國家衛生研究院 NHRI:Item 3990099045/6548
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    题名: Synthesis and biological evaluation of novel C-indolylxylosides as sodium-dependent glucose co-transporter 2 inhibitors
    作者: Yao, CH;Song, JS;Chen, CT;Yeh, TK;Hsieh, TC;Wu, SH;Huang, CY;Huang, YL;Wang, MH;Liu, YW;Tsai, CH;Kumar, CR;Lee, JC
    贡献者: Institute of Biotechnology and Pharmaceutical Research
    摘要: Sodium-dependent glucose co-transporter 2 (SGLT2) inhibitors are the current focus on the indication for the management of hyperglycemia in diabetes. Here, a novel series of C-linked indolylxyloside-based inhibitors of SGLT2 has been discovered. Structure-activity relationship studies revealed that substituents at the 7-position of the indole moiety and a p-cyclopropylphenyl group in the distal position were necessary for optimum inhibitory activity. The pharmacokinetic study demonstrates that the most potent compound 1i is metabolically stable with a low clearance in rats. In further efficacy study, 1i is found to significantly lower blood glucose levels of streptozotocin (STZ)-induced diabetic rats.
    日期: 2012-09
    關聯: European Journal of Medicinal Chemistry. 2012 Sep;55:32-38.
    Link to: http://dx.doi.org/10.1016/j.ejmech.2012.06.053
    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:000309494100004
    Cited Times(Scopus): http://www.scopus.com/inward/record.url?partnerID=HzOxMe3b&scp=84865785537
    显示于类别:[李靜琪] 期刊論文
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