國家衛生研究院 NHRI:Item 3990099045/5362

NHRI > Institute of Biotechnology and Pharmaceutical Research > Yu-Sheng Chao(2002-2013) > Periodical Articles > Item 3990099045/5362

Please use this identifier to cite or link to this item: http://ir.nhri.org.tw/handle/3990099045/5362

Title:	Discovery of novel N -Beta- d -Xylosylindole derivatives as sodium-dependent glucose cotransporter 2 (SGLT2) inhibitors for the management of hyperglycemia in diabetes
Other Titles:	Discovery of novel N -β- d -Xylosylindole derivatives as sodium-dependent glucose cotransporter 2 (SGLT2) inhibitors for the management of hyperglycemia in diabetes
Authors:	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
Contributors:	Institute of Biotechnology and Pharmaceutical Research
Abstract:	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.
Date:	2011-01-13
Relation:	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
Appears in Collections:	[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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