C-Aryl glucoside SGLT2 inhibitors containing a biphenyl motif as potential anti-diabetic agents. Issue 14 (15th July 2015)

• Record Type: Journal Article
• Authors: Ding, Yuyang; Mao, Liufeng; Xu, Dengfeng; Xie, Hui; Yang, Ling; Xu, Hongjiang; Geng, Wenjun; Gao, Yong; Xia, Chunguang; Zhang, Xiquan; Meng, Qingyi; Wu, Donghai; Zhao, Junling; Hu, Wenhui
• Is Part Of: Bioorganic & medicinal chemistry letters. Volume 25:Issue 14(2015)
• Page Start: 2744
• Page End: 2748
• Publication Date: 2015-07-15
• Subjects: SGLT2 inhibitor -- Type 2 diabetes -- C-Aryl glucoside -- Biphenyl; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1016/j.bmcl.2015.05.040
• Languages: English
• ISSNs: 0960-894X

Abstract

Graphical abstract: Abstract: A series of highly active C -aryl glucoside SGLT2 inhibitors containing a biphenyl motif were designed and synthesized for biological evaluation. Among the compounds tested, compound16l demonstrated high inhibitory activity against SGLT2 (IC50 = 1.9 nM) with an excellent pharmacokinetic profile. Further study indicated that the in vivo efficacy of compound16l was comparable to that of dapagliflozin, suggesting that further development would be worthwhile.