| Literature DB >> 26026363 |
Yuyang Ding1, Liufeng Mao1, Dengfeng Xu1, Hui Xie1, Ling Yang2, Hongjiang Xu2, Wenjun Geng2, Yong Gao2, Chunguang Xia2, Xiquan Zhang2, Qingyi Meng2, Donghai Wu1, Junling Zhao3, Wenhui Hu4.
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, compound 16l demonstrated high inhibitory activity against SGLT2 (IC50=1.9 nM) with an excellent pharmacokinetic profile. Further study indicated that the in vivo efficacy of compound 16l was comparable to that of dapagliflozin, suggesting that further development would be worthwhile.Entities:
Keywords: Biphenyl; C-Aryl glucoside; SGLT2 inhibitor; Type 2 diabetes
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Year: 2015 PMID： 26026363 DOI： 10.1016/j.bmcl.2015.05.040
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823