Synthesis and biological evaluation of novel dioxa-bicycle C-aryl glucosides as SGLT2 inhibitors

Qi Yan; Ning Ding; Yingxia Li

doi:10.1016/j.carres.2015.10.011

Synthesis and biological evaluation of novel dioxa-bicycle C-aryl glucosides as SGLT2 inhibitors

Carbohydr Res. 2016 Feb 8:421:1-8. doi: 10.1016/j.carres.2015.10.011. Epub 2015 Dec 7.

Authors

Qi Yan¹, Ning Ding¹, Yingxia Li²

Affiliations

¹ School of Pharmacy, Fudan University, Shanghai 201203, China.
² School of Pharmacy, Fudan University, Shanghai 201203, China. Electronic address: liyx417@fudan.edu.cn.

PMID: 26735747
DOI: 10.1016/j.carres.2015.10.011

Abstract

A series of novel C-aryl glucosides containing dioxa-bicycle were synthesized and evaluated for inhibition activity against hSGLT2. Among the compounds tested, compound 6a showed moderate SGLT2 inhibition activities at 700 nM. The results could benefit the discovery of new SGLT2 inhibitors.

Keywords: C-aryl glucosides; Diabetes; SGLT2.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Animals
CHO Cells
Cricetulus
Glucosides / chemical synthesis*
Glucosides / pharmacology
Humans
Hypoglycemic Agents / chemical synthesis*
Hypoglycemic Agents / pharmacology
Molecular Structure
Sodium-Glucose Transporter 2
Sodium-Glucose Transporter 2 Inhibitors*
Structure-Activity Relationship

Substances

Glucosides
Hypoglycemic Agents
SLC5A2 protein, human
Sodium-Glucose Transporter 2
Sodium-Glucose Transporter 2 Inhibitors