1396259-53-2Relevant academic research and scientific papers
Synthesis and biological evaluation of novel C-indolylxylosides as sodium-dependent glucose co-transporter 2 inhibitors
Yao, Chun-Hsu,Song, Jen-Shin,Chen, Chiung-Tong,Yeh, Teng-Kuang,Hsieh, Tsung-Chih,Wu, Szu-Huei,Huang, Chung-Yu,Huang, Yu-Lin,Wang, Min-Hsien,Liu, Yu-Wei,Tsai, Chi-Hui,Kumar, Chidambaram Ramesh,Lee, Jinq-Chyi
, p. 32 - 38,7 (2020/07/31)
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.
