Synthesis and biological evaluation of novel dioxa-bicycle C-aryl glucosides as SGLT2 inhibitors. (8th February 2016)

• Record Type: Journal Article
• Authors: Yan, Qi; Ding, Ning; Li, Yingxia
• Is Part Of: Carbohydrate research. Volume 421(2016)
• Page Start: 1
• Page End: 8
• Publication Date: 2016-02-08
• Subjects: SGLT2 -- C-aryl glucosides -- Diabetes; Carbohydrates -- Periodicals; Chemistry, Organic -- Periodicals; Biochemistry -- Periodicals; Carbohydrates -- Periodicals; Chimie organique -- Périodiques; Glucides -- Périodiques; Biochemistry; Carbohydrates; Chemistry, Organic; Periodicals; Electronic journals; 507.78
• DOI: 10.1016/j.carres.2015.10.011
• Languages: English
• ISSNs: 0008-6215

Abstract

Highlights: Novel dioxa-bicycle C-aryl glucosides were synthesized. SGLT2 inhibitory activities were evaluated. The most potent compound showed an IC50 value of 714 nM. Graphical Abstract: 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.