التفاصيل البيبلوغرافية
| العنوان: |
ortho-Substituted C-aryl glucosides as highly potent and selective renal sodium-dependent glucose co-transporter 2 (SGLT2) inhibitors |
| المؤلفون: |
Xu, Baihua1,2,3 baihuaxu@egretpharma.com, Feng, Yan2, Lv, Binhua1,2,3, Xu, Ge2, Zhang, Lili2, Du, Jiyan2, Peng, Kun2, Xu, Min2, Dong, Jiajia2, Zhang, Wenbin2, Zhang, Ting2, Zhu, Liangcheng2, Ding, Haifeng2, Sheng, Zelin2, Welihinda, Ajith4, Seed, Brian4, Chen, Yuanwei1,2 chenyw@cioc.ac.cn |
| المصدر: |
Bioorganic & Medicinal Chemistry. Jun2010, Vol. 18 Issue 12, p4422-4432. 11p. |
| مصطلحات موضوعية: |
*GLUCOSIDES, *GLUCOSE, *AROMATIC amines, *PHENYL compounds, *BLOOD sugar, *URINALYSIS, *DIABETES |
| مستخلص: |
Abstract: A series of 2-substituted C-aryl glucosides have been synthesized and evaluated for inhibition of hSGLT1 and hSGLT2. Introduction of an appropriate ortho substituent at the proximal phenyl ring adjacent to the glycosidic bond was found to improve SGLT2 inhibitory activity and dramatically increase selectivity for hSGLT2 over hSGLT1. Selected compounds were investigated for in vivo efficacy. [Copyright &y& Elsevier] |
| قاعدة البيانات: |
Academic Search Index |