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ACS Med Chem Lett. 2013 Nov 13;5(1):51-5. doi: 10.1021/ml400339b. eCollection 2014 Jan 9.

Novel Indole-N-glucoside, TA-1887 As a Sodium Glucose Cotransporter 2 Inhibitor for Treatment of Type 2 Diabetes.

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Medicinal Chemistry Research Laboratories, Pharmacology Research Laboratories, and DMPK Research Laboratories, Mitsubishi Tanabe Pharma Corporation , 2-2-50 Kawagishi, Toda, Saitama 335-8505, Japan.


Inhibition of the renal sodium glucose cotransporter (SGLT) increases urinary glucose excretion (UGE) and thus reduces blood glucose levels during hyperglycemia. To explore the potential of new antihyperglycemic agents, we synthesized and determined the human SGLT2 (hSGLT2) inhibitory potential of novel substituted 3-benzylindole-N-glucosides 6. Optimization of 6 resulted in the discovery of 3-(4-cyclopropylbenzyl)-4-fluoroindole-N-glucoside 6a-4 (TA-1887), a highly potent and selective hSGLT2 inhibitor, with pronounced antihyperglycemic effects in high-fat diet-fed KK (HF-KK) mice. Our results suggest the potential of indole-N-glucosides as novel antihyperglycemic agents through inhibition of renal SGLT2.


TA-1887; Type 2 diabetes; antihyperglycemic effect; indole-N-glucoside; sodium glucose cotransporter 2 inhibitor; urinary glucose excretion

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