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Bioorg Med Chem Lett. 2011 Aug 1;21(15):4465-70. doi: 10.1016/j.bmcl.2011.06.032. Epub 2011 Jun 16.

C-aryl glucosides substituted at the 4'-position as potent and selective renal sodium-dependent glucose co-transporter 2 (SGLT2) inhibitors for the treatment of type 2 diabetes.

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Chengdu Institute of Organic Chemistry, Chinese Academy of Sciences, Chengdu, Sichuan, PR China.


A series of C-aryl glucosides with various substituents at the 4'-position of the distal aryl ring have been synthesized and evaluated for inhibition of hSGLT1 and hSGLT2. Introduction of alkyl or alkoxy substituents at the 4'-position was found to improve SGLT2 potency, whereas introduction of a hydrophilic group at this position was deleterious. Compounds with alkoxy-, cycloalkoxy- or cycloalkenyloxy-ethoxy scaffolds exhibited good inhibitory activity and high selectivity toward SGLT2. Selected compounds were investigated for in vivo efficacy.

[Indexed for MEDLINE]

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