國家衛生研究院 NHRI:Item 3990099045/5362
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    題名: Discovery of novel N -Beta- d -Xylosylindole derivatives as sodium-dependent glucose cotransporter 2 (SGLT2) inhibitors for the management of hyperglycemia in diabetes
    其他題名: Discovery of novel N -β- d -Xylosylindole derivatives as sodium-dependent glucose cotransporter 2 (SGLT2) inhibitors for the management of hyperglycemia in diabetes
    作者: Yao, CH;Song, JS;Chen, CT;Yeh, TK;Hung, MS;Chang, CC;Liu, YW;Yuan, MC;Hsieh, CJ;Huang, CY;Wang, MH;Chiu, CH;Hsieh, TC;Wu, SH;Hsiao, WC;Chu, KF;Tsai, CH;Chao, YS;Lee, JC
    貢獻者: Institute of Biotechnology and Pharmaceutical Research
    摘要: A novel series of N-linked β-d-xylosides were synthesized and evaluated for inhibitory activity against sodium-dependent glucose cotransporter 2 (SGLT2) in a cell-based assay. Of these, the 4-chloro-3-(4-cyclopropylbenzyl) -1-(β-d-xylopyranosyl)-1H-indole 19m was found to be the most potent inhibitor, with an EC<sub>50</sub> value similar to that of the natural SGLT2 inhibitor phlorizin. Further studies in Sprague-Dawley (SD) rats indicated that 19m significantly increased urine glucose excretion in a dose-dependent manner with oral administration. The antihyperglycemic effect of 19m was also observed in streptozotocin (STZ) induced diabetic SD rats. These results described here are a good starting point for further investigations into N-glycoside SGLT2 inhibitors.
    日期: 2011-01-13
    關聯: Journal of Medicinal Chemistry. 2011 Jan 13;54(1):166-178.
    Link to: http://dx.doi.org/10.1021/jm101072y
    JIF/Ranking 2023: http://gateway.webofknowledge.com/gateway/Gateway.cgi?GWVersion=2&SrcAuth=NHRI&SrcApp=NHRI_IR&KeyISSN=0022-2623&DestApp=IC2JCR
    Cited Times(WOS): https://www.webofscience.com/wos/woscc/full-record/WOS:000285818000013
    Cited Times(Scopus): http://www.scopus.com/inward/record.url?partnerID=HzOxMe3b&scp=78651112964
    顯示於類別:[趙宇生(2002-2013)] 期刊論文
    [李靜琪] 期刊論文
    [洪明秀] 期刊論文
    [葉燈光] 期刊論文
    [陳炯東] 期刊論文

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