;Wu, SH;Chang, WE;Chao, YS;Lee, JC
    贡献者: Institute of Biotechnology and Pharmaceutical Research
    摘要: Suppression of glucose reabsorption through the inhibition of sodium-dependent glucose co-transporter 2 (SGLT2) is a promising therapeutic approach for the treatment of type 2 diabetes. To investigate the effect of C6-substitution on inhibition of SGLT2 by N-indolylglucosides, a small library of 6-triazole, 6-amide, 6-urea, and 6-thiourea N-indolylglycosides were synthesized and tested. A detailed structure-activity relationship (SAR) study culminated in the identification of 6-amide derivatives 6a and 6o as potent SGLT2 inhibitors, which were further tested for inhibitory activity against SGLT1. The data obtained indicated that 6a and 6o are mildly to moderately selective for SGLT2 over SGLT1. Both compounds were also evaluated in a urinary glucose excretion test and pharmacokinetic study; 6a was found capable of inducing urinary glucose excretion in normal SD rats.
    日期: 2016-05
    關聯: Bioorganic and Medicinal Chemistry. 2016 May;24(10):2242-2250.
    Link to: http://dx.doi.org/10.1016/j.bmc.2016.03.058
    JIF/Ranking 2023: http://gateway.webofknowledge.com/gateway/Gateway.cgi?GWVersion=2&SrcAuth=NHRI&SrcApp=NHRI_IR&KeyISSN=0968-0896&DestApp=IC2JCR
    Cited Times(WOS): https://www.webofscience.com/wos/woscc/full-record/WOS:000374332500007
    Cited Times(Scopus): http://www.scopus.com/inward/record.url?partnerID=HzOxMe3b&scp=84962838931
    显示于类别:[李靜琪] 期刊論文
    [葉燈光] 期刊論文
    [趙宇生(2002-2013)] 期刊論文
    [陳炯東] 期刊論文

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