國家衛生研究院 NHRI:Item 3990099045/10914
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    题名: Identification of an oxime-containing C-glucosylarene as a potential inhibitor of sodium-dependent glucose co-transporter 2
    作者: Yuan, MC;Yeh, TK;Chen, CT;Song, JS;Huang, YC;Hsieh, TC;Huang, CY;Huang, YL;Wang, MH;Wu, SH;Yao, CH;Chao, YS;Lee, JC
    贡献者: Institute of Biotechnology and Pharmaceutical Research
    摘要: Treatment of hyperglycemia with drugs that block renal glucose reabsorption via inhibition of sodium-dependent glucose cotransporter 2 (SGLT2) is a novel approach to diabetes management. In this study, twenty-seven aryl C-glycosides bearing a C=N/C−N linkage at the glucosyl C6 position were designed, synthesized and evaluated for their inhibitory activity against human SGLT2 (hSGLT2). Compounds with good hSGLT2 inhibition were further investigated to determine their selectivity over hSGLT1. Of these, five representative aryl C-glycosides were chosen for pharmacokinetic analysis. Oxime 2a was determined to have the most promising pharmacokinetic properties and was selected for in vivo glucosuria and plasma glucose level studies, which found it to exhibit comparable efficacy to dapagliflozin (1). Furthermore, 2a was not found to exhibit either significant cytotoxicity (CC50 > 50 μM) or human ether-a-go-go related gene (hERG) inhibition (2% inhibition at 10 μM). Taken together, these efforts culminated in the discovery of oxime 2a as a potential SGLT2 inhibitor
    日期: 2018-01-01
    關聯: European Journal of Medicinal Chemistry. 2018 Jan 1;143:611-620.
    Link to: http://dx.doi.org/10.1016/j.ejmech.2017.11.019
    JIF/Ranking 2023: http://gateway.webofknowledge.com/gateway/Gateway.cgi?GWVersion=2&SrcAuth=NHRI&SrcApp=NHRI_IR&KeyISSN=0223-5234&DestApp=IC2JCR
    Cited Times(WOS): https://www.webofscience.com/wos/woscc/full-record/WOS:000428216700051
    Cited Times(Scopus): http://www.scopus.com/inward/record.url?partnerID=HzOxMe3b&scp=85036563478
    显示于类别:[李靜琪] 期刊論文
    [趙宇生(2002-2013)] 期刊論文
    [陳炯東] 期刊論文
    [葉燈光] 期刊論文

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