國家衛生研究院 NHRI:Item 3990099045/6548

NHRI > Institute of Biotechnology and Pharmaceutical Research > Jinq-Chyi Lee > Periodical Articles > Item 3990099045/6548

Please use this identifier to cite or link to this item: http://ir.nhri.org.tw/handle/3990099045/6548

Title:	Synthesis and biological evaluation of novel C-indolylxylosides as sodium-dependent glucose co-transporter 2 inhibitors
Authors:	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
Contributors:	Institute of Biotechnology and Pharmaceutical Research
Abstract:	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.
Date:	2012-09
Relation:	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
Appears in Collections:	[Jinq-Chyi Lee] Periodical Articles [Teng-Kuang Yeh] Periodical Articles [Chiung-Tong Chen] Periodical Articles

Files in This Item:

File	Description	Size	Format
PUB2012072608.pdf		493Kb	Adobe PDF	698	View/Open

Loading...