Discovery of a Potent, Selective Renal Sodium-Dependent Glucose Cotransporter 2 (SGLT2) Inhibitor (HSK0935) for the Treatment of Type 2 Diabetes
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https://figshare.com/articles/dataset/Discovery_of_a_Potent_Selective_Renal_Sodium-Dependent_Glucose_Cotransporter_2_SGLT2_Inhibitor_HSK0935_for_the_Treatment_of_Type_2_Diabetes/4980599
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资源简介:
A new class of potent and highly
selective SGLT2 inhibitors is
disclosed. Compound 31 (HSK0935) demonstrated excellent
hSGLT2 inhibition of 1.3 nM and a high hSGLT1/hSGLT2 selectivity of
843-fold. It showed robust urinary glucose excretion in Sprague–Dawley
(SD) rats and affected more urinary glucose excretion in Rhesus monkeys.
Finally, an efficient synthetic route has been developed featuring
a ring-closing cascade reaction to incorporate a double ketal 1-methoxy-6,8-dioxabicyclo[3.2.1]octane
ring system.
创建时间:
2017-05-05



