2. Academic Validation
  3. Synthesis and biological evaluation of novel C-indolylxylosides as sodium-dependent glucose co-transporter 2 inhibitors

Synthesis and biological evaluation of novel C-indolylxylosides as sodium-dependent glucose co-transporter 2 inhibitors

  • Eur J Med Chem. 2012 Sep:55:32-8. doi: 10.1016/j.ejmech.2012.06.053.
Chun-Hsu Yao 1,  Jen-Shin Song,  Chiung-Tong Chen,  Teng-Kuang Yeh,  Tsung-Chih Hsieh,  Szu-Huei Wu,  Chung-Yu Huang,  Yu-Lin Huang,  Min-Hsien Wang,  Yu-Wei Liu,  Chi-Hui Tsai,  Chidambaram Ramesh Kumar,  Jinq-Chyi Lee
Affiliations

Affiliation

  • 1 Institute of Biotechnology and Pharmaceutical Research, National Health Research Institutes, 35 Keyan Road, Zhunan Town, Miaoli County 35053, Taiwan.
PMID: 22818040 DOI: 10.1016/j.ejmech.2012.06.053
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.

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